PARP

PARP製品

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S1060 Olaparib (AZD2281) オラパリブ (Olaparib (AZD2281, KU0059436)) は選択的 PARP1/2 阻害剤であり、cell-free assay における IC50 はそれぞれ 5 nM および 1 nM です。タンキラーゼ-1 (Tankyrase-1) に対しては 1/300 の効果を示します。オラパリブは BRCA に変異をきたした細胞において、マイトファジー (mitophagy) に関連した顕著なオートファジー (mitophagy) を誘発します。
Nature, 2024, 10.1038/s41586-024-07217-2
Nature, 2024, 628(8007):433-441
Cell, 2024, 187(4):945-961.e18
S1180 XAV-939 XAV-939 (NVP-XAV939) selectively inhibits Wnt/β-catenin-mediated transcription through tankyrase1/2 inhibition with IC50 of 11 nM/4 nM in cell-free assays, regulates axin levels and does not affect CRE, NF-κB or TGF-β.
Adv Sci (Weinh), 2024, 11(1):e2303637
J Nanobiotechnology, 2024, 22(1):373
Cell Death Dis, 2024, 15(3):211
S1004 Veliparib (ABT-888) Veliparib (ABT-888, NSC 737664) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM in cell-free assays, respectively. It is inactive to SIRT2. Veliparib increases autophagy and apoptosis. Phase 3.
Nature, 2024, 10.1038/s41586-024-07217-2
Nature, 2024, 628(8007):433-441
Cell Rep, 2024, 43(5):114205
S7048 Talazoparib (BMN 673) タラゾパリブ (Talazoparib (BMN 673、LT-673)) は、新規 PARP 阻害剤 (無細胞アッセイで IC50 = 0.57 nM) です。 また PARP-2 の強力な阻害剤でもありますが、PARG を阻害せず PTEN 変異に非常に敏感です。 臨床フェーズ 3。
Nature, 2024, 10.1038/s41586-024-07217-2
Nature, 2024, 628(8007):433-441
Gastroenterology, 2024, S0016-5085(24)00062-3
S1098 Rucaparib phosphate Rucaparib phosphate is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. Phase 3.
Int J Mol Sci, 2024, 25(2)886
J Biol Chem, 2024, 300(6):107377
Cancer Res, 2023, 83(10):1699-1710
S2741 Niraparib (MK-4827) ニラパリブ (Niraparib (MK-4827)) は PARP1/2 の選択的阻害剤 (IC50 = 3.8 nM/2.1 nM) であり、変異型 BRCA-1 および BRCA-2 を持つ癌細胞で高い活性を示します。PARP3, V-PARP, Tank1 に比べて 330 倍以上の選択性があります。 ニラパリブは PARP-DNA 複合体を形成し、DNA損傷、アポトーシス (apoptossis)、および細胞死を引き起こします。臨床フェーズ 3。
Nat Genet, 2024, 10.1038/s41588-024-01948-8
EBioMedicine, 2024, 103:105129
Cell Death Discov, 2024, 10(1):74
S7300 PJ34 HCl PJ34 HCl is the hydrochloride salt of PJ34, which is a PARP inhibitor with EC50 of 20 nM and is equally potent to PARP1/2.
J Neuroinflammation, 2024, 21(1):235
Nat Commun, 2023, 14(1):7161
Nat Commun, 2023, 14(1):4310
S4948 Rucaparib Rucaparib is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains.
Nat Commun, 2024, 15(1):2862
Nucleic Acids Res, 2024, gkae316
EBioMedicine, 2024, 103:105129
S7625 Niraparib tosylate Niraparib tosylate is a selective inhibitor of PARP1/PARP2 with IC50 of 3.8 nM/2.1 nM. Niraparib increases formation of PARP-DNA complexes resulting in DNA damage, apoptosis, and cell death.
Nat Commun, 2024, 15(1):1041
Cancer Res, 2023, 83(10):1699-1710
Cancer Res, 2023, 83(16):2750-2762
S2178 AG-14361 AG14361 is a potent inhibitor of PARP1 with Ki of <5 nM in a cell-free assay. It is at least 1000-fold more potent than the benzamides.
Nat Commun, 2024, 15(1):1041
Cell Stem Cell, 2022, S1934-5909(22)00010-8
Cell Rep, 2022, 39(12):110994
S1087 Iniparib (BSI-201) Iniparib (BSI-201, NSC-746045, IND-71677) is a PARP1 inhibitor with demonstrated effectiveness in triple-negative breast cancer (TNBC). Phase 3.
Nat Commun, 2021, 12(1):736
Front Oncol, 2021, 11:773186
PLoS Pathog, 2020, 21;16(4):e1008474
S5195 Rucaparib Camsylate Rucaparib (Rubraca, AG014699, PF01367338) Camsylate is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains.
Adv Sci (Weinh), 2022, 9(30):e2201210
Cell Death Dis, 2022, 13(6):558
Int J Mol Sci, 2022, 23(10)5770
S2197 A-966492 A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively.
Nat Commun, 2021, 12(1):736
Front Immunol, 2021, 12:712021
Front Immunol, 2021, 12:712021
S7239 G007-LK G007-LK is a potent and selective tankyrase inhibitor with IC50 of 46 nM and 25 nM for TNKS1/2, respectively.
EBioMedicine, 2024, 103:105129
bioRxiv, 2024, 2024.02.02.578667
Nat Commun, 2023, 14(1):110
S8038 UPF 1069 UPF 1069 is a selective PARP2 inhibitor with IC50 of 0.3 μM. It is ~27-fold selective against PARP1.
Cell Rep, 2023, 42(9):113113
Res Sq, 2023, rs.3.rs-2688694
Res Sq, 2023, rs.3.rs-2688694
S7029 AZD2461 AZD2461 is a novel PARP inhibitor with low affinity for Pgp. Phase 1.
Nat Commun, 2021, 12(1):736
Cell Chem Biol, 2021, S2451-9456(21)00058-1
Dev Cell, 2020, 53(2):240-252.e7
S8592 Pamiparib Pamiparib is a potent and selective inhibitor of PARP1 and PARP2 with IC50 values of 0.83 and 0.11 nM, respectively in biochemical assays. It shows high selectivity over other PARP enzymes.
Cell Death Discov, 2024, 10(1):74
Clin Cancer Res, 2023, 29(9):1763-1782
J Neurooncol, 2023, 164(3):617-632
S1132 3-Aminobenzamide 3-Aminobenzamide (3-ABA , 3-Amino Benzamide, 3-AB) is a potent inhibitor of Poly(ADP-ribose)polymerase (PARP) and inhibits cell apoptosis after SCI (Spinal Cord Injury) in caspase-independent way.
Int J Mol Sci, 2023, 24(2)1667
Psychopharmacology (Berl), 2022, 10.1007/s00213-022-06188-4
Cell Death Discov, 2021, 7(1):181
S7438 ME0328 ME0328 is a potent and selective PARP inhibitor with IC50 of 0.89 μM for PARP3, about 7-fold selectivity over PARP1.
Biomed Pharmacother, 2018, 97:115-119
Mol Cancer Ther, 2018, 17(10):2206-2216
Breast Cancer Res Treat, 2018, 172(1):23-32
S8363 NMS-P118 NMS-P118 is a potent, orally available, and highly selective PARP-1 inhibitor endowed with excellent ADME and pharmacokinetic profiles, showing 150-fold selectivity for PARP-1 over PARP-2 (Kd 0.009 μM vs 1.39 μM, respectively).
Res Sq, 2023, rs.3.rs-2688694
Res Sq, 2023, rs.3.rs-2688694
Int J Biol Sci, 2022, 18(3):1238-1253
S8419 Stenoparib (E7449) Stenoparib (E7449, 2X-121, MGI25036) is an orally bioavailable, brain penetrable, small molecule dual inhibitor of PARP1/2 and also inhibits PARP5a/5b, otherwise known as tankyrase1 and 2 (TNKS1/2), important regulators of canonical Wnt/β-catenin signaling. It has IC50 values of 1.0 and 1.2 nM for PARP1 and 2, respectively.
Br J Pharmacol, 2024, 10.1111/bph.17305
Cell Death Discov, 2024, 10(1):74
J Cell Mol Med, 2024, 28(12):e18467
S7238 NVP-TNKS656 NVP-TNKS656 is a highly potent, selective, and orally active tankyrase inhibitor with IC50 of 6 nM for TNKS2, > 300-fold selectivity against PARP1 and PARP2.
Cell, 2024, 187(14):3671-3689.e23
bioRxiv, 2023, 2023.07.19.549714
bioRxiv, 2023, 2023.07.19.549714
S7490 WIKI4 WIKI4 is a novel Tankyrase inhibitor with IC50 of 15 nM for TNKS2, and leads to inhibition of Wnt/beta-catenin signaling.
Sci Rep, 2022, 12(1):7
Carcinogenesis, 2020, 41(7):993-1004
Nat Commun, 2019, 10(1):4363
S4715 Benzamide Benzamide, an inhibitor of poly(ADP-ribose) polymerase, is a derivative of benzoic acid.
Int J Mol Sci, 2019, 20(21)
Mol Pharmacol, 2019, 96(4):419-429
Acta Neuropathol Commun, 2014, 2:57
S8370 BGP-15 2HCl BGP-15, is a nicotinic amidoxime derivative with PARP inhibitory activity. It has been demonstrated that BGP-15 protects against ischemia-reperfusion injury.
Part Fibre Toxicol, 2023, 20(1):28
Part Fibre Toxicol, 2023, 20(1):28
Respir Res, 2023, 24(1):319
S7730 NU1025 NU1025 (NSC 696807) is a potent PARP inhibitor with IC50 of 400 nM.
J Clin Med, 2020, 30;9(4)
Med Sci Monit, 2019, 25:2886-2895
S5967 Berberine chloride hydrate Berberine (Natural Yellow 18) chloride hydrate is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.
Front Biosci (Landmark Ed), 2022, 27(8):242
Front Pharmacol, 2021, 12:632201
S6745 JW55 JW55 is a potent and selective inhibitor of the canonical Wnt pathway that functions via inhibition of the PARP domain of tankyrase 1 and tankyrase 2 (TNKS1/2).
Cell Discov, 2024, 10(1):39
Oncotarget, 2021, 12(7):674-685
Chin J Integr Med, 2021, 10.1007/s11655-021-3282-0
S0519 BYK204165 BYK204165 is a potent and selective inhibitor of the poly(ADP-ribose) polymerase (PARP). BYK204165 inhibits cell-free recombinant human PARP-1 (hPARP-1) with pIC50 of 7.35 and pKi of 7.05 and murine PARP-2 (mPARP-2) with pIC50 of 5.38, respectively.
Sci Transl Med, 2021, 13(592)eabc7211
S9712 Fluzoparib (SHR-3162)

Fluzoparib (SHR3162, HS10160) is a potent Poly (ADP-ribose) polymerase (PARP) inhibitor that shows anti-tumor activity with an IC50 of 1.46±0.72 nM for PARP1.

Biochemistry, 2023, 62(16):2382-2390
S4710 Picolinamide Picolinamide (2-Pyridinecarboxamide, Picolinoylamide, 2-Carbamoylpyridine) is found to be a strong inhibitor of poly (ADP-ribose) synthetase of nuclei from rat pancreatic islet cells.
Neural Regen Res, 2023, 18(10):2252-2259
Neural Regen Res, 2023, 18(10):2252-2259
E1425 Nesuparib Nesuparib (JPI-547, NOV140201) is a potential inhibitor of both PARP and tankyrases, with IC50 of 0.005 μM, 0.001 μM, 0.002 μM, and ND for TNKS1, TNKS2, PARP1, and PARP2, respectively. Nesuparib exhibits anti-tumor activity in BRCA-deficient xenograft models.
S6899 Licochalcone D Licochalcone D (Lico D, LCD, LD), a flavonoid isolated from a Chinese medicinal plant Glycyrrhiza inflata, has antioxidant, anti-inflammatory and anti-cancer properties. Licochalcone D inhibit phosphorylation of NF-κB p65 in LPS signaling pathway. Licochalcone D inhibits JAK2, EGFR and Met (c-Met) activities and induces ROS-dependent apoptosis. Licochalcone D also induces caspases activation and poly (ADP-ribose) polymerase (PARP) cleavage.
S6977 DR2313 DR2313 is a potent, selective, competitive and brain-penetrant inhibitor of poly(ADP-ribose) polymerase (PARP), with IC50s of 0.20 μM and 0.24 μM for PARP-1 and PARP-2, respectively. 
S6739 MN 64 MN-64 is a potent inhibitor of TNKS1 and TNKS2 with IC50 value of 6 and 72 nM, respectively.
S0913 4',5,7-Trimethoxyflavone 4',5,7-Trimethoxyflavone (5,​7,​4'-​Trimethoxyflavone, TMF) is a flavonoid isolated from Kaempferia parviflora (KP) that induces apoptosis. 4',5,7-Trimethoxyflavone increases sub-G1 phase, DNA fragmentation, annexin-V/PI staining and Bax/Bcl-xL ratio, activates caspase-3 and degrades poly (ADP-ribose) polymerase (PARP) protein.
E1069 M2912 M2912 (MSC2504877) is a very potent TNKS1/TNKS2 inhibitor (IC50=0.6 nM for TNKS1) with exquisite selectivity over other PARP family enzymes and favorable compound properties. This inhibitor potently modulates the Wnt/β-catenin pathway by elevating the levels of axin2 (EC50=17 nM) and tankyrase in DLD1 cells in a dose-dependent manner resulting in reduced cellular Wnt reporter activity.
S0732 GeA-69 GeA-69 is a cell-permeable, selective allosteric inhibitor targeting macrodomain 2 (MD2) of poly-adenosine-diphosphate-ribose polymerase 14 (PARP14) with Kd of 860 nM.
S8993 Atamparib (RBN-2397) Atamparib (RBN-2397) is a potent, selective and orally active NAD+ competitive inhibitor PARP7 with IC50 of <3 nM and Kd of <0.001 μM. RBN-2397 has the potential for the research of tumor treatment.
bioRxiv, 2024, 2024.03.15.584457
E1614New OUL232 OUL232 (Compound 27) is an potent inhibitor of mono-ADP-ribosylation (mono-ARTs) PARP10 with IC50 of 7.8 nM. It also inhibits PARP7, PARP11, PARP12, PARP14, and PARP15 at nM potencies.
S9893 Venadaparib(IDX-1197) Venadaparib (IDX-1197), a potent PARP1/2 inhibitor with IC50 values of 1.4 nM and 1.0 nM respectively, prevents the repair of DNA single-strand breaks (SSB) and promotes the conversion of SSB to double-stranded breaks (DSB), which ultimately leads to synthetic lethality in cancer cells.
S2271 Berberine chloride Berberine chloride is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.
Adv Healthc Mater, 2023, e2300591.
Transl Oncol, 2023, 35:101712
J Biomol Struct Dyn, 2022, 1-11
S6882 HI-TOPK-032 HI-TOPK-032 is a potent and specific inhibitor of TOPK. HI-TOPK-032 also reduces ERK-RSK phosphorylation, regulates of the abundance of p53, cleaved caspase-7, and cleaved PARP, and induces apoptosis in cancer cells.
E4869New Niraparib hydrochloride Niraparib hydrochloride (MK-4827 hydrochloride) is a potent poly(ADP-ribose)polymerase (PARP) inhibitor with IC50s of 3.8 and 2.1 nM against both the PARP-1 and PARP-2 enzymes, respectively.It inhibits the repair of radiation-induced DNA double-strand breaks, activates apoptosis, and exhibits anti-tumor activity.
S9360 4-Hydroxyquinazoline 4-Hydroxyquinazoline (Quinazolin-4-ol, 4-Quinazolinol) is a PARP inhibitor with a high potency for PARP-1 with IC50 of 9.5 μM.
S8992 RBN012759 RBN012759 is a potent and selective inhibitor of PARP14 with IC50 of <3 nM and 5 nM for human catalytic domain and mouse catalytic domain, respectively. RBN012759 contributes to anti-tumor immune response.
S9875 Saruparib (AZD5305)

Saruparib (AZD5305) is a highly selective and potent inhibitor of PARP1 with an IC50 of 3 nM in wild-type A549 lung cancer cells. AZD5305 shows no or minimal growth inhibitory effects in other cells (IC50s >10μM).

Nature, 2024, 10.1038/s41586-024-07217-2
Nature, 2024, 628(8007):433-441
Nat Commun, 2024, 15(1):5822
E2147 AZD9574 AZD9574 is a novel PARP inhibitor which combines PARP1 selectivity, trapping and high CNS penetration in a single molecule.
S8876 RK-287107 RK-287107 is a novel, potent and selective tankyrase inhibitor with antitumor activity. RK-287107 inhibits tankyrase-1 and tankyrase-2 in vitro with IC50 of 14.3 nM and 10.6 nM.
S1060 Olaparib (AZD2281) オラパリブ (Olaparib (AZD2281, KU0059436)) は選択的 PARP1/2 阻害剤であり、cell-free assay における IC50 はそれぞれ 5 nM および 1 nM です。タンキラーゼ-1 (Tankyrase-1) に対しては 1/300 の効果を示します。オラパリブは BRCA に変異をきたした細胞において、マイトファジー (mitophagy) に関連した顕著なオートファジー (mitophagy) を誘発します。
Nature, 2024, 10.1038/s41586-024-07217-2
Nature, 2024, 628(8007):433-441
Cell, 2024, 187(4):945-961.e18
S1180 XAV-939 XAV-939 (NVP-XAV939) selectively inhibits Wnt/β-catenin-mediated transcription through tankyrase1/2 inhibition with IC50 of 11 nM/4 nM in cell-free assays, regulates axin levels and does not affect CRE, NF-κB or TGF-β.
Adv Sci (Weinh), 2024, 11(1):e2303637
J Nanobiotechnology, 2024, 22(1):373
Cell Death Dis, 2024, 15(3):211
S1004 Veliparib (ABT-888) Veliparib (ABT-888, NSC 737664) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM in cell-free assays, respectively. It is inactive to SIRT2. Veliparib increases autophagy and apoptosis. Phase 3.
Nature, 2024, 10.1038/s41586-024-07217-2
Nature, 2024, 628(8007):433-441
Cell Rep, 2024, 43(5):114205
S7048 Talazoparib (BMN 673) タラゾパリブ (Talazoparib (BMN 673、LT-673)) は、新規 PARP 阻害剤 (無細胞アッセイで IC50 = 0.57 nM) です。 また PARP-2 の強力な阻害剤でもありますが、PARG を阻害せず PTEN 変異に非常に敏感です。 臨床フェーズ 3。
Nature, 2024, 10.1038/s41586-024-07217-2
Nature, 2024, 628(8007):433-441
Gastroenterology, 2024, S0016-5085(24)00062-3
S1098 Rucaparib phosphate Rucaparib phosphate is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. Phase 3.
Int J Mol Sci, 2024, 25(2)886
J Biol Chem, 2024, 300(6):107377
Cancer Res, 2023, 83(10):1699-1710
S2741 Niraparib (MK-4827) ニラパリブ (Niraparib (MK-4827)) は PARP1/2 の選択的阻害剤 (IC50 = 3.8 nM/2.1 nM) であり、変異型 BRCA-1 および BRCA-2 を持つ癌細胞で高い活性を示します。PARP3, V-PARP, Tank1 に比べて 330 倍以上の選択性があります。 ニラパリブは PARP-DNA 複合体を形成し、DNA損傷、アポトーシス (apoptossis)、および細胞死を引き起こします。臨床フェーズ 3。
Nat Genet, 2024, 10.1038/s41588-024-01948-8
EBioMedicine, 2024, 103:105129
Cell Death Discov, 2024, 10(1):74
S7300 PJ34 HCl PJ34 HCl is the hydrochloride salt of PJ34, which is a PARP inhibitor with EC50 of 20 nM and is equally potent to PARP1/2.
J Neuroinflammation, 2024, 21(1):235
Nat Commun, 2023, 14(1):7161
Nat Commun, 2023, 14(1):4310
S4948 Rucaparib Rucaparib is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains.
Nat Commun, 2024, 15(1):2862
Nucleic Acids Res, 2024, gkae316
EBioMedicine, 2024, 103:105129
S7625 Niraparib tosylate Niraparib tosylate is a selective inhibitor of PARP1/PARP2 with IC50 of 3.8 nM/2.1 nM. Niraparib increases formation of PARP-DNA complexes resulting in DNA damage, apoptosis, and cell death.
Nat Commun, 2024, 15(1):1041
Cancer Res, 2023, 83(10):1699-1710
Cancer Res, 2023, 83(16):2750-2762
S2178 AG-14361 AG14361 is a potent inhibitor of PARP1 with Ki of <5 nM in a cell-free assay. It is at least 1000-fold more potent than the benzamides.
Nat Commun, 2024, 15(1):1041
Cell Stem Cell, 2022, S1934-5909(22)00010-8
Cell Rep, 2022, 39(12):110994
S1087 Iniparib (BSI-201) Iniparib (BSI-201, NSC-746045, IND-71677) is a PARP1 inhibitor with demonstrated effectiveness in triple-negative breast cancer (TNBC). Phase 3.
Nat Commun, 2021, 12(1):736
Front Oncol, 2021, 11:773186
PLoS Pathog, 2020, 21;16(4):e1008474
S5195 Rucaparib Camsylate Rucaparib (Rubraca, AG014699, PF01367338) Camsylate is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains.
Adv Sci (Weinh), 2022, 9(30):e2201210
Cell Death Dis, 2022, 13(6):558
Int J Mol Sci, 2022, 23(10)5770
S2197 A-966492 A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively.
Nat Commun, 2021, 12(1):736
Front Immunol, 2021, 12:712021
Front Immunol, 2021, 12:712021
S7239 G007-LK G007-LK is a potent and selective tankyrase inhibitor with IC50 of 46 nM and 25 nM for TNKS1/2, respectively.
EBioMedicine, 2024, 103:105129
bioRxiv, 2024, 2024.02.02.578667
Nat Commun, 2023, 14(1):110
S8038 UPF 1069 UPF 1069 is a selective PARP2 inhibitor with IC50 of 0.3 μM. It is ~27-fold selective against PARP1.
Cell Rep, 2023, 42(9):113113
Res Sq, 2023, rs.3.rs-2688694
Res Sq, 2023, rs.3.rs-2688694
S7029 AZD2461 AZD2461 is a novel PARP inhibitor with low affinity for Pgp. Phase 1.
Nat Commun, 2021, 12(1):736
Cell Chem Biol, 2021, S2451-9456(21)00058-1
Dev Cell, 2020, 53(2):240-252.e7
S8592 Pamiparib Pamiparib is a potent and selective inhibitor of PARP1 and PARP2 with IC50 values of 0.83 and 0.11 nM, respectively in biochemical assays. It shows high selectivity over other PARP enzymes.
Cell Death Discov, 2024, 10(1):74
Clin Cancer Res, 2023, 29(9):1763-1782
J Neurooncol, 2023, 164(3):617-632
S1132 3-Aminobenzamide 3-Aminobenzamide (3-ABA , 3-Amino Benzamide, 3-AB) is a potent inhibitor of Poly(ADP-ribose)polymerase (PARP) and inhibits cell apoptosis after SCI (Spinal Cord Injury) in caspase-independent way.
Int J Mol Sci, 2023, 24(2)1667
Psychopharmacology (Berl), 2022, 10.1007/s00213-022-06188-4
Cell Death Discov, 2021, 7(1):181
S7438 ME0328 ME0328 is a potent and selective PARP inhibitor with IC50 of 0.89 μM for PARP3, about 7-fold selectivity over PARP1.
Biomed Pharmacother, 2018, 97:115-119
Mol Cancer Ther, 2018, 17(10):2206-2216
Breast Cancer Res Treat, 2018, 172(1):23-32
S8363 NMS-P118 NMS-P118 is a potent, orally available, and highly selective PARP-1 inhibitor endowed with excellent ADME and pharmacokinetic profiles, showing 150-fold selectivity for PARP-1 over PARP-2 (Kd 0.009 μM vs 1.39 μM, respectively).
Res Sq, 2023, rs.3.rs-2688694
Res Sq, 2023, rs.3.rs-2688694
Int J Biol Sci, 2022, 18(3):1238-1253
S8419 Stenoparib (E7449) Stenoparib (E7449, 2X-121, MGI25036) is an orally bioavailable, brain penetrable, small molecule dual inhibitor of PARP1/2 and also inhibits PARP5a/5b, otherwise known as tankyrase1 and 2 (TNKS1/2), important regulators of canonical Wnt/β-catenin signaling. It has IC50 values of 1.0 and 1.2 nM for PARP1 and 2, respectively.
Br J Pharmacol, 2024, 10.1111/bph.17305
Cell Death Discov, 2024, 10(1):74
J Cell Mol Med, 2024, 28(12):e18467
S7238 NVP-TNKS656 NVP-TNKS656 is a highly potent, selective, and orally active tankyrase inhibitor with IC50 of 6 nM for TNKS2, > 300-fold selectivity against PARP1 and PARP2.
Cell, 2024, 187(14):3671-3689.e23
bioRxiv, 2023, 2023.07.19.549714
bioRxiv, 2023, 2023.07.19.549714
S7490 WIKI4 WIKI4 is a novel Tankyrase inhibitor with IC50 of 15 nM for TNKS2, and leads to inhibition of Wnt/beta-catenin signaling.
Sci Rep, 2022, 12(1):7
Carcinogenesis, 2020, 41(7):993-1004
Nat Commun, 2019, 10(1):4363
S4715 Benzamide Benzamide, an inhibitor of poly(ADP-ribose) polymerase, is a derivative of benzoic acid.
Int J Mol Sci, 2019, 20(21)
Mol Pharmacol, 2019, 96(4):419-429
Acta Neuropathol Commun, 2014, 2:57
S8370 BGP-15 2HCl BGP-15, is a nicotinic amidoxime derivative with PARP inhibitory activity. It has been demonstrated that BGP-15 protects against ischemia-reperfusion injury.
Part Fibre Toxicol, 2023, 20(1):28
Part Fibre Toxicol, 2023, 20(1):28
Respir Res, 2023, 24(1):319
S7730 NU1025 NU1025 (NSC 696807) is a potent PARP inhibitor with IC50 of 400 nM.
J Clin Med, 2020, 30;9(4)
Med Sci Monit, 2019, 25:2886-2895
S6745 JW55 JW55 is a potent and selective inhibitor of the canonical Wnt pathway that functions via inhibition of the PARP domain of tankyrase 1 and tankyrase 2 (TNKS1/2).
Cell Discov, 2024, 10(1):39
Oncotarget, 2021, 12(7):674-685
Chin J Integr Med, 2021, 10.1007/s11655-021-3282-0
S0519 BYK204165 BYK204165 is a potent and selective inhibitor of the poly(ADP-ribose) polymerase (PARP). BYK204165 inhibits cell-free recombinant human PARP-1 (hPARP-1) with pIC50 of 7.35 and pKi of 7.05 and murine PARP-2 (mPARP-2) with pIC50 of 5.38, respectively.
Sci Transl Med, 2021, 13(592)eabc7211
S9712 Fluzoparib (SHR-3162)

Fluzoparib (SHR3162, HS10160) is a potent Poly (ADP-ribose) polymerase (PARP) inhibitor that shows anti-tumor activity with an IC50 of 1.46±0.72 nM for PARP1.

Biochemistry, 2023, 62(16):2382-2390
S4710 Picolinamide Picolinamide (2-Pyridinecarboxamide, Picolinoylamide, 2-Carbamoylpyridine) is found to be a strong inhibitor of poly (ADP-ribose) synthetase of nuclei from rat pancreatic islet cells.
Neural Regen Res, 2023, 18(10):2252-2259
Neural Regen Res, 2023, 18(10):2252-2259
E1425 Nesuparib Nesuparib (JPI-547, NOV140201) is a potential inhibitor of both PARP and tankyrases, with IC50 of 0.005 μM, 0.001 μM, 0.002 μM, and ND for TNKS1, TNKS2, PARP1, and PARP2, respectively. Nesuparib exhibits anti-tumor activity in BRCA-deficient xenograft models.
S6899 Licochalcone D Licochalcone D (Lico D, LCD, LD), a flavonoid isolated from a Chinese medicinal plant Glycyrrhiza inflata, has antioxidant, anti-inflammatory and anti-cancer properties. Licochalcone D inhibit phosphorylation of NF-κB p65 in LPS signaling pathway. Licochalcone D inhibits JAK2, EGFR and Met (c-Met) activities and induces ROS-dependent apoptosis. Licochalcone D also induces caspases activation and poly (ADP-ribose) polymerase (PARP) cleavage.
S6977 DR2313 DR2313 is a potent, selective, competitive and brain-penetrant inhibitor of poly(ADP-ribose) polymerase (PARP), with IC50s of 0.20 μM and 0.24 μM for PARP-1 and PARP-2, respectively. 
S6739 MN 64 MN-64 is a potent inhibitor of TNKS1 and TNKS2 with IC50 value of 6 and 72 nM, respectively.
S0913 4',5,7-Trimethoxyflavone 4',5,7-Trimethoxyflavone (5,​7,​4'-​Trimethoxyflavone, TMF) is a flavonoid isolated from Kaempferia parviflora (KP) that induces apoptosis. 4',5,7-Trimethoxyflavone increases sub-G1 phase, DNA fragmentation, annexin-V/PI staining and Bax/Bcl-xL ratio, activates caspase-3 and degrades poly (ADP-ribose) polymerase (PARP) protein.
E1069 M2912 M2912 (MSC2504877) is a very potent TNKS1/TNKS2 inhibitor (IC50=0.6 nM for TNKS1) with exquisite selectivity over other PARP family enzymes and favorable compound properties. This inhibitor potently modulates the Wnt/β-catenin pathway by elevating the levels of axin2 (EC50=17 nM) and tankyrase in DLD1 cells in a dose-dependent manner resulting in reduced cellular Wnt reporter activity.
S0732 GeA-69 GeA-69 is a cell-permeable, selective allosteric inhibitor targeting macrodomain 2 (MD2) of poly-adenosine-diphosphate-ribose polymerase 14 (PARP14) with Kd of 860 nM.
S8993 Atamparib (RBN-2397) Atamparib (RBN-2397) is a potent, selective and orally active NAD+ competitive inhibitor PARP7 with IC50 of <3 nM and Kd of <0.001 μM. RBN-2397 has the potential for the research of tumor treatment.
bioRxiv, 2024, 2024.03.15.584457
E1614New OUL232 OUL232 (Compound 27) is an potent inhibitor of mono-ADP-ribosylation (mono-ARTs) PARP10 with IC50 of 7.8 nM. It also inhibits PARP7, PARP11, PARP12, PARP14, and PARP15 at nM potencies.
S9893 Venadaparib(IDX-1197) Venadaparib (IDX-1197), a potent PARP1/2 inhibitor with IC50 values of 1.4 nM and 1.0 nM respectively, prevents the repair of DNA single-strand breaks (SSB) and promotes the conversion of SSB to double-stranded breaks (DSB), which ultimately leads to synthetic lethality in cancer cells.
E4869New Niraparib hydrochloride Niraparib hydrochloride (MK-4827 hydrochloride) is a potent poly(ADP-ribose)polymerase (PARP) inhibitor with IC50s of 3.8 and 2.1 nM against both the PARP-1 and PARP-2 enzymes, respectively.It inhibits the repair of radiation-induced DNA double-strand breaks, activates apoptosis, and exhibits anti-tumor activity.
S9360 4-Hydroxyquinazoline 4-Hydroxyquinazoline (Quinazolin-4-ol, 4-Quinazolinol) is a PARP inhibitor with a high potency for PARP-1 with IC50 of 9.5 μM.
S8992 RBN012759 RBN012759 is a potent and selective inhibitor of PARP14 with IC50 of <3 nM and 5 nM for human catalytic domain and mouse catalytic domain, respectively. RBN012759 contributes to anti-tumor immune response.
S9875 Saruparib (AZD5305)

Saruparib (AZD5305) is a highly selective and potent inhibitor of PARP1 with an IC50 of 3 nM in wild-type A549 lung cancer cells. AZD5305 shows no or minimal growth inhibitory effects in other cells (IC50s >10μM).

Nature, 2024, 10.1038/s41586-024-07217-2
Nature, 2024, 628(8007):433-441
Nat Commun, 2024, 15(1):5822
E2147 AZD9574 AZD9574 is a novel PARP inhibitor which combines PARP1 selectivity, trapping and high CNS penetration in a single molecule.
S8876 RK-287107 RK-287107 is a novel, potent and selective tankyrase inhibitor with antitumor activity. RK-287107 inhibits tankyrase-1 and tankyrase-2 in vitro with IC50 of 14.3 nM and 10.6 nM.
S5967 Berberine chloride hydrate Berberine (Natural Yellow 18) chloride hydrate is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.
Front Biosci (Landmark Ed), 2022, 27(8):242
Front Pharmacol, 2021, 12:632201
S2271 Berberine chloride Berberine chloride is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.
Adv Healthc Mater, 2023, e2300591.
Transl Oncol, 2023, 35:101712
J Biomol Struct Dyn, 2022, 1-11
S6882 HI-TOPK-032 HI-TOPK-032 is a potent and specific inhibitor of TOPK. HI-TOPK-032 also reduces ERK-RSK phosphorylation, regulates of the abundance of p53, cleaved caspase-7, and cleaved PARP, and induces apoptosis in cancer cells.
E1614New OUL232 OUL232 (Compound 27) is an potent inhibitor of mono-ADP-ribosylation (mono-ARTs) PARP10 with IC50 of 7.8 nM. It also inhibits PARP7, PARP11, PARP12, PARP14, and PARP15 at nM potencies.
E4869New Niraparib hydrochloride Niraparib hydrochloride (MK-4827 hydrochloride) is a potent poly(ADP-ribose)polymerase (PARP) inhibitor with IC50s of 3.8 and 2.1 nM against both the PARP-1 and PARP-2 enzymes, respectively.It inhibits the repair of radiation-induced DNA double-strand breaks, activates apoptosis, and exhibits anti-tumor activity.

PARP阻害剤の選択性比較

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