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PLK
PLK製品
- All (17)
- PLK阻害剤 (17)
- 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 |
|---|---|---|---|---|
| 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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| S1109 | BI 2536 | BI-2536 is a potent Plk1 inhibitor with IC50 of 0.83 nM in a cell-free assay. BI-2536 inhibits Bromodomain 4 (BRD4) with Kd of 37 nM and potently suppresses c-Myc expression. BI-2536 induces apoptosis and attenuates autophagy. Phase 2. |
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| S2235 | Volasertib | Volasertib is a highly potent Plk1 inhibitor with IC50 of 0.87 nM in a cell-free assay. It shows 6- and 65-fold greater selectivity against Plk2 and Plk3. Volasertib induces cell cycle arrest and apoptosis in various cancer cells. Phase 3. |
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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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| S2193 | GSK461364 | GSK461364 (GSK461364A) inhibits purified Plk1 with Ki of 2.2 nM in a cell-free assay. It is more than 1000-fold selective against Plk2/3. |
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| S7255 | Onvansertib (NMS-P937) | Onvansertib (NMS-P937, PCM-075, NMS1286937) is an orally available, selective Polo-like Kinase 1 (PLK1) inhibitor with IC50 of 2 nM, 5000-fold selectivity over PLK2/PLK3. Onvansertib (NMS-P937) potently causes a mitotic cell-cycle arrest followed by apoptosis in cancer cell lines and inhibits tumor growth. Phase 1. | ||
| S7720 | SBE 13 HCl | SBE 13 HCl is a potent and selective PLK1 inhibitor with IC50 of 200 pM, >4000-fold selectivity over Aurora A kinase, Plk2 and Plk3. | ||
| S1485 | HMN-214 | HMN-214 is a prodrug of HMN-176, which alters the cellular spatial orientation of Plk1. |
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| S7248 | Ro3280 | RO3280 (Ro5203280) is a potent, highly selective inhibitor of Polo-like kinase 1 (PLK1) with IC50 of 3 nM. |
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| S7552 | CFI-400945 | CFI-400945 is an orally active, potent and selective polo-like kinase 4(PLK4) inhibitor with Ki value of 0.26 nM. | ||
| S2898 | MLN0905 | MLN0905 is a potent inhibitor of PLK1 with IC50 of 2 nM. | ||
| S5893 | Poloxin | Poloxin is a non-ATP competitive Polo-like Kinase 1 polo-box domain (Plk1 PBD) inhibitor with an apparent IC50 of 4.8 μM. Poloxin's IC50 values against the PBDs of Plk2 and Plk3 as Plk1 are approximately 4-fold and 11-fold higher, respectively in fluorescence polarization assays. | ||
| S1239 | TAK-960 | TAK-960 is a novel, investigational, orally bioavailable, potent, and selective PLK1 inhibitor that has shown activity in several tumor cell lines, including those that express multidrug-resistant protein 1 (MDR1). | ||
| S2880 | GW843682X | GW843682X is a selective, ATP-competitive inhibitor of PLK1 and PLK3, with IC50s of 2.2 nM and 9.1 nM, respectively, and is also >100-fold selective against ~30 other kinases. | ||
| S5807 | HMN-176 | HMN-176 is an active metabolite of HMN-214, which has a potent antitumor activity in mouse xenograft models. HMN-176 effectively inhibits PLK-1 by interference with its normal subcellular spatial distribution at centrosomes and along the cytoskeletal structure. | ||
| S7837 | Centrinone (LCR-263) | Centrinone (LCR-263) is a selective and reversible polo-like kinase 4 (PLK4) inhibitor with Ki of 0.16 nM. | ||
| S8342 | ON1231320 | ON1231320 (7ao), an arylsulfonyl pyrido-pyrimidinone, is a highly specific inhibitor of polo like kinase 2 (PLK2). It also blocks tumor cell cycle progression in the G2/M phase in mitosis and causes apoptosis. | ||
| 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. |
|
|
| S1109 | BI 2536 | BI-2536 is a potent Plk1 inhibitor with IC50 of 0.83 nM in a cell-free assay. BI-2536 inhibits Bromodomain 4 (BRD4) with Kd of 37 nM and potently suppresses c-Myc expression. BI-2536 induces apoptosis and attenuates autophagy. Phase 2. |
|
|
| S2235 | Volasertib | Volasertib is a highly potent Plk1 inhibitor with IC50 of 0.87 nM in a cell-free assay. It shows 6- and 65-fold greater selectivity against Plk2 and Plk3. Volasertib induces cell cycle arrest and apoptosis in various cancer cells. Phase 3. |
|
|
| 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. |
|
|
| S2193 | GSK461364 | GSK461364 (GSK461364A) inhibits purified Plk1 with Ki of 2.2 nM in a cell-free assay. It is more than 1000-fold selective against Plk2/3. |
|
|
| S7255 | Onvansertib (NMS-P937) | Onvansertib (NMS-P937, PCM-075, NMS1286937) is an orally available, selective Polo-like Kinase 1 (PLK1) inhibitor with IC50 of 2 nM, 5000-fold selectivity over PLK2/PLK3. Onvansertib (NMS-P937) potently causes a mitotic cell-cycle arrest followed by apoptosis in cancer cell lines and inhibits tumor growth. Phase 1. | ||
| S7720 | SBE 13 HCl | SBE 13 HCl is a potent and selective PLK1 inhibitor with IC50 of 200 pM, >4000-fold selectivity over Aurora A kinase, Plk2 and Plk3. | ||
| S1485 | HMN-214 | HMN-214 is a prodrug of HMN-176, which alters the cellular spatial orientation of Plk1. |
|
|
| S7248 | Ro3280 | RO3280 (Ro5203280) is a potent, highly selective inhibitor of Polo-like kinase 1 (PLK1) with IC50 of 3 nM. |
|
|
| S7552 | CFI-400945 | CFI-400945 is an orally active, potent and selective polo-like kinase 4(PLK4) inhibitor with Ki value of 0.26 nM. | ||
| S2898 | MLN0905 | MLN0905 is a potent inhibitor of PLK1 with IC50 of 2 nM. | ||
| S5893 | Poloxin | Poloxin is a non-ATP competitive Polo-like Kinase 1 polo-box domain (Plk1 PBD) inhibitor with an apparent IC50 of 4.8 μM. Poloxin's IC50 values against the PBDs of Plk2 and Plk3 as Plk1 are approximately 4-fold and 11-fold higher, respectively in fluorescence polarization assays. | ||
| S1239 | TAK-960 | TAK-960 is a novel, investigational, orally bioavailable, potent, and selective PLK1 inhibitor that has shown activity in several tumor cell lines, including those that express multidrug-resistant protein 1 (MDR1). | ||
| S2880 | GW843682X | GW843682X is a selective, ATP-competitive inhibitor of PLK1 and PLK3, with IC50s of 2.2 nM and 9.1 nM, respectively, and is also >100-fold selective against ~30 other kinases. | ||
| S5807 | HMN-176 | HMN-176 is an active metabolite of HMN-214, which has a potent antitumor activity in mouse xenograft models. HMN-176 effectively inhibits PLK-1 by interference with its normal subcellular spatial distribution at centrosomes and along the cytoskeletal structure. | ||
| S7837 | Centrinone (LCR-263) | Centrinone (LCR-263) is a selective and reversible polo-like kinase 4 (PLK4) inhibitor with Ki of 0.16 nM. | ||
| S8342 | ON1231320 | ON1231320 (7ao), an arylsulfonyl pyrido-pyrimidinone, is a highly specific inhibitor of polo like kinase 2 (PLK2). It also blocks tumor cell cycle progression in the G2/M phase in mitosis and causes apoptosis. |
PLK阻害剤の選択性比較
Tags: PLK inhibition | PLK activation | PLK1 cancer | PLK1 phosphorylation | PLK1 pathway | PLK1 activation | PLK1 signaling | PLK1 kinase assay | PLK pathway | PLK inhibitors cancer | PLK1 inhibitor development | PLK inhibitor review
納期 国内在庫品：受注日の翌日（15時までの受注分） ＊北海道、九州、沖縄への配送は受注日より２日以上 を要する場合あり 海外在庫品：受注後１〜２週間