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PI3K
PI3K製品
- All (119)
- PI3K阻害剤 (110)
- PI3K活性剤(6)
- PI3Kモジュレータ(3)
- 新製品
| 製品コード | 製品名称 | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
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| S1105 | LY294002 | LY294002 (SF 1101, NSC 697286) は人工的に合成した分子としては初めての PI3Kα/δ/β 阻害剤であり、IC50 はそれぞれ 0.5 μM/ 0.57 μM/ 0.97 μM です。溶液中でウォルトマンニン (wortmannin) よりも安定しています。クラス I PI3K および PI3K 関連キナーゼだけでなく、一見 PI3K ファミリーには無関係にある新規のターゲットにも結合します。LY294002 は CK2 阻害剤でもあり、IC50 は 98 nM です。また LY294002 はオートファゴソーム (autophagosome) の形成をブロックする一方で、DNA-PKｃｓ を非特異的に阻害することによりオートファジー (autophagy) を活性化し、アポトーシス (apoptosis) を誘導します。 |
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| S2767 | 3-MA (3-Methyladenine) | 3-MA (3-Methyladenine) is a selective PI3K inhibitor for Vps34 and PI3Kγ with IC50 of 25 μM and 60 μM in HeLa cells; blocks class I PI3K consistently, whereas suppression of class III PI3K is transient, and also blocks autophagosome formation. Solutions are unstable and should be fresh-prepared. |
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| S1009 | Dactolisib (BEZ235) | Dactolisib (BEZ235, NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell. Dactolisib induces autophagy and suppresses HIV-1 replication. Phase 2. |
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| S1065 | Pictilisib (GDC-0941) | Pictilisib (GDC-0941, RG7321) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM in cell-free assays, with modest selectivity against p110β (11-fold) and p110γ (25-fold). Pictilisib (GDC-0941) induces autophagy and apoptosis. Phase 2. |
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| S2758 | Wortmannin | Wortmannin is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Wortmannin blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays. Wortmannin also inhibits PLK1 activity. |
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| S2226 | Idelalisib (CAL-101) | Idelalisib (CAL-101) is a selective p110δ inhibitor with IC50 of 2.5 nM in cell-free assays; shown to have 40- to 300-fold greater selectivity for p110δ than p110α/β/γ, and 400- to 4000-fold more selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR. Idelalisib also stimulates autophagy. |
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| S2247 | Buparlisib (BKM120) | Buparlisib (BKM120, NVP-BKM120) is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM in cell-free assays, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ. Buparlisib induces apoptosis. Phase 2. |
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| S2638 | NU7441 (KU-57788) | NU7441 (KU-57788) is a highly potent and selective DNA-PK inhibitor with IC50 of 14 nM and also inhibits mTOR and PI3K with IC50 of 1.7 μM and 5 μM in cell-free assays, respectively. It reduces the frequency of NHEJ while increasing the rate of HDR following Cas9-mediated DNA cleavage. |
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| S2814 | Alpelisib (BYL719) | アルペリシブ (Alpelisib (BYL719)) はPI3Kβ/γ/δ に対する影響が最小限の、強力かつ選択的な PI3Kα 阻害剤(無細胞アッセイで IC50 = 5 nM) です。 臨床フェーズ2。 |
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| S1038 | PI-103 | PI-103 is a multi-targeted PI3K inhibitor for p110α/β/δ/γ with IC50 of 2 nM/3 nM/3 nM/15 nM in cell-free assays, less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM. PI-103 induces apoptosis in murine T-cell Lymphoma. |
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| S1169 | TGX-221 | TGX-221 is a p110β-specific inhibitor with IC50 of 5 nM in a cell-free assay, 1000-fold more selective for p110β than p110α. |
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| S1072 | ZSTK474 | ZSTK474 inhibits class I PI3K isoforms with IC50 of 37 nM in a cell-free assay, mostly PI3Kδ. Phase1/2. |
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| S2893 | NU7026 | NU7026 (LY293646) is a potent DNA-PK inhibitor with IC50 of 0.23 μM in cell-free assays, 60-fold selective for DNA-PK than PI3K and inactive against both ATM and ATR. NU7026 enhances G2/M cell arrest and apoptosis. |
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| S2658 | Omipalisib (GSK2126458) | Omipalisib (GSK2126458, GSK458) is a highly selective and potent inhibitor of p110α/β/δ/γ, mTORC1/2 with Ki of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM in cell-free assays, respectively. Omipalisib induces autophagy. Phase 1. |
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| S2636 | A66 | A66 is a potent and specific p110α inhibitor with IC50 of 32 nM in a cell-free assay, >100 fold selectivity for p110α over other class-I PI3K isoforms. |
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| S2743 | PF-04691502 | PF-04691502 (PF4691502) is an ATP-competitive PI3K(α/β/δ/γ)/mTOR dual inhibitor with Ki of 1.8 nM/2.1 nM/1.6 nM/1.9 nM and 16 nM in cell-free assays, little activity against either Vps34, AKT, PDK1, p70S6K, MEK, ERK, p38, or JNK. PF-04691502 induces apoptosis. Phase 2. |
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| S7028 | Duvelisib (IPI-145) | Duvelisib (IPI-145, INK1197) is a novel and selective PI3K δ/γ inhibitor with Ki and IC50 of 23 pM/243 pM and 1 nM/50 nM in cell-free assays, highly selective for PI3K δ/γ than other protein kinases. Phase 3. |
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| S2802 | Copanlisib | Copanlisib is a potent pan-class I PI3K with IC50 of 0.5, 3.7, 6.4, and 0.7 nM in cell-free assays for PI3Kα/β/γ/δ , respectively. Phase 3.This product has poor solubility, animal experiments are available, cell experiments please choose carefully! |
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| S1205 | PIK-75 HCl | PIK-75 HCl is a p110α inhibitor with IC50 of 5.8 nM (200-fold more potently than p110β), isoform-specific mutants at Ser773, and also potently inhibits DNA-PK with IC50 of 2 nM in cell-free assays. |
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| S1268 | IC-87114 | IC-87114 is a selective PI3Kδ inhibitor with IC50 of 0.5 μM in a cell-free assay, 58-fold more selective for PI3Kδ than PI3Kγ, and over 100-fold more selective than PI3Kα/β. |
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| S2391 | Quercetin | Quercetin, a natural flavonoid present in vegetables, fruit and wine, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4-5.4 μM. Quercetin induces mitophagy, apoptosis and protective autophagy. Phase 4. |
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| S7865 | 740 Y-P (PDGFR 740Y-P) | 740 Y-P (PDGFR 740Y-P, 740YPDGFR) is a cell-permeable phosphopeptide activator of PI3K. | ||
| S2759 | Fimepinostat (CUDC-907) | CUDC-907 is a dual PI3K and HDAC inhibitor for PI3Kα and HDAC1/2/3/10 with IC50 of 19 nM and 1.7 nM/5 nM/1.8 nM/2.8 nM, respectively. CUDC-907 induces cell cycle arrest and apoptosis in breast cancer cells. Phase 1. |
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| S1410 | AS-605240 | AS-605240 selectively inhibits PI3Kγ with IC50 of 8 nM, over 30-fold and 7.5-fold more selective for PI3Kγ than PI3Kδ/β and PI3Kα in cell-free assays, respectively. |
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| S1362 | Rigosertib (ON-01910) | Rigosertib (ON-01910) is a non-ATP-competitive inhibitor of PLK1 with IC50 of 9 nM in a cell-free assay. It shows 30-fold greater selectivity against Plk2 and no activity to Plk3. Rigosertib inhibits PI3K/Akt pathway and activates oxidative stress signals. Rigosertib induces apoptosis in various cancer cells. Phase 3. |
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| S7103 | Taselisib (GDC 0032) | Taselisib (GDC 0032, RG7604) is a potent, next-generation β isoform-sparing PI3K inhibitor targeting PI3Kα/δ/γ with Ki of 0.29 nM/0.12 nM/0.97nM, >10 fold selective over PI3Kβ. | ||
| S2696 | Apitolisib (GDC-0980) | Apitolisib (GDC-0980, RG7422, GNE 390) is a potent, class I PI3K inhibitor for PI3Kα/β/δ/γ with IC50 of 5 nM/27 nM/7 nM/14 nM in cell-free assays, respectively. Also a mTOR inhibitor with Ki of 17 nM in a cell-free assay, and highly selective versus other PIKK family kinases. Apitolisib activates autophagy and apoptosis simultaneously in pancreatic cancer cells. Phase 2. |
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| S7682 | SAR405 | SAR405 is a low-molecular-mass kinase inhibitor of PIK3C3/Vps34 (KD 1.5 nM) showing high selectivity and not be active up to 10 μM on class I and class II PI3Ks as well as on mTOR. SAR405 prevents autophagy and synergizes with MTOR (mechanistic target of rapamycin) inhibition in tumor cells. |
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| S7980 | VPS34-IN1 | Vps34-IN1 is a potent and highly selective Vps34 inhibitor with IC50 of 25 nM invitro,which does not significantly inhibit the isoforms of class I as well as class II PI3Ks. Vps34-IN1 modulates autophagy. |
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| S1187 | PIK-90 | PIK-90 is a PI3Kα/γ/δ inhibitor with IC50 of 11 nM/18 nM/58 nM, respectively, less potent to PI3Kβ. |
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| S1462 | AZD6482 | AZD6482 (KIN-193) is a PI3Kβ inhibitor with IC50 of 10 nM, 8-, 87- and 109-fold more selective to PI3Kβ than PI3Kδ, PI3Kα and PI3Kγ in cell-free assays. Phase 1. |
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| S2628 | Gedatolisib (PKI-587) | Gedatolisib (PF-05212384, PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ and mTOR with IC50 of 0.4 nM, 5.4 nM and 1.6 nM in cell-free assays, respectively. Phase 2. |
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| S2671 | AS-252424 | AS-252424 is a novel, potent PI3Kγ inhibitor with IC50 of 30 nM in a cell-free assay with 30-fold selectivity for PI3Kγ than PI3Kα, and low inhibitory activity towards PI3Kδ/β. |
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| S7356 | HS-173 | HS-173 is a potent PI3Kα inhibitor with IC50 of 0.8 nM. |
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| S8330 | Eganelisib (IPI-549) | Eganelisib (IPI-549) is a potent inhibitor of PI3K-γ with >100-fold selectivity over other lipid and protein kinases. The biochemical IC50 for PI3K-γ is 16 nM. | ||
| S7683 | PIK-III | PIK-III (VPS34-IN2), which is a selective inhibitor of VPS34 enzymatic activity, inhibits autophagy and de novo lipidation of LC3 and leads to the stabilization of autophagy substrates. |
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| S7016 | VS-5584 (SB2343) | VS-5584 (SB2343) is a potent and selective dual PI3K/mTOR inhibitor for mTOR, PI3Kα/β/δ/γ with IC50 of 3.4 nM and 2.6-21 nM, respectively. Phase 1. |
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| S8002 | GSK2636771 | GSK2636771 is a potent, orally bioavailable and selective inhibitor of PI3Kβ with >900-fold selectivity over PI3Kα/PI3Kγ and >10-fold over PI3Kδ. Sensitive to PTEN null cell lines. |
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| S1219 | YM201636 | YM201636 is a selective PIKfyve inhibitor with IC50 of 33 nM, less potent to p110α and insensitive to Fabl (yeast orthologue). YM-201636 suppresses the growth of liver cancer via the induction of autophagy. |
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| S7694 | AZD8186 | AZD8186 is a potent and selective inhibitor of PI3Kβ and PI3Kδ with IC50 of 4 nM and 12 nM, respectively. Phase 1. | ||
| S1360 | GSK1059615 | GSK1059615 is a dual inhibitor of PI3Kα/β/δ/γ (reversible) and mTOR with IC50 of 0.4 nM/0.6 nM/2 nM/5 nM and 12 nM, respectively. Phase 1. |
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| S7645 | Pilaralisib (XL147) | Pilaralisib (XL147) is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ with IC50 of 39 nM/36 nM/23 nM in cell-free assays, less potent to PI3Kβ. Phase 1/2. |
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| S1352 | TG100-115 | TG100-115 is a PI3Kγ/δ inhibitor with IC50 of 83 nM/235 nM, with little effect on PI3Kα/β. Phase 1/2. |
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| S7018 | CZC24832 | CZC24832 is the first selective PI3Kγ inhibitor with IC50 of 27 nM, with 10-fold selectivity over PI3Kβ and >100-fold selectivity over PI3Kα and PI3Kδ. |
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| S7646 | Voxtalisib (XL765) | Voxtalisib (SAR245409, XL765) is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR. Phase 1/2. |
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| S1118 | XL147 analogue | XL147 analogue (SAR245408) is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ with IC50 of 39 nM/36 nM/23 nM in cell-free assays, less potent to PI3Kβ. XL147 analogue induces apoptosis. Phase 1/2. |
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| S2681 | AS-604850 | AS-604850 is a selective, ATP-competitive PI3Kγ inhibitor with IC50 of 250 nM, over 80-fold selectivity for PI3Kγ than PI3Kδ/β, and 18-fold more selective for PI3Kγ than PI3Kα. |
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| S8045 | KU-0060648 | KU-0060648 is a dual inhibitor of DNA-PK and PI3Kα, PI3Kβ, PI3Kδ with IC50 of 8.6 nM and 4 nM, 0.5 nM, 0.1 nM respectively, less inhibition of PI3Kγ with IC50 of 0.59 μM. |
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| S2749 | BGT226 (NVP-BGT226) maleate | BGT226 (NVP-BGT226) is a novel class I PI3K/mTOR inhibitor for PI3Kα/β/γ with IC50 of 4 nM/63 nM/38 nM. Phase 1/2. |
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| S2347 | Quercetin Dihydrate | Quercetin (Sophoretin), a polyphenolic flavonoid found in a wide variety of plant-based foods, such as apples, onions, berries, and red wine, is utilized in many different cultures for their nervous system and anticancer effects. Quercetin (dihydrate), a natural flavonoid, is a stimulator of recombinant SIRT1 and a PI3K inhibitor with IC50s of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively. |
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| S8456 | VPS34 inhibitor 1 (Compound 19) | VPS34 inhibitor 1 (Compound 19, PIK-III analogue) is a potent and selective inhibitor of VPS34 with an IC50 of 15 nM. |
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| S8322 | Samotolisib (LY3023414) | LY3023414 (Samotolisib, GTPL8918) is an oral ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK. |
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| S1523 | Voxtalisib (XL765) Analogue | Voxtalisib (SAR245409, XL765) Analogue is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR. Phase 1/2. |
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| S8596 | Autophinib | Autophinib is a potent autophagy inhibitor with a novel chemotype with IC50 values of 90 and 40 nM for autophagy in starvation induced autophagy assay and rapamycin induced autophagy assay. The IC50 value for Vps34 is 19 nM in vitro. | ||
| S7813 | AMG319 | AMG319 is a potent and selective PI3Kδ inhibitor with IC50 of 18 nM, >47-fold selectivity over other PI3Ks. Phase 2. | ||
| S8194 | umbralisib (TGR-1202) | Umbralisib (TGR-1202, Rp-5264), a novel, next generation PI3Kδ inhibitor, inhibits PI3Kδ activity in enzyme and cell based assays with IC50 and EC50 values of 22.2 & 24.3 nM, respectively. | ||
| S7937 | Nemiralisib | Nemiralisib, also known as GSK-2269557, is a potent and selective PI3Kδ inhibitor(pKi = 9.9). | ||
| S2699 | CH5132799 | CH5132799 (MEN1611, PA799) inhibits class I PI3Ks, particularly PI3Kα with IC50 of 14 nM; less potent to PI3Kβδγ, while sensitive in PIK3CA mutations cell lines. Phase 1. |
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| S2739 | PKI-402 | PKI-402 is a potent dual pan-PI3K/mTOR inhibitor targeting PI3Kα/β/γ/δ and mTOR with IC50 of 2 nM/7 nM/16 nM/14 nM and 3 nM, respectively; also potent to PI3Kα mutants E545K and H1047R. | ||
| S8738 | Bimiralisib (PQR309) | Bimiralisib (PQR309) is a novel brain-penetrant dual PI3K/mTOR inhibitor with in vitro and in vivo antilymphoma activity. It displays excellent selectivity versus PI3K-related lipid kinases, protein kinases and unrelated targets. | ||
| S2870 | TG100713 | TG100713 is a pan-PI3K inhibitor against PI3Kγ, PI3Kδ, PI3Kα and PI3Kβ with IC50 of 50 nM, 24 nM, 165 nM and 215 nM, respectively. |
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| S9190 | Oroxin B | Oroxin B (Hypocretin-2), one of flavonoids isolated from traditional Chinese herbal medicine Oroxylum indicum (L.) Vent, selectively induces tumor-suppressive ER stress in malignant lymphoma cells and has antioxidant activity. Oroxin B significantly inhibits proliferation and induce apoptosis, which may be strongly associated with the inhibiting COX-2/VEGF and PTEN/PI3K/AKT signaling pathway in SMMC-7721 cells, Oroxin B potentially be used as a novel therapeutic agent for liver cancer.COX-2, VEGF, PI3K, and p-AKT expression levels is found to be downregulated, while PTEN was upregulated after Oroxin B treatment. | ||
| S8163 | Paxalisib (GDC-0084) | Paxalisib (GDC-0084, RG7666) is a brain penetrant inhibitor of PI3K and mTOR. | ||
| S8589 | SF2523 | SF2523 is a highly selective and potent inhibitor of PI3K with IC50 values of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively. | ||
| S8581 | Serabelisib (TAK-117) | Serabelisib (TAK-117, INK-1117, MLN-1117) is a potent and selective oral PI3Kα isoform inhibitor (IC50 of 21 nmol/L against PI3Kα) that has demonstrated > 100-fold selectivity relative to other class I PI3K family members (PI3Kβ/γ/δ) and mTOR, and a high degree of selectivity against many other kinase. | ||
| S8132 | Deguelin | Deguelin, a natural product isolated from plants in the Mundulea sericea family, is an PI3K/AKT Inhibitor. | ||
| S2227 | PIK-294 | PIK-294 is a highly selective p110δ inhibitor with IC50 of 10 nM, 1000-, 49- and 16-fold less potent to PI3Kα/β/γ, respectively. |
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| S8157 | GDC-0326 | GDC-0326 is a potent and selective inhibitor of PI3Kα with Ki value of 0.2 nM; remarkably selective over the other class I isoforms in enzymatic assays. | ||
| S7798 | GNE-317 | GNE-317 is a potent, brain-penetrant PI3K inhibitor. | ||
| S8668 | Inavolisib (GDC-0077) | Inavolisib (GDC-0077, RG6114, RO-7113755) is a potent selective inhibitor of PI3K alpha (PI3Kα) with an IC50 of 0.038 nM. GDC-0077 is >300-fold more selective for PI3K alpha over the other class I PI3K isoforms (beta, delta, and gamma) and >2000-fold more selective over PIK family members. GDC-0077 binds to the ATP binding site of PI3K and inhibits the phosphorylation of PIP2 to PIP3. | ||
| S7623 | PI-3065 | PI-3065 is a selective p110δ inhibitor with IC50 of 15 nM, >70-fold selectivity over other PI3K family members. | ||
| S7966 | AZD8835 | AZD8835 ia a novel mixed inhibitor of PI3Kα and PI3Kδ with IC50 of 6.2 nM and 5.7 nM, respectively, also with selectivity against PI3Kβ (IC50=431 nM) and PI3Kγ (IC50=90 nM). | ||
| S2682 | CAY10505 | CAY10505 is dehydroxyl of AS-252424, which is a PI3Kγ inhibitor with IC50 of 33 nM. |
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| S3238 | Resibufogenin | Resibufogenin (Bufogenin, Recibufogenin), a component of huachansu with anticancer effect, triggers necroptosis through upregulating receptor-interacting protein kinase 3 (RIP3) and phosphorylating mixed lineage kinase domain-like protein at Ser358. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression. | ||
| S3296 | Hispidulin | Hispidulin (Dinatin), an active natrual ingredient in a number of traditional Chinese medicinal herbs, exhibits inhibitory activity against the oncogenic protein kinase Pim-1 with IC50 of 2.71 μM. Hispidulin induces apoptosis through mitochondrial dysfunction and inhibition of P13k/Akt signalling pathway in HepG2 cancer cells. Hispidulin exerts anti-osteoporotic and bone resorption attenuating effects via activating the AMPK signaling pathway. | ||
| S0817 | SKI-V | SKI V is a noncompetitive and potent inhibitor of non-lipid sphingosine kinase with IC50 of 2 μM for GST-hSK. SKI-V also inhibits PI3K with IC50 of 6 μM for hPI3k. SKI-V decreases formation of the mitogenic second messenger sphingosine-1-phosphate (S1P) and induces apoptosis with antitumor activity. | ||
| S6541 | MTX-211 | MTX-211 is a first-in-class dual inhibitor of PI3K and EGFR kinase. | ||
| S8560 | Seletalisib (UCB-5857) | Seletalisib (UCB-5857) is a novel small-molecule inhibitor of PI3Kδ with an IC50 value of 12 nM and shows significant selectivity to PI3Kδ with respect to the other class I PI3K isoforms (between 24- and 303-fold). | ||
| S8752 | leniolisib (CDZ 173) | Leniolisib (CDZ 173) is a potent PI3Kδ selective inhibitor with biochemical IC50 values of 0.244, 0.424, 2.23 and 0.011 μM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively. | ||
| E2384 | (E)-Akt inhibitor-IV | (E)-Akt inhibitor-IV is a PI3K-Akt inhibitor, with potent cytotoxic. | ||
| S3785 | Notoginsenoside R1 | Notoginsenoside R1 (Sanchinoside R1) is the main ingredient with cardiovascular activity in Panax notoginseng. It inhibits TNF-α-induced PAI-1 overexpression via extracellular signal-related kinases (ERK1/2) and phosphatidylinositol 3-kinase (PI3K)/protein kinase B (PKB) signaling pathways. | ||
| S5978 | Gallein | Gallein (Pyrogallol phthalein) is an inhibitor of G protein βγ (G beta-gamma complex, Gβγ) subunit interaction with PI3 kinase. Gallein inhibits β-ionone effects and exhibits anti-tumor activity. Gallein can be used as a biological stain. | ||
| S3220 | Trigonelline | Trigonelline (Trigenolline) is a plant alkaloid and a major component of coffee and fenugreek with anti-degranulation, anti-diabetic, antioxidant, anti-inflammatory, and neuroprotective effects. Trigonelline inhibits FcεRI-mediated intracellular signaling pathways, such as phosphorylation of PLCγ1, PI3K, and Akt. Trigonelline (Trigenolline) also inhibits the microtubule formation in RBL-2H3 cells. | ||
| S8693 | Selective PI3Kδ Inhibitor 1 (compound 7n) | Selective PI3Kδ Inhibitor 1 (compound 7n) is an inhibitor of PI3Kδ with an IC50 of 0.9 nM and >1000-fold selectivity against other class I PI3K isoforms [PI3K α/γ/β=3670/1460/21300 nM]. | ||
| S7675 | PF-4989216 | PF-4989216 is a potent and selective PI3K inhibitor with IC50 of 2 nM, 142 nM, 65 nM, 1 nM, and 110 nM for p110α, p110β, p110γ, p110δ, and VPS34, respectively. | ||
| S6516 | GNE-477 | GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor with an IC50 of 4 nM for PI3Kα and Kiapp of 21 nM for mTOR. | ||
| S6517 | GNE-493 | GNE-493 (compound 5) is a potent, selective and orally available dual inhibitor of pan-PI3-kinase and mTOR with IC50 of 3.4 nM, 12 nM, 16 nM, 16 nM and 32 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR, respectively. | ||
| S2207 | PIK-293 | PIK-293 is a PI3K inhibitor, mostly for PI3Kδ with IC50 of 0.24 μM, 500-, 100- and 50-fold less potent to PI3Kα/β/γ, respectively. |
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| S3294 | Demethyl-Coclaurine | Demethyl-Coclaurine (Higenamine, Norcoclaurine), the key component of the Chinese herb aconite root, is a beta-2 adrenergic receptor (β2-AR) agonist. Demethyl-Coclaurine stimulates AKT phosphorylation and requires PI3K activation for the anti-apoptotic effect in cardiomyocytes. | ||
| E2947 | Recilisib | Recilisib (ON01210, EX-RAD) is a radioprotectant that activates the activity of AKT and PI3K in cells. It has been studied as prophylactic (use prior to radiation exposure) and therapeutic (after exposure to radiation) drug. | ||
| S4572 | Homosalate | Homosalate (HMS, Homomenthyl salicylate) is an organic ultraviolet filter used in most sunscreens but has been reported to be toxic to marine organisms. Homosalate aggravates the invasion of human trophoblast cells as well as regulates intracellular signaling pathways including PI3K/AKT and MAPK pathways. | ||
| S3224 | Cinobufagin | Cinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. Cinobufagin increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. Cinobufagin inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, Cinobufagin induces cell cycle arrest at the G2/M phase and apoptosis. | ||
| S7938 | GSK2292767 | GSK2292767 is a potent and selective PI3Kδ inhibitor. | ||
| S5554 | Lanatoside C | Lanatoside C is a cardiac glycoside with antiviral and anti-tumor activity. Lanatoside C induces G2/M cell cycle arrest and induces autophagy and apoptosis via attenuating MAPK, Wnt, JAK-STAT, and PI3K/AKT/mTOR signaling pathways. | ||
| E2375 | PI3K/mTOR Inhibitor-2 | PI3K/mTOR Inhibitor-2 is a potent dual pan-PI3K/mTOR inhibitor with antitumor activity. | ||
| S3243 | Zeaxanthin | Zeaxanthin, the carotenoid alcohol participates in the xanthophyll cycle, activates the extrinsic apoptosis pathway which induces apoptosis on uveal melanoma cells with IC50 value 40.8 µM. | ||
| S0947 | Cafestol | Cafestol is a natural diterpenes extracted from coffee beans. Cafestol induces apoptosis and regulates a variety of inflammatory mediators to reduce inflammation. Cafestol inhibits PI3K/Akt pathway. Cafestol also can reduce the production of ROS in the leukemia cell line HL60. | ||
| E2823 | PIK-108 | PIK-108 is a non-ATP competitive, allosteric p110β/p110δ selective inhibitor. | ||
| E0020 | Lupenone | Lupenone (Lup-20(29)-en-3-one, lupeone) is an isolated compound exhibiting anti-oxidative, anti-inflammation, and anti-diabetic activities. Lupenone can protect SH-SY5y cells against METH-induced neuronal apoptosis through the PI3K/Akt pathway. | ||
| E2366 | IHMT-PI3Kδ-372 | IHMT-PI3Kδ-372 is a potent and selective phosphatidylinositol 3-kinase δ (PI3Kδ) inhibitor with an IC50 of 14 nM in the biochemical assay | ||
| S8672 | Tenalisib | Tenalisib is a potent and selective dual PI3Kδ/γ inhibitor with IC50 values of 24.5 nM and 33.2 nM for PI3Kδ and PI3Kγ, respectively. Its selectivity over α and β isoforms are more than 300-fold and 100-fold, respectively. | ||
| S3309 | Solasodine | Solasodine (Purapuridine, Solancarpidine, Solasodin, Salasodine, Salasdine) is a poisonous alkaloid chemical compound that occurs in plants of the Solanaceae family. Solasodine reduces the mRNA level of matrix metalloproteinase-2 (MMP-2), MMP-9 and extracellular inducer of matrix metalloproteinase (EMMPRIN), but increases the expression of reversion-inducing cysteine-rich protein with kazal motifs (RECK). Solasodine downregulates oncogenic microRNA-21 (miR-21), which has been known to target RECK. Solasodine also reduces PI3K/Akt signaling pathways and downregulates expression of miR-21. | ||
| S9054 | Pectolinarin | Pectolinarin is a major compound in Cirsium setidens with anti-inflammatory activity. Pectolinarin inhibits secretion of IL-6 and IL-8, as well as the production of PGE2 and NO. Pectolinarin induces apoptosis via inactivation of the PI3K/Akt pathway. | ||
| S8948 | SRX3207 | SRX3207 is an orally active dual inhibitor of Syk-PI3K with IC50 of 39.9 nM, 31200 nM, 3070 nM, 3070 nM, 244 nM, 388 nM, 9790 nM for Syk, Zap70, BRD41, BRD42, PI3K alpha, PI3K delta, PI3K gamma, respectively. SRX3207 blocks tumor immunosuppression and increases anti-tumor immunity. | ||
| E2391 | α-Linolenic acid | α-Linolenic acid, an essential fatty acid isolated from seed oils, affects the process of thrombotic through the modulation of PI3K/Akt signaling, and possesses the anti-arrhythmic properties. | ||
| S5818 | acalisib (GS-9820) | Acalisib (GS-9820, CAL-120) is a highly selective and potent p110δ inhibitor (IC50 = 14 nM) with 114- to 400-fold selectivity over the other class I PI3K enzymes and no activity against Class II and III PI3K family members or other PI3K-related proteins including mTOR and DNA-PK. | ||
| S8917 | P110δ-IN-1 | P110δ-IN-1 is an oral, potent and selective inhibitor of Phosphatidylinositol 3-Kinase (PI3K) P110δ with IC50 of 0.6 nM in cellular assay. | ||
| S3575 | Zandelisib | Zandelisib(ME-401; PWT-143) is an orally bioavailable inhibitor of the phosphatidylinositide 3-kinase (PI3K). It selectively inhibits the delta isoform of PI3K (p110δ) and prevents the activation of the PI3K/AKT signaling pathway with an IC50 of 3.5 nM. It functions as an antineoplastic agent. | ||
| S6885 | Ailanthone | Ailanthone (AIL, Δ13-Dehydrochaparrinone), a natural anti-hepatocellular carcinoma (HCC) component in Ailanthus altissima, induces G0/G1-phase cell cycle arrest by decreasing expression of cyclins and CDKs and increases expression of p21 and p27. Ailanthone triggers DNA damage characterized by activation of the ATM/ATR pathway. Ailanthone induces apoptosis which is mitochondrion-mediated and involves the PI3K/AKT signaling pathway in Huh7 cells. Ailanthone is also a potent inhibitor of both full-length Androgen Receptor (AR-FL) and constitutively active truncated AR splice variants (AR-Vs, AR1-651) with IC50 of 69 nM and 309 nM, respectively. | ||
| S7335 | IPI-3063 | IPI-3063 is a potent and selective p110δ inhibitor with biochemical IC50 of 2.5 ± 1.2 nM and IC50 values for the other class I PI3K isoforms (p110α, p110β, p110γ) are at least 400-fold higher. | ||
| E0121 | Parsaclisib (INCB050465) | Parsaclisib (INCB050465, INCB-50465, IBI376) is a potent and highly selective PI3Kδ(PI3K delta) inhibitor with an IC50 of 1 nM at 1 mM ATP in biochemical assay and approximately 20,000-fold selectivity for PI3Kα, PI3Kβ, PI3Kγ and 57 other kinases. | ||
| E1579New | UCL-TRO-1938 | UCL-TRO-1938 is a potent allosteric activator of PI3Kα. UCL-TRO-1938 can induce cell proliferation and has cardioprotective and neural regeneration effects. | ||
| E1834New | iMDK | iMDK is a potent inhibitor of PI3K. It also inhibits the growth factor MDK (also known as midkine or MK). iMDK use along with a MEK inhibitor suppresses tumor growth of non-small cell lung cancer (NSCLC), including KRAS-mutant NSCLC and squamous NSCLC. | ||
| E2401 | SPP-86 | SPP-86, a potent and selective cell permeable inhibitor of rearranged during transfection (RET) tyrosine kinase with an IC50 of 8 nM, inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling, also inhibits RET-induced estrogen receptorα (ERα) phosphorylation in MCF7 cells. | ||
| E4680New | MTX-531 | MTX-531(NSC827271) is a first-in-class, potent and selective inhibitor of EGFR and PI3Kα with an IC50 of 14.7 nM and 6.4 nM, respectively. It may play a role in treating Head and Neck Squamous Cell Carcinoma (HSNCC), squamous lung cancers, and certain EGFR/PI3K-driven triple-negative breast cancers. | ||
| S5383 | Erucic acid | Erucic acid (cis-13-docosenoic acid) is a monounsaturated omega-9 fatty acid used as mineral oil and a precursor to biodiesel fuel. | ||
| S1273 | Amarogentin | Amarogentin (AG), a secoiridoid glycoside mainly extracted from Swertia and Gentiana roots, exhibits anti-oxidative, anti-tumour, and anti-diabetic activities. Amarogentin is an agonist for the bitter taste receptor TAS2R1 and inhibits in LAD-2 cells substance P-induced production of newly synthesized TNF-α. Amarogentin induces apoptosis in human gastric cancer cells (SNU-16) through G2/M cell cycle arrest and PI3K/Akt signalling pathway. Amarogentin (AG) interacts with the α2 subunit of AMP-activated protein kinase (AMPK) and activates the trimeric kinase with EC50 of 277 pM. |
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| S3241 | Loureirin A | Loureirin A is a flavonoid extracted from the red resin of the herbs of Dracaena cochinchinensis, which is known as Dragon's Blood. Loureirin A inhibits platelet activation by an impairment of PI3K/Akt signaling. Loureirin A inhibits Akt phosphorylation. | ||
| E0785 | YS-49 | YS-49 is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells, inhibits angiotensin II (Ang II)-stimulated proliferation of VSMCs via induction of heme oxygenase (HO)-1, also is an isoquinoline compound alkaloid, has a strong positive inotropic action through activation of cardiac β-adrenoceptors. | ||
| S1105 | LY294002 | LY294002 (SF 1101, NSC 697286) は人工的に合成した分子としては初めての PI3Kα/δ/β 阻害剤であり、IC50 はそれぞれ 0.5 μM/ 0.57 μM/ 0.97 μM です。溶液中でウォルトマンニン (wortmannin) よりも安定しています。クラス I PI3K および PI3K 関連キナーゼだけでなく、一見 PI3K ファミリーには無関係にある新規のターゲットにも結合します。LY294002 は CK2 阻害剤でもあり、IC50 は 98 nM です。また LY294002 はオートファゴソーム (autophagosome) の形成をブロックする一方で、DNA-PKｃｓ を非特異的に阻害することによりオートファジー (autophagy) を活性化し、アポトーシス (apoptosis) を誘導します。 |
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| S2767 | 3-MA (3-Methyladenine) | 3-MA (3-Methyladenine) is a selective PI3K inhibitor for Vps34 and PI3Kγ with IC50 of 25 μM and 60 μM in HeLa cells; blocks class I PI3K consistently, whereas suppression of class III PI3K is transient, and also blocks autophagosome formation. Solutions are unstable and should be fresh-prepared. |
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| S1009 | Dactolisib (BEZ235) | Dactolisib (BEZ235, NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell. Dactolisib induces autophagy and suppresses HIV-1 replication. Phase 2. |
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| S1065 | Pictilisib (GDC-0941) | Pictilisib (GDC-0941, RG7321) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM in cell-free assays, with modest selectivity against p110β (11-fold) and p110γ (25-fold). Pictilisib (GDC-0941) induces autophagy and apoptosis. Phase 2. |
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| S2758 | Wortmannin | Wortmannin is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Wortmannin blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays. Wortmannin also inhibits PLK1 activity. |
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| S2226 | Idelalisib (CAL-101) | Idelalisib (CAL-101) is a selective p110δ inhibitor with IC50 of 2.5 nM in cell-free assays; shown to have 40- to 300-fold greater selectivity for p110δ than p110α/β/γ, and 400- to 4000-fold more selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR. Idelalisib also stimulates autophagy. |
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| S2247 | Buparlisib (BKM120) | Buparlisib (BKM120, NVP-BKM120) is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM in cell-free assays, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ. Buparlisib induces apoptosis. Phase 2. |
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| S2638 | NU7441 (KU-57788) | NU7441 (KU-57788) is a highly potent and selective DNA-PK inhibitor with IC50 of 14 nM and also inhibits mTOR and PI3K with IC50 of 1.7 μM and 5 μM in cell-free assays, respectively. It reduces the frequency of NHEJ while increasing the rate of HDR following Cas9-mediated DNA cleavage. |
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| S2814 | Alpelisib (BYL719) | アルペリシブ (Alpelisib (BYL719)) はPI3Kβ/γ/δ に対する影響が最小限の、強力かつ選択的な PI3Kα 阻害剤(無細胞アッセイで IC50 = 5 nM) です。 臨床フェーズ2。 |
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| S1038 | PI-103 | PI-103 is a multi-targeted PI3K inhibitor for p110α/β/δ/γ with IC50 of 2 nM/3 nM/3 nM/15 nM in cell-free assays, less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM. PI-103 induces apoptosis in murine T-cell Lymphoma. |
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| S1169 | TGX-221 | TGX-221 is a p110β-specific inhibitor with IC50 of 5 nM in a cell-free assay, 1000-fold more selective for p110β than p110α. |
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| S1072 | ZSTK474 | ZSTK474 inhibits class I PI3K isoforms with IC50 of 37 nM in a cell-free assay, mostly PI3Kδ. Phase1/2. |
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| S2893 | NU7026 | NU7026 (LY293646) is a potent DNA-PK inhibitor with IC50 of 0.23 μM in cell-free assays, 60-fold selective for DNA-PK than PI3K and inactive against both ATM and ATR. NU7026 enhances G2/M cell arrest and apoptosis. |
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| S2658 | Omipalisib (GSK2126458) | Omipalisib (GSK2126458, GSK458) is a highly selective and potent inhibitor of p110α/β/δ/γ, mTORC1/2 with Ki of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM in cell-free assays, respectively. Omipalisib induces autophagy. Phase 1. |
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| S2636 | A66 | A66 is a potent and specific p110α inhibitor with IC50 of 32 nM in a cell-free assay, >100 fold selectivity for p110α over other class-I PI3K isoforms. |
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| S2743 | PF-04691502 | PF-04691502 (PF4691502) is an ATP-competitive PI3K(α/β/δ/γ)/mTOR dual inhibitor with Ki of 1.8 nM/2.1 nM/1.6 nM/1.9 nM and 16 nM in cell-free assays, little activity against either Vps34, AKT, PDK1, p70S6K, MEK, ERK, p38, or JNK. PF-04691502 induces apoptosis. Phase 2. |
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| S7028 | Duvelisib (IPI-145) | Duvelisib (IPI-145, INK1197) is a novel and selective PI3K δ/γ inhibitor with Ki and IC50 of 23 pM/243 pM and 1 nM/50 nM in cell-free assays, highly selective for PI3K δ/γ than other protein kinases. Phase 3. |
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| S2802 | Copanlisib | Copanlisib is a potent pan-class I PI3K with IC50 of 0.5, 3.7, 6.4, and 0.7 nM in cell-free assays for PI3Kα/β/γ/δ , respectively. Phase 3.This product has poor solubility, animal experiments are available, cell experiments please choose carefully! |
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| S1205 | PIK-75 HCl | PIK-75 HCl is a p110α inhibitor with IC50 of 5.8 nM (200-fold more potently than p110β), isoform-specific mutants at Ser773, and also potently inhibits DNA-PK with IC50 of 2 nM in cell-free assays. |
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| S1268 | IC-87114 | IC-87114 is a selective PI3Kδ inhibitor with IC50 of 0.5 μM in a cell-free assay, 58-fold more selective for PI3Kδ than PI3Kγ, and over 100-fold more selective than PI3Kα/β. |
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| S2391 | Quercetin | Quercetin, a natural flavonoid present in vegetables, fruit and wine, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4-5.4 μM. Quercetin induces mitophagy, apoptosis and protective autophagy. Phase 4. |
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| S2759 | Fimepinostat (CUDC-907) | CUDC-907 is a dual PI3K and HDAC inhibitor for PI3Kα and HDAC1/2/3/10 with IC50 of 19 nM and 1.7 nM/5 nM/1.8 nM/2.8 nM, respectively. CUDC-907 induces cell cycle arrest and apoptosis in breast cancer cells. Phase 1. |
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| S1410 | AS-605240 | AS-605240 selectively inhibits PI3Kγ with IC50 of 8 nM, over 30-fold and 7.5-fold more selective for PI3Kγ than PI3Kδ/β and PI3Kα in cell-free assays, respectively. |
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| S1362 | Rigosertib (ON-01910) | Rigosertib (ON-01910) is a non-ATP-competitive inhibitor of PLK1 with IC50 of 9 nM in a cell-free assay. It shows 30-fold greater selectivity against Plk2 and no activity to Plk3. Rigosertib inhibits PI3K/Akt pathway and activates oxidative stress signals. Rigosertib induces apoptosis in various cancer cells. Phase 3. |
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| S7103 | Taselisib (GDC 0032) | Taselisib (GDC 0032, RG7604) is a potent, next-generation β isoform-sparing PI3K inhibitor targeting PI3Kα/δ/γ with Ki of 0.29 nM/0.12 nM/0.97nM, >10 fold selective over PI3Kβ. | ||
| S2696 | Apitolisib (GDC-0980) | Apitolisib (GDC-0980, RG7422, GNE 390) is a potent, class I PI3K inhibitor for PI3Kα/β/δ/γ with IC50 of 5 nM/27 nM/7 nM/14 nM in cell-free assays, respectively. Also a mTOR inhibitor with Ki of 17 nM in a cell-free assay, and highly selective versus other PIKK family kinases. Apitolisib activates autophagy and apoptosis simultaneously in pancreatic cancer cells. Phase 2. |
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| S7682 | SAR405 | SAR405 is a low-molecular-mass kinase inhibitor of PIK3C3/Vps34 (KD 1.5 nM) showing high selectivity and not be active up to 10 μM on class I and class II PI3Ks as well as on mTOR. SAR405 prevents autophagy and synergizes with MTOR (mechanistic target of rapamycin) inhibition in tumor cells. |
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| S7980 | VPS34-IN1 | Vps34-IN1 is a potent and highly selective Vps34 inhibitor with IC50 of 25 nM invitro,which does not significantly inhibit the isoforms of class I as well as class II PI3Ks. Vps34-IN1 modulates autophagy. |
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| S1187 | PIK-90 | PIK-90 is a PI3Kα/γ/δ inhibitor with IC50 of 11 nM/18 nM/58 nM, respectively, less potent to PI3Kβ. |
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| S1462 | AZD6482 | AZD6482 (KIN-193) is a PI3Kβ inhibitor with IC50 of 10 nM, 8-, 87- and 109-fold more selective to PI3Kβ than PI3Kδ, PI3Kα and PI3Kγ in cell-free assays. Phase 1. |
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| S2628 | Gedatolisib (PKI-587) | Gedatolisib (PF-05212384, PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ and mTOR with IC50 of 0.4 nM, 5.4 nM and 1.6 nM in cell-free assays, respectively. Phase 2. |
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| S2671 | AS-252424 | AS-252424 is a novel, potent PI3Kγ inhibitor with IC50 of 30 nM in a cell-free assay with 30-fold selectivity for PI3Kγ than PI3Kα, and low inhibitory activity towards PI3Kδ/β. |
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| S7356 | HS-173 | HS-173 is a potent PI3Kα inhibitor with IC50 of 0.8 nM. |
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| S8330 | Eganelisib (IPI-549) | Eganelisib (IPI-549) is a potent inhibitor of PI3K-γ with >100-fold selectivity over other lipid and protein kinases. The biochemical IC50 for PI3K-γ is 16 nM. | ||
| S7683 | PIK-III | PIK-III (VPS34-IN2), which is a selective inhibitor of VPS34 enzymatic activity, inhibits autophagy and de novo lipidation of LC3 and leads to the stabilization of autophagy substrates. |
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| S7016 | VS-5584 (SB2343) | VS-5584 (SB2343) is a potent and selective dual PI3K/mTOR inhibitor for mTOR, PI3Kα/β/δ/γ with IC50 of 3.4 nM and 2.6-21 nM, respectively. Phase 1. |
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| S8002 | GSK2636771 | GSK2636771 is a potent, orally bioavailable and selective inhibitor of PI3Kβ with >900-fold selectivity over PI3Kα/PI3Kγ and >10-fold over PI3Kδ. Sensitive to PTEN null cell lines. |
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| S1219 | YM201636 | YM201636 is a selective PIKfyve inhibitor with IC50 of 33 nM, less potent to p110α and insensitive to Fabl (yeast orthologue). YM-201636 suppresses the growth of liver cancer via the induction of autophagy. |
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| S7694 | AZD8186 | AZD8186 is a potent and selective inhibitor of PI3Kβ and PI3Kδ with IC50 of 4 nM and 12 nM, respectively. Phase 1. | ||
| S1360 | GSK1059615 | GSK1059615 is a dual inhibitor of PI3Kα/β/δ/γ (reversible) and mTOR with IC50 of 0.4 nM/0.6 nM/2 nM/5 nM and 12 nM, respectively. Phase 1. |
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| S7645 | Pilaralisib (XL147) | Pilaralisib (XL147) is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ with IC50 of 39 nM/36 nM/23 nM in cell-free assays, less potent to PI3Kβ. Phase 1/2. |
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| S1352 | TG100-115 | TG100-115 is a PI3Kγ/δ inhibitor with IC50 of 83 nM/235 nM, with little effect on PI3Kα/β. Phase 1/2. |
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| S7018 | CZC24832 | CZC24832 is the first selective PI3Kγ inhibitor with IC50 of 27 nM, with 10-fold selectivity over PI3Kβ and >100-fold selectivity over PI3Kα and PI3Kδ. |
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| S7646 | Voxtalisib (XL765) | Voxtalisib (SAR245409, XL765) is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR. Phase 1/2. |
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| S1118 | XL147 analogue | XL147 analogue (SAR245408) is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ with IC50 of 39 nM/36 nM/23 nM in cell-free assays, less potent to PI3Kβ. XL147 analogue induces apoptosis. Phase 1/2. |
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| S2681 | AS-604850 | AS-604850 is a selective, ATP-competitive PI3Kγ inhibitor with IC50 of 250 nM, over 80-fold selectivity for PI3Kγ than PI3Kδ/β, and 18-fold more selective for PI3Kγ than PI3Kα. |
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| S8045 | KU-0060648 | KU-0060648 is a dual inhibitor of DNA-PK and PI3Kα, PI3Kβ, PI3Kδ with IC50 of 8.6 nM and 4 nM, 0.5 nM, 0.1 nM respectively, less inhibition of PI3Kγ with IC50 of 0.59 μM. |
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| S2749 | BGT226 (NVP-BGT226) maleate | BGT226 (NVP-BGT226) is a novel class I PI3K/mTOR inhibitor for PI3Kα/β/γ with IC50 of 4 nM/63 nM/38 nM. Phase 1/2. |
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| S2347 | Quercetin Dihydrate | Quercetin (Sophoretin), a polyphenolic flavonoid found in a wide variety of plant-based foods, such as apples, onions, berries, and red wine, is utilized in many different cultures for their nervous system and anticancer effects. Quercetin (dihydrate), a natural flavonoid, is a stimulator of recombinant SIRT1 and a PI3K inhibitor with IC50s of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively. |
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| S8456 | VPS34 inhibitor 1 (Compound 19) | VPS34 inhibitor 1 (Compound 19, PIK-III analogue) is a potent and selective inhibitor of VPS34 with an IC50 of 15 nM. |
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| S8322 | Samotolisib (LY3023414) | LY3023414 (Samotolisib, GTPL8918) is an oral ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK. |
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| S1523 | Voxtalisib (XL765) Analogue | Voxtalisib (SAR245409, XL765) Analogue is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR. Phase 1/2. |
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| S8596 | Autophinib | Autophinib is a potent autophagy inhibitor with a novel chemotype with IC50 values of 90 and 40 nM for autophagy in starvation induced autophagy assay and rapamycin induced autophagy assay. The IC50 value for Vps34 is 19 nM in vitro. | ||
| S7813 | AMG319 | AMG319 is a potent and selective PI3Kδ inhibitor with IC50 of 18 nM, >47-fold selectivity over other PI3Ks. Phase 2. | ||
| S8194 | umbralisib (TGR-1202) | Umbralisib (TGR-1202, Rp-5264), a novel, next generation PI3Kδ inhibitor, inhibits PI3Kδ activity in enzyme and cell based assays with IC50 and EC50 values of 22.2 & 24.3 nM, respectively. | ||
| S7937 | Nemiralisib | Nemiralisib, also known as GSK-2269557, is a potent and selective PI3Kδ inhibitor(pKi = 9.9). | ||
| S2699 | CH5132799 | CH5132799 (MEN1611, PA799) inhibits class I PI3Ks, particularly PI3Kα with IC50 of 14 nM; less potent to PI3Kβδγ, while sensitive in PIK3CA mutations cell lines. Phase 1. |
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| S2739 | PKI-402 | PKI-402 is a potent dual pan-PI3K/mTOR inhibitor targeting PI3Kα/β/γ/δ and mTOR with IC50 of 2 nM/7 nM/16 nM/14 nM and 3 nM, respectively; also potent to PI3Kα mutants E545K and H1047R. | ||
| S8738 | Bimiralisib (PQR309) | Bimiralisib (PQR309) is a novel brain-penetrant dual PI3K/mTOR inhibitor with in vitro and in vivo antilymphoma activity. It displays excellent selectivity versus PI3K-related lipid kinases, protein kinases and unrelated targets. | ||
| S2870 | TG100713 | TG100713 is a pan-PI3K inhibitor against PI3Kγ, PI3Kδ, PI3Kα and PI3Kβ with IC50 of 50 nM, 24 nM, 165 nM and 215 nM, respectively. |
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| S9190 | Oroxin B | Oroxin B (Hypocretin-2), one of flavonoids isolated from traditional Chinese herbal medicine Oroxylum indicum (L.) Vent, selectively induces tumor-suppressive ER stress in malignant lymphoma cells and has antioxidant activity. Oroxin B significantly inhibits proliferation and induce apoptosis, which may be strongly associated with the inhibiting COX-2/VEGF and PTEN/PI3K/AKT signaling pathway in SMMC-7721 cells, Oroxin B potentially be used as a novel therapeutic agent for liver cancer.COX-2, VEGF, PI3K, and p-AKT expression levels is found to be downregulated, while PTEN was upregulated after Oroxin B treatment. | ||
| S8163 | Paxalisib (GDC-0084) | Paxalisib (GDC-0084, RG7666) is a brain penetrant inhibitor of PI3K and mTOR. | ||
| S8589 | SF2523 | SF2523 is a highly selective and potent inhibitor of PI3K with IC50 values of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively. | ||
| S8581 | Serabelisib (TAK-117) | Serabelisib (TAK-117, INK-1117, MLN-1117) is a potent and selective oral PI3Kα isoform inhibitor (IC50 of 21 nmol/L against PI3Kα) that has demonstrated > 100-fold selectivity relative to other class I PI3K family members (PI3Kβ/γ/δ) and mTOR, and a high degree of selectivity against many other kinase. | ||
| S8132 | Deguelin | Deguelin, a natural product isolated from plants in the Mundulea sericea family, is an PI3K/AKT Inhibitor. | ||
| S2227 | PIK-294 | PIK-294 is a highly selective p110δ inhibitor with IC50 of 10 nM, 1000-, 49- and 16-fold less potent to PI3Kα/β/γ, respectively. |
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| S8157 | GDC-0326 | GDC-0326 is a potent and selective inhibitor of PI3Kα with Ki value of 0.2 nM; remarkably selective over the other class I isoforms in enzymatic assays. | ||
| S7798 | GNE-317 | GNE-317 is a potent, brain-penetrant PI3K inhibitor. | ||
| S8668 | Inavolisib (GDC-0077) | Inavolisib (GDC-0077, RG6114, RO-7113755) is a potent selective inhibitor of PI3K alpha (PI3Kα) with an IC50 of 0.038 nM. GDC-0077 is >300-fold more selective for PI3K alpha over the other class I PI3K isoforms (beta, delta, and gamma) and >2000-fold more selective over PIK family members. GDC-0077 binds to the ATP binding site of PI3K and inhibits the phosphorylation of PIP2 to PIP3. | ||
| S7623 | PI-3065 | PI-3065 is a selective p110δ inhibitor with IC50 of 15 nM, >70-fold selectivity over other PI3K family members. | ||
| S7966 | AZD8835 | AZD8835 ia a novel mixed inhibitor of PI3Kα and PI3Kδ with IC50 of 6.2 nM and 5.7 nM, respectively, also with selectivity against PI3Kβ (IC50=431 nM) and PI3Kγ (IC50=90 nM). | ||
| S2682 | CAY10505 | CAY10505 is dehydroxyl of AS-252424, which is a PI3Kγ inhibitor with IC50 of 33 nM. |
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| S3238 | Resibufogenin | Resibufogenin (Bufogenin, Recibufogenin), a component of huachansu with anticancer effect, triggers necroptosis through upregulating receptor-interacting protein kinase 3 (RIP3) and phosphorylating mixed lineage kinase domain-like protein at Ser358. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression. | ||
| S3296 | Hispidulin | Hispidulin (Dinatin), an active natrual ingredient in a number of traditional Chinese medicinal herbs, exhibits inhibitory activity against the oncogenic protein kinase Pim-1 with IC50 of 2.71 μM. Hispidulin induces apoptosis through mitochondrial dysfunction and inhibition of P13k/Akt signalling pathway in HepG2 cancer cells. Hispidulin exerts anti-osteoporotic and bone resorption attenuating effects via activating the AMPK signaling pathway. | ||
| S0817 | SKI-V | SKI V is a noncompetitive and potent inhibitor of non-lipid sphingosine kinase with IC50 of 2 μM for GST-hSK. SKI-V also inhibits PI3K with IC50 of 6 μM for hPI3k. SKI-V decreases formation of the mitogenic second messenger sphingosine-1-phosphate (S1P) and induces apoptosis with antitumor activity. | ||
| S6541 | MTX-211 | MTX-211 is a first-in-class dual inhibitor of PI3K and EGFR kinase. | ||
| S8560 | Seletalisib (UCB-5857) | Seletalisib (UCB-5857) is a novel small-molecule inhibitor of PI3Kδ with an IC50 value of 12 nM and shows significant selectivity to PI3Kδ with respect to the other class I PI3K isoforms (between 24- and 303-fold). | ||
| S8752 | leniolisib (CDZ 173) | Leniolisib (CDZ 173) is a potent PI3Kδ selective inhibitor with biochemical IC50 values of 0.244, 0.424, 2.23 and 0.011 μM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively. | ||
| E2384 | (E)-Akt inhibitor-IV | (E)-Akt inhibitor-IV is a PI3K-Akt inhibitor, with potent cytotoxic. | ||
| S3785 | Notoginsenoside R1 | Notoginsenoside R1 (Sanchinoside R1) is the main ingredient with cardiovascular activity in Panax notoginseng. It inhibits TNF-α-induced PAI-1 overexpression via extracellular signal-related kinases (ERK1/2) and phosphatidylinositol 3-kinase (PI3K)/protein kinase B (PKB) signaling pathways. | ||
| S5978 | Gallein | Gallein (Pyrogallol phthalein) is an inhibitor of G protein βγ (G beta-gamma complex, Gβγ) subunit interaction with PI3 kinase. Gallein inhibits β-ionone effects and exhibits anti-tumor activity. Gallein can be used as a biological stain. | ||
| S3220 | Trigonelline | Trigonelline (Trigenolline) is a plant alkaloid and a major component of coffee and fenugreek with anti-degranulation, anti-diabetic, antioxidant, anti-inflammatory, and neuroprotective effects. Trigonelline inhibits FcεRI-mediated intracellular signaling pathways, such as phosphorylation of PLCγ1, PI3K, and Akt. Trigonelline (Trigenolline) also inhibits the microtubule formation in RBL-2H3 cells. | ||
| S8693 | Selective PI3Kδ Inhibitor 1 (compound 7n) | Selective PI3Kδ Inhibitor 1 (compound 7n) is an inhibitor of PI3Kδ with an IC50 of 0.9 nM and >1000-fold selectivity against other class I PI3K isoforms [PI3K α/γ/β=3670/1460/21300 nM]. | ||
| S7675 | PF-4989216 | PF-4989216 is a potent and selective PI3K inhibitor with IC50 of 2 nM, 142 nM, 65 nM, 1 nM, and 110 nM for p110α, p110β, p110γ, p110δ, and VPS34, respectively. | ||
| S6516 | GNE-477 | GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor with an IC50 of 4 nM for PI3Kα and Kiapp of 21 nM for mTOR. | ||
| S6517 | GNE-493 | GNE-493 (compound 5) is a potent, selective and orally available dual inhibitor of pan-PI3-kinase and mTOR with IC50 of 3.4 nM, 12 nM, 16 nM, 16 nM and 32 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR, respectively. | ||
| S2207 | PIK-293 | PIK-293 is a PI3K inhibitor, mostly for PI3Kδ with IC50 of 0.24 μM, 500-, 100- and 50-fold less potent to PI3Kα/β/γ, respectively. |
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| S3224 | Cinobufagin | Cinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. Cinobufagin increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. Cinobufagin inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, Cinobufagin induces cell cycle arrest at the G2/M phase and apoptosis. | ||
| S7938 | GSK2292767 | GSK2292767 is a potent and selective PI3Kδ inhibitor. | ||
| S5554 | Lanatoside C | Lanatoside C is a cardiac glycoside with antiviral and anti-tumor activity. Lanatoside C induces G2/M cell cycle arrest and induces autophagy and apoptosis via attenuating MAPK, Wnt, JAK-STAT, and PI3K/AKT/mTOR signaling pathways. | ||
| E2375 | PI3K/mTOR Inhibitor-2 | PI3K/mTOR Inhibitor-2 is a potent dual pan-PI3K/mTOR inhibitor with antitumor activity. | ||
| S3243 | Zeaxanthin | Zeaxanthin, the carotenoid alcohol participates in the xanthophyll cycle, activates the extrinsic apoptosis pathway which induces apoptosis on uveal melanoma cells with IC50 value 40.8 µM. | ||
| S0947 | Cafestol | Cafestol is a natural diterpenes extracted from coffee beans. Cafestol induces apoptosis and regulates a variety of inflammatory mediators to reduce inflammation. Cafestol inhibits PI3K/Akt pathway. Cafestol also can reduce the production of ROS in the leukemia cell line HL60. | ||
| E2823 | PIK-108 | PIK-108 is a non-ATP competitive, allosteric p110β/p110δ selective inhibitor. | ||
| E0020 | Lupenone | Lupenone (Lup-20(29)-en-3-one, lupeone) is an isolated compound exhibiting anti-oxidative, anti-inflammation, and anti-diabetic activities. Lupenone can protect SH-SY5y cells against METH-induced neuronal apoptosis through the PI3K/Akt pathway. | ||
| E2366 | IHMT-PI3Kδ-372 | IHMT-PI3Kδ-372 is a potent and selective phosphatidylinositol 3-kinase δ (PI3Kδ) inhibitor with an IC50 of 14 nM in the biochemical assay | ||
| S8672 | Tenalisib | Tenalisib is a potent and selective dual PI3Kδ/γ inhibitor with IC50 values of 24.5 nM and 33.2 nM for PI3Kδ and PI3Kγ, respectively. Its selectivity over α and β isoforms are more than 300-fold and 100-fold, respectively. | ||
| S3309 | Solasodine | Solasodine (Purapuridine, Solancarpidine, Solasodin, Salasodine, Salasdine) is a poisonous alkaloid chemical compound that occurs in plants of the Solanaceae family. Solasodine reduces the mRNA level of matrix metalloproteinase-2 (MMP-2), MMP-9 and extracellular inducer of matrix metalloproteinase (EMMPRIN), but increases the expression of reversion-inducing cysteine-rich protein with kazal motifs (RECK). Solasodine downregulates oncogenic microRNA-21 (miR-21), which has been known to target RECK. Solasodine also reduces PI3K/Akt signaling pathways and downregulates expression of miR-21. | ||
| S9054 | Pectolinarin | Pectolinarin is a major compound in Cirsium setidens with anti-inflammatory activity. Pectolinarin inhibits secretion of IL-6 and IL-8, as well as the production of PGE2 and NO. Pectolinarin induces apoptosis via inactivation of the PI3K/Akt pathway. | ||
| S8948 | SRX3207 | SRX3207 is an orally active dual inhibitor of Syk-PI3K with IC50 of 39.9 nM, 31200 nM, 3070 nM, 3070 nM, 244 nM, 388 nM, 9790 nM for Syk, Zap70, BRD41, BRD42, PI3K alpha, PI3K delta, PI3K gamma, respectively. SRX3207 blocks tumor immunosuppression and increases anti-tumor immunity. | ||
| S5818 | acalisib (GS-9820) | Acalisib (GS-9820, CAL-120) is a highly selective and potent p110δ inhibitor (IC50 = 14 nM) with 114- to 400-fold selectivity over the other class I PI3K enzymes and no activity against Class II and III PI3K family members or other PI3K-related proteins including mTOR and DNA-PK. | ||
| S8917 | P110δ-IN-1 | P110δ-IN-1 is an oral, potent and selective inhibitor of Phosphatidylinositol 3-Kinase (PI3K) P110δ with IC50 of 0.6 nM in cellular assay. | ||
| S3575 | Zandelisib | Zandelisib(ME-401; PWT-143) is an orally bioavailable inhibitor of the phosphatidylinositide 3-kinase (PI3K). It selectively inhibits the delta isoform of PI3K (p110δ) and prevents the activation of the PI3K/AKT signaling pathway with an IC50 of 3.5 nM. It functions as an antineoplastic agent. | ||
| S7335 | IPI-3063 | IPI-3063 is a potent and selective p110δ inhibitor with biochemical IC50 of 2.5 ± 1.2 nM and IC50 values for the other class I PI3K isoforms (p110α, p110β, p110γ) are at least 400-fold higher. | ||
| E0121 | Parsaclisib (INCB050465) | Parsaclisib (INCB050465, INCB-50465, IBI376) is a potent and highly selective PI3Kδ(PI3K delta) inhibitor with an IC50 of 1 nM at 1 mM ATP in biochemical assay and approximately 20,000-fold selectivity for PI3Kα, PI3Kβ, PI3Kγ and 57 other kinases. | ||
| E1834New | iMDK | iMDK is a potent inhibitor of PI3K. It also inhibits the growth factor MDK (also known as midkine or MK). iMDK use along with a MEK inhibitor suppresses tumor growth of non-small cell lung cancer (NSCLC), including KRAS-mutant NSCLC and squamous NSCLC. | ||
| E2401 | SPP-86 | SPP-86, a potent and selective cell permeable inhibitor of rearranged during transfection (RET) tyrosine kinase with an IC50 of 8 nM, inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling, also inhibits RET-induced estrogen receptorα (ERα) phosphorylation in MCF7 cells. | ||
| E4680New | MTX-531 | MTX-531(NSC827271) is a first-in-class, potent and selective inhibitor of EGFR and PI3Kα with an IC50 of 14.7 nM and 6.4 nM, respectively. It may play a role in treating Head and Neck Squamous Cell Carcinoma (HSNCC), squamous lung cancers, and certain EGFR/PI3K-driven triple-negative breast cancers. | ||
| S1273 | Amarogentin | Amarogentin (AG), a secoiridoid glycoside mainly extracted from Swertia and Gentiana roots, exhibits anti-oxidative, anti-tumour, and anti-diabetic activities. Amarogentin is an agonist for the bitter taste receptor TAS2R1 and inhibits in LAD-2 cells substance P-induced production of newly synthesized TNF-α. Amarogentin induces apoptosis in human gastric cancer cells (SNU-16) through G2/M cell cycle arrest and PI3K/Akt signalling pathway. Amarogentin (AG) interacts with the α2 subunit of AMP-activated protein kinase (AMPK) and activates the trimeric kinase with EC50 of 277 pM. |
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| S3241 | Loureirin A | Loureirin A is a flavonoid extracted from the red resin of the herbs of Dracaena cochinchinensis, which is known as Dragon's Blood. Loureirin A inhibits platelet activation by an impairment of PI3K/Akt signaling. Loureirin A inhibits Akt phosphorylation. | ||
| S7865 | 740 Y-P (PDGFR 740Y-P) | 740 Y-P (PDGFR 740Y-P, 740YPDGFR) is a cell-permeable phosphopeptide activator of PI3K. | ||
| S3294 | Demethyl-Coclaurine | Demethyl-Coclaurine (Higenamine, Norcoclaurine), the key component of the Chinese herb aconite root, is a beta-2 adrenergic receptor (β2-AR) agonist. Demethyl-Coclaurine stimulates AKT phosphorylation and requires PI3K activation for the anti-apoptotic effect in cardiomyocytes. | ||
| E2947 | Recilisib | Recilisib (ON01210, EX-RAD) is a radioprotectant that activates the activity of AKT and PI3K in cells. It has been studied as prophylactic (use prior to radiation exposure) and therapeutic (after exposure to radiation) drug. | ||
| E1579New | UCL-TRO-1938 | UCL-TRO-1938 is a potent allosteric activator of PI3Kα. UCL-TRO-1938 can induce cell proliferation and has cardioprotective and neural regeneration effects. | ||
| S5383 | Erucic acid | Erucic acid (cis-13-docosenoic acid) is a monounsaturated omega-9 fatty acid used as mineral oil and a precursor to biodiesel fuel. | ||
| E0785 | YS-49 | YS-49 is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells, inhibits angiotensin II (Ang II)-stimulated proliferation of VSMCs via induction of heme oxygenase (HO)-1, also is an isoquinoline compound alkaloid, has a strong positive inotropic action through activation of cardiac β-adrenoceptors. | ||
| S4572 | Homosalate | Homosalate (HMS, Homomenthyl salicylate) is an organic ultraviolet filter used in most sunscreens but has been reported to be toxic to marine organisms. Homosalate aggravates the invasion of human trophoblast cells as well as regulates intracellular signaling pathways including PI3K/AKT and MAPK pathways. | ||
| E2391 | α-Linolenic acid | α-Linolenic acid, an essential fatty acid isolated from seed oils, affects the process of thrombotic through the modulation of PI3K/Akt signaling, and possesses the anti-arrhythmic properties. | ||
| S6885 | Ailanthone | Ailanthone (AIL, Δ13-Dehydrochaparrinone), a natural anti-hepatocellular carcinoma (HCC) component in Ailanthus altissima, induces G0/G1-phase cell cycle arrest by decreasing expression of cyclins and CDKs and increases expression of p21 and p27. Ailanthone triggers DNA damage characterized by activation of the ATM/ATR pathway. Ailanthone induces apoptosis which is mitochondrion-mediated and involves the PI3K/AKT signaling pathway in Huh7 cells. Ailanthone is also a potent inhibitor of both full-length Androgen Receptor (AR-FL) and constitutively active truncated AR splice variants (AR-Vs, AR1-651) with IC50 of 69 nM and 309 nM, respectively. | ||
| E1579New | UCL-TRO-1938 | UCL-TRO-1938 is a potent allosteric activator of PI3Kα. UCL-TRO-1938 can induce cell proliferation and has cardioprotective and neural regeneration effects. | ||
| E1834New | iMDK | iMDK is a potent inhibitor of PI3K. It also inhibits the growth factor MDK (also known as midkine or MK). iMDK use along with a MEK inhibitor suppresses tumor growth of non-small cell lung cancer (NSCLC), including KRAS-mutant NSCLC and squamous NSCLC. | ||
| E4680New | MTX-531 | MTX-531(NSC827271) is a first-in-class, potent and selective inhibitor of EGFR and PI3Kα with an IC50 of 14.7 nM and 6.4 nM, respectively. It may play a role in treating Head and Neck Squamous Cell Carcinoma (HSNCC), squamous lung cancers, and certain EGFR/PI3K-driven triple-negative breast cancers. |
PI3K阻害剤の選択性比較
Tags: PI3K inhibition | PI3K cancer | PI3K activation | PI3K signaling pathway | PI3 kinase pathway | PI3K activity | PI3K phosphorylation | PI3K assay | PI3K inhibitor cancer | PI3K inhibitor drugs | PI3K targets | PI3K inhibitors ic50 | PI3K inhibitors in clinical trials | PI3K inhibitor review
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