PARP

Inhibitory Selectivity

Catalog No.	Inhibitor Name	PARP	PARP1	PARP2	PARP3	V-PARP	Tankyrase-1
A10111	Olaparib		***	****			*
A10026	Veliparib		***	***
A14182	Rucaparib	****
A11243	Talazoparib	****
A10046	AG-14361		***
A10475	INO-1001	**
A10019	A-966492		****	****
A15215	PJ34	***
A12665	PJ34 HCl	***
A11026	Niraparib		***	****	*	**	**
A12750	UPF 1069		*	**
A14309	ME0328		*		**
A14371	Benzamide	*
A15375	NU1025	**
A10164	Iniparib
A12393	AZD2461
A16344	BGP-15
A10045	AG-014699 (Rucaparib)	****
A15370	4-HQN	*
A15371	BYK 204165		*	*
A15372	BYK 49187		*	*
A15374	EB 47		**
A15373	DR 2313		*	**

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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AG14361

Catalog No. A10046
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PARP 抑制剂

AG14361是一种有效的PARP抑制剂，可在MMR（错配修复）有效/不足的细胞中增强替莫唑胺（TMZ）的细胞毒性。了解更多

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- Vimal Pandey, .et al. Roscovitine effectively enhances antitumor activity of temozolomide in vitro and in vivo mediated by increased autophagy and Caspase-3 dependent apoptosis, Scientific Reports, 2019, 9, Article number: 5012
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BMN-673 8R,9S

Catalog No. A15024
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PARP 抑制剂

BMN-673 8R,9S 是BMN-673的（8R，9S）对映异构体。BMN 673是一种新型PARP抑制剂，IC50为0.58 nM。了解更多

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Olaparib (AZD2281)

Catalog No. A10111
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PARP 抑制剂

Olaparib (AZD2281)是聚ADP核糖聚合酶（PARP）的抑制剂，该酶是一种与DNA修复有关的酶。了解更多

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- Saptarshi Sinha, .et al. Olaparib enhances the Resveratrol-mediated apoptosis in breast cancer cells by inhibiting the homologous recombination repair pathway, Exp Cell Res, 2022, Nov 1;420(1):113338 PMID: 36075449
- Subhajit Chatterjee, .et al. Combination of talazoparib and olaparib enhanced the curcumin-mediated apoptosis in oral cancer cells by PARP-1 trapping, J Cancer Res Clin Oncol, 2022, Dec;148(12):3521-3535 PMID: 35962813
- Yuki Uchihara, .et al. DNA damage promotes HLA class I presentation by stimulating a pioneer round of translation-associated antigen production, Mol Cell, 2022, Jul 21;82(14):2557-2570 PMID: 35594857
- Ji-Ye Kim, .et al. ARL6IP5 reduces cisplatin-resistance by suppressing DNA repair and promoting apoptosis pathways in ovarian carcinoma, Cell Death Dis, 2022, Mar 15;13(3):239 PMID: 35293383
- Emad Matanes, .et al. Inhibition of Poly ADP-Ribose Glycohydrolase Sensitizes Ovarian Cancer Cells to Poly ADP-Ribose Polymerase Inhibitors and Platinum Agents, Front Oncol, 2021, Oct 27;11:745981 PMID: 34778062
- Shino Endo, .et al. BRCA1/ATF1-Mediated Transactivation is Involved in Resistance to PARP Inhibitors and Cisplatin, Cancer Res Commun, 2021, 1(2): 90-105
- Yan Baglo, .et al. Evolutionary dynamics of cancer multidrug resistance in response to olaparib and photodynamic therapy, Transl Oncol, 2021, Nov;14(11):101198 PMID: 34418731
- Joseph M Gozgit, .et al. PARP7 negatively regulates the type I interferon response in cancer cells and its inhibition triggers antitumor immunity, Cancer cell, 2021, Jul 22;S1535-6108(21)00340-8 PMID: 34375612
- Sefinew Molla, .et al. Olaparib enhances curcumin-mediated apoptosis in oral cancer cells by inducing PARP trapping through modulation of BER and chromatin assembly, DNA Repair (Amst), 2021, Jun 10;105:103157 PMID: 34144488
- Jianming Wang, .et al. Persistence of RNA transcription during DNA replication delays duplication of transcription start sites until G2/M, Cell Rep, 2021, Feb 16;34(7):108759 PMID: 33596418
- Ai Ito, .et al. Metolazone upregulates mitochondrial chaperones and extends lifespan in Caenorhabditis elegans, Biogerontology, 2021, Feb;22(1):119-131 PMID: 33216250
- Tim J Wigle, .et al. In Vitro and Cellular Probes to Study PARP Enzyme Target Engagement, Cell Chem Biol, 2020, Jul 16;27(7):877-887 PMID: 32679093
- Ali Divan, .et al. Structurally unique PARP-1 inhibitors for the treatment of prostate cancer, Pharmacol Res Perspect, 2020, Apr; 8(2): e00586 PMID: 32342655
- Jianwei Dou, .et al. Development and evaluation of poly adenosine 5'-diphosphate-ribose polymerase 1 immobilization-based receptor chromatography, J Sep Sci, 2020, Dec 4 PMID: 33275824
- Sai Dimple Manavitha Gullipalli, .et al. Development and Validation of Bioanalytical Method for Estimation of Niraparib in Rat Plasma Using High Performance LC-MS/MS And Its Application to Pharmacokinetic Study, Int. J. Adv. Pharm. Biotech, 2020, 6(2) 01-08
- Chao Zhang, .et al. Phenotypic Switching of Atherosclerotic Smooth Muscle Cells is Regulated by Activated PARP1-Dependent TET1 Expression, J Atheroscler Thromb, 2020, Sep 25 PMID: 32981917
- Wigle TJ, .et al. Forced Self-Modification Assays as a Strategy to Screen MonoPARP Enzymes, SLAS Discov, 2019, Dec 19:2472555219883623 PMID: 31855104
- Wang Q, .et al. Biguanides in combination with olaparib limits tumorigenesis of drug-resistant ovarian cancer cells through inhibition of Snail, Cancer Med, 2019, Dec 21 PMID: 31863638
- Molla S, .et al. PARP inhibitor Olaparib Enhances the Apoptotic Potentiality of Curcumin by Increasing the DNA Damage in Oral Cancer Cells through Inhibition of BER Cascade, Pathol Oncol Res, 2019, Nov 25 PMID: 31768967
- Alvin Z.Lu, .et al. Enabling drug discovery for the PARP protein family through the detection of mono-ADP-ribosylation, Biochem Pharmacol, 2019, May 7. pii: S0006-2952(19)30171-6 PMID: 31075269
- Bian C, .et al. NADP+ is an endogenous PARP inhibitor in DNA damage response and tumor suppression, Nat Commun, 2019, Feb 11;10(1):693 PMID: 30741937
- HC de Silva, .et al. IGFBP-3 interacts with NONO and SFPQ in PARP-dependent DNA damage repair in triple-negative breast cancer, Cell Mol Life Sci, 2019, 1-16 PMID: 30725116
- Kamada Y, .et al. Castalagin and vescalagin purified from leaves of Syzygium samarangense (Blume) Merrill & L.M. Perry: Dual inhibitory activity against PARP1 and DNA topoisomerase II, Fitoterapia, 2018, Sep;129:94-101 PMID: 29928967
- 2018, .et al. Augmentation of the therapeutic efficacy of WEE1 kinase inhibitor AZD1775 by inhibiting the YAP-E2F1-DNA damage response pathway axis, FEBS Open Bio, 2018, Jun; 8(6): 1001-1012 PMID: 29928579
- Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
- Hiro Sato, .et al. DNA double-strand break repair pathway regulates PD-L1 expression in cancer cells, Nat Commun, 2017, 8: 1751 PMID: 29170499
- Charles-André Philip, .et al. Inhibition of PI3K-AKT-mTOR pathway sensitizes endometrial cancer cell lines to PARP inhibitors, BMC Cancer, 2017, 17: 638 PMID: 28886696
- Rulina AV, .et al. Distinct outcomes of CRL-Nedd8 pathway inhibition reveal cancer cell plasticity, Cell Death Dis, 2016, Dec 1;7(12):e2505 PMID: 27906189
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PJ 34 hydrochloride

Catalog No. A12665
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PARP 抑制剂

PJ 34 hydrochloride是聚（ADP-核糖）聚合酶（PARP）（EC50 = 20 nM）的有效抑制剂。了解更多

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- Alvin Z.Lu, .et al. Enabling drug discovery for the PARP protein family through the detection of mono-ADP-ribosylation, Biochem Pharmacol, 2019, May 7. pii: S0006-2952(19)30171-6 PMID: 31075269
- Wigle TJ, .et al. Forced Self-Modification Assays as a Strategy to Screen MonoPARP Enzymes, SLAS Discov, 2019, Dec 19:2472555219883623 PMID: 31855104
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3-Aminobenzamide

Catalog No. A10475
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PARP 抑制剂

3-Aminobenzamide是一种新型PARP抑制剂，已知它通过抑制DNA损伤的修复使细胞在体外对辐射敏感。了解更多

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- Kamada Y, .et al. Castalagin and vescalagin purified from leaves of Syzygium samarangense (Blume) Merrill & L.M. Perry: Dual inhibitory activity against PARP1 and DNA topoisomerase II, Fitoterapia, 2018, Sep;129:94-101 PMID: 29928967
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PJ34

Catalog No. A15215
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PARP 抑制剂

PJ34是新型有效的PARP-1/2特异性抑制剂，EC50为20 nM。了解更多

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- Tim J Wigle, .et al. In Vitro and Cellular Probes to Study PARP Enzyme Target Engagement, Cell Chem Biol, 2020, Jul 16;27(7):877-887 PMID: 32679093
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AG-014699 (Rucaparib)

Catalog No. A10045
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PARP 抑制剂

AG-014699 (Rucaparib)是一种PARP抑制剂，可抑制聚（ADP-核糖）聚合酶（PARP，后者是DNA修复中的关键酶。无细胞试验中作用于PARP1的Ki为1.4 nM，对其余8个PARP位点也有结合亲和力。了解更多

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- Tahira Baloch, .et al. Sequential therapeutic targeting of ovarian Cancer harboring dysfunctional BRCA1, BMC Cancer, 2019, Jan 10;19(1):44 PMID: 30630446
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AZD-2461

Catalog No. A12393
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PARP 抑制剂

AZD2461是新型有效的PARP抑制剂，对P-糖蛋白的亲和力较低。了解更多

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BGP-15

Catalog No. A16344
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PARP 抑制剂

BGP-15是一种PARP抑制剂，可以预防小鼠的心力衰竭和心房颤动。了解更多

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ABT-888 (Veliparib)

Catalog No. A10026
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PARP 抑制剂

ABT-888 (Veliparib)是一种潜在的抗癌药物，可作为PARP抑制剂。了解更多

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- Subhajit Chatterjee, .et al. PARP inhibitor Veliparib (ABT-888) enhances the anti-angiogenic potentiality of Curcumin through deregulation of NECTIN-4 in oral cancer: Role of nitric oxide (NO), Cell Signal, 2021, Apr;80:109902 PMID: 33373686
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BMN673

Catalog No. A11243
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PARP 抑制剂

BMN-673是核酶聚（ADP-核糖）聚合酶（PARP）的口服生物利用抑制剂，无细胞试验中对PARP1的IC50为0.57 nM。它也是有效的PARP-2抑制剂，但不抑制PARG，对PTEN突变型高度敏感。具有潜在的抗肿瘤活性。了解更多

Product Citations (2)

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- Subhajit Chatterjee, .et al. Combination of talazoparib and olaparib enhanced the curcumin-mediated apoptosis in oral cancer cells by PARP-1 trapping, J Cancer Res Clin Oncol, 2022, Dec;148(12):3521-3535 PMID: 35962813
- Charles-André Philip, .et al. Inhibition of PI3K-AKT-mTOR pathway sensitizes endometrial cancer cell lines to PARP inhibitors, BMC Cancer, 2017, 17: 638 PMID: 28886696
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NU 1025

Catalog No. A15375
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PARP 抑制剂

NU 1025是一种有效的聚（ADP-核糖）聚合酶（PARP）抑制剂，可增强L1210细胞中一系列机制多样的抗癌药的细胞毒性。了解更多

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4-HQN

Catalog No. A15370
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PARP 抑制剂

4-HQN已显示抑制PARP（聚（ADP-核糖）合成酶），该酶催化NAD+的ADP-核糖部分与各种蛋白质的共价结合。了解更多

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