PARP

Choose Selective PARP Inhibitors

PARP Signaling Pathway Map

PARP Signaling Pathways

PARP Products

  • All (43)
  • PARP Inhibitors (40)
  • PARP Modulators (3)
  • New PARP Products
Catalog No. Product Name Information Product Use Citations Product Validations
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
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.
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.
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.
Cell, 2022, 185(11):1943-1959.e21
Cell, 2022, 185(1):169-183.e19
Mol Cell, 2022, S1097-2765(22)00085-5
S1060 Olaparib (AZD2281) Olaparib (AZD2281, KU0059436) is a selective inhibitor of PARP1/2 with IC50 of 5 nM/1 nM in cell-free assays, 300-times less effective against tankyrase-1. Olaparib induces significant autophagy that is associated with mitophagy in cells with BRCA mutations.
Cell, 2022, 185(1):169-183.e19
Cancer Cell, 2022, S1535-6108(21)00662-0
Nat Cell Biol, 2022, 24(1):51-61
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.
Front Oncol, 2021, 11:773186
Nat Commun, 2021, 12(1):736
PLoS Pathog, 2020, 21;16(4):e1008474
S1098 Rucaparib (AG-014699) phosphate Rucaparib (AG-014699, PF-01367338) 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.
Mol Cell, 2022, S1097-2765(22)00394-X
Cancer Lett, 2022, 530:29-44
Mol Cancer Ther, 2022, molcanther.0798.2021
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.
Cell Death Discov, 2021, 7(1):181
Acta Pharm Sin B, 2019, 9(4):782-793
J Cell Biochem, 2017, 118(11):3943-3952
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.
Cancer Discov, 2022, candisc.0680.2021
Cell Res, 2022, 10.1038/s41422-022-00668-0
Nat Commun, 2022, 13(1):2548
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.
Cell Stem Cell, 2022, S1934-5909(22)00010-8
J Neurochem, 2022, 10.1111/jnc.15606
Front Cell Dev Biol, 2021, 9:621906
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.
Front Immunol, 2021, 12:712021
bioRxiv, 2021, 10.1101/2020.10.18.333070
Nat Commun, 2021, 12(1):736
S2741 Niraparib (MK-4827) Niraparib (MK-4827) is a selective inhibitor of PARP1/2 with IC50 of 3.8 nM/2.1 nM, with great activity in cancer cells with mutant BRCA-1 and BRCA-2. It is >330-fold selective against PARP3, V-PARP and Tank1. Niraparib can form PARP–DNA complexes resulting in DNA damage, apoptosis, and cell death. Phase 3.
Nucleic Acids Res, 2022, 50(7):3958-3973
Mol Cancer Ther, 2022, molcanther.0604.2021
Sci Transl Med, 2021, 13(592)eabc7211
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.
S4715 Benzamide Benzamide, a derivative of benzoic acid, is an inhibitor of poly(ADP-ribose) polymerase with an IC50 of 3.3 μM.
Int J Mol Sci, 2019, 20(21)
Mol Pharmacol, 2019, 96(4):419-429
Acta Neuropathol Commun, 2014, 2:57
S4948 Rucaparib Rucaparib (Rubraca, AG014699, PF01367338) 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.
Mol Cancer Ther, 2022, 21(4):647-657
Int J Mol Sci, 2022, 23(10)5770
Cancer Lett, 2021, S0304-3835(21)00571-1
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.
Int J Mol Sci, 2022, 23(10)5770
J Exp Clin Cancer Res, 2021, 40(1):276
Cell Death Dis, 2021, 12(6):546
S6739 MN 64 MN-64 is a potent inhibitor of TNKS1 and TNKS2 with IC50 value of 6 and 72 nM, respectively.
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).
Chin J Integr Med, 2021, 10.1007/s11655-021-3282-0
Oncotarget, 2021, 12(7):674-685
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.
S7029 AZD2461 AZD2461 is a novel PARP inhibitor with low affinity for Pgp than Olaparib. Phase 1.
Cell Chem Biol, 2021, S2451-9456(21)00058-1
Nat Commun, 2021, 12(1):736
Dev Cell, 2020, 53(2):240-252.e7
S7048 Talazoparib (BMN 673) Talazoparib (BMN 673, LT-673) is a novel PARP inhibitor with IC50 of 0.57 nM for PARP1 in a cell-free assay. It is also a potent inhibitor of PARP-2, but does not inhibit PARG and is highly sensitive to PTEN mutation. Phase 3.
Cell, 2022, 185(1):169-183.e19
Mol Cell, 2022, S1097-2765(22)00394-X
Mol Cell, 2022, 82(10):1924-1939.e10
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.
Med Sci Monit, 2018, 24: 5914–5924
Med Sci Monit, 2018, 24:5914-5924
S7239 G007-LK G007-LK is a potent and selective tankyrase inhibitor with IC50 of 46 nM and 25 nM for TNKS1/2, respectively.
J Clin Med, 2020, 30;9(4)
Cancer Discov, 2020, 6 pii: CD-19-1242
J Cell Sci, 2020, 14;jcs245811
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.
Cell Rep, 2022, 39(6):110792
J Neurochem, 2022, 10.1111/jnc.15606
Nat Commun, 2021, 12(1):6362
S7438 ME0328 ME0328 is a potent and selective PARP inhibitor with IC50 of 0.89 μM for PARP3, about 7-fold selectivity over PARP1.
Mol Cancer Ther, 2018, 17(10):2206-2216
SLAS Discov, 2018, 23(6):545-553
Breast Cancer Res Treat, 2018, 172(1):23-32
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
S7625 Niraparib (MK-4827) tosylate Niraparib tosylate (MK-4827, ZEJULA) 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.
Sci Transl Med, 2021, 13(592)eabc7211
Sci Adv, 2021, 7(21)eabf0197
Proc Natl Acad Sci U S A, 2021, 118(40)e2109252118
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
S8038 UPF 1069 UPF 1069 is a selective PARP2 inhibitor with IC50 of 0.3 μM. It is ~27-fold selective against PARP1.
Cell Death Differ, 2021, 10.1038/s41418-020-00733-4
J Clin Med, 2020, 30;9(4)
Biochem Pharmacol, 2019, 10.1016/j.bcp.2019.05.007
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).
bioRxiv, 2021, 10.1101/2020.10.18.333070
J Clin Med, 2020, 30;9(4)
Biochem Pharmacol, 2019, 10.1016/j.bcp.2019.05.007
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.
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.
bioRxiv, 2021, 10.1101/2020.10.18.333070
J Clin Med, 2020, 30;9(4)
S8592 Pamiparib (BGB-290) Pamiparib (BGB-290) 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.
Neuro Oncol, 2021, 23(6):920-931
Cell Rep, 2021, 36(4):109429
Front Immunol, 2021, 12:712021
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.
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.
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.
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.
S9712 Fluzoparib (SHR-3162)

Fluzoparib (SHR3162, HS10160) is a potent Poly (ADP-ribose) polymerase (PARP) inhibitor that shows anti-tumor activity.

S9875New AZD5305 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).
S9893New 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 (NSC 646666) Berberine chloride (NSC 646666, Natural Yellow 18) 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.
J Biomol Struct Dyn, 2022, 1-11
Front Pharmacol, 2021, 12:632201
Molecules, 2021, 26(5)1210
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 Pharmacol, 2021, 12:632201
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.
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
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.
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.
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.
Cell, 2022, 185(11):1943-1959.e21
Cell, 2022, 185(1):169-183.e19
Mol Cell, 2022, S1097-2765(22)00085-5
S1060 Olaparib (AZD2281) Olaparib (AZD2281, KU0059436) is a selective inhibitor of PARP1/2 with IC50 of 5 nM/1 nM in cell-free assays, 300-times less effective against tankyrase-1. Olaparib induces significant autophagy that is associated with mitophagy in cells with BRCA mutations.
Cell, 2022, 185(1):169-183.e19
Cancer Cell, 2022, S1535-6108(21)00662-0
Nat Cell Biol, 2022, 24(1):51-61
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.
Front Oncol, 2021, 11:773186
Nat Commun, 2021, 12(1):736
PLoS Pathog, 2020, 21;16(4):e1008474
S1098 Rucaparib (AG-014699) phosphate Rucaparib (AG-014699, PF-01367338) 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.
Mol Cell, 2022, S1097-2765(22)00394-X
Cancer Lett, 2022, 530:29-44
Mol Cancer Ther, 2022, molcanther.0798.2021
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.
Cell Death Discov, 2021, 7(1):181
Acta Pharm Sin B, 2019, 9(4):782-793
J Cell Biochem, 2017, 118(11):3943-3952
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.
Cancer Discov, 2022, candisc.0680.2021
Cell Res, 2022, 10.1038/s41422-022-00668-0
Nat Commun, 2022, 13(1):2548
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.
Cell Stem Cell, 2022, S1934-5909(22)00010-8
J Neurochem, 2022, 10.1111/jnc.15606
Front Cell Dev Biol, 2021, 9:621906
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.
Front Immunol, 2021, 12:712021
bioRxiv, 2021, 10.1101/2020.10.18.333070
Nat Commun, 2021, 12(1):736
S2741 Niraparib (MK-4827) Niraparib (MK-4827) is a selective inhibitor of PARP1/2 with IC50 of 3.8 nM/2.1 nM, with great activity in cancer cells with mutant BRCA-1 and BRCA-2. It is >330-fold selective against PARP3, V-PARP and Tank1. Niraparib can form PARP–DNA complexes resulting in DNA damage, apoptosis, and cell death. Phase 3.
Nucleic Acids Res, 2022, 50(7):3958-3973
Mol Cancer Ther, 2022, molcanther.0604.2021
Sci Transl Med, 2021, 13(592)eabc7211
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.
S4715 Benzamide Benzamide, a derivative of benzoic acid, is an inhibitor of poly(ADP-ribose) polymerase with an IC50 of 3.3 μM.
Int J Mol Sci, 2019, 20(21)
Mol Pharmacol, 2019, 96(4):419-429
Acta Neuropathol Commun, 2014, 2:57
S4948 Rucaparib Rucaparib (Rubraca, AG014699, PF01367338) 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.
Mol Cancer Ther, 2022, 21(4):647-657
Int J Mol Sci, 2022, 23(10)5770
Cancer Lett, 2021, S0304-3835(21)00571-1
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.
Int J Mol Sci, 2022, 23(10)5770
J Exp Clin Cancer Res, 2021, 40(1):276
Cell Death Dis, 2021, 12(6):546
S6739 MN 64 MN-64 is a potent inhibitor of TNKS1 and TNKS2 with IC50 value of 6 and 72 nM, respectively.
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).
Chin J Integr Med, 2021, 10.1007/s11655-021-3282-0
Oncotarget, 2021, 12(7):674-685
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.
S7029 AZD2461 AZD2461 is a novel PARP inhibitor with low affinity for Pgp than Olaparib. Phase 1.
Cell Chem Biol, 2021, S2451-9456(21)00058-1
Nat Commun, 2021, 12(1):736
Dev Cell, 2020, 53(2):240-252.e7
S7048 Talazoparib (BMN 673) Talazoparib (BMN 673, LT-673) is a novel PARP inhibitor with IC50 of 0.57 nM for PARP1 in a cell-free assay. It is also a potent inhibitor of PARP-2, but does not inhibit PARG and is highly sensitive to PTEN mutation. Phase 3.
Cell, 2022, 185(1):169-183.e19
Mol Cell, 2022, S1097-2765(22)00394-X
Mol Cell, 2022, 82(10):1924-1939.e10
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.
Med Sci Monit, 2018, 24: 5914–5924
Med Sci Monit, 2018, 24:5914-5924
S7239 G007-LK G007-LK is a potent and selective tankyrase inhibitor with IC50 of 46 nM and 25 nM for TNKS1/2, respectively.
J Clin Med, 2020, 30;9(4)
Cancer Discov, 2020, 6 pii: CD-19-1242
J Cell Sci, 2020, 14;jcs245811
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.
Cell Rep, 2022, 39(6):110792
J Neurochem, 2022, 10.1111/jnc.15606
Nat Commun, 2021, 12(1):6362
S7438 ME0328 ME0328 is a potent and selective PARP inhibitor with IC50 of 0.89 μM for PARP3, about 7-fold selectivity over PARP1.
Mol Cancer Ther, 2018, 17(10):2206-2216
SLAS Discov, 2018, 23(6):545-553
Breast Cancer Res Treat, 2018, 172(1):23-32
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
S7625 Niraparib (MK-4827) tosylate Niraparib tosylate (MK-4827, ZEJULA) 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.
Sci Transl Med, 2021, 13(592)eabc7211
Sci Adv, 2021, 7(21)eabf0197
Proc Natl Acad Sci U S A, 2021, 118(40)e2109252118
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
S8038 UPF 1069 UPF 1069 is a selective PARP2 inhibitor with IC50 of 0.3 μM. It is ~27-fold selective against PARP1.
Cell Death Differ, 2021, 10.1038/s41418-020-00733-4
J Clin Med, 2020, 30;9(4)
Biochem Pharmacol, 2019, 10.1016/j.bcp.2019.05.007
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).
bioRxiv, 2021, 10.1101/2020.10.18.333070
J Clin Med, 2020, 30;9(4)
Biochem Pharmacol, 2019, 10.1016/j.bcp.2019.05.007
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.
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.
bioRxiv, 2021, 10.1101/2020.10.18.333070
J Clin Med, 2020, 30;9(4)
S8592 Pamiparib (BGB-290) Pamiparib (BGB-290) 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.
Neuro Oncol, 2021, 23(6):920-931
Cell Rep, 2021, 36(4):109429
Front Immunol, 2021, 12:712021
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.
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.
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.
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.
S9712 Fluzoparib (SHR-3162)

Fluzoparib (SHR3162, HS10160) is a potent Poly (ADP-ribose) polymerase (PARP) inhibitor that shows anti-tumor activity.

S9875New AZD5305 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).
S9893New 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 (NSC 646666) Berberine chloride (NSC 646666, Natural Yellow 18) 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.
J Biomol Struct Dyn, 2022, 1-11
Front Pharmacol, 2021, 12:632201
Molecules, 2021, 26(5)1210
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 Pharmacol, 2021, 12:632201
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.
S9875New AZD5305 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).
S9893New 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.
Tags: PARP inhibition | PARP cancer | PARP inhibitor cancer | PARP signaling | PARP activity | PARP assay | PARP activity | PARP inhibitor trial | PARP activation | PARP inhibitors clinical trials | FDA approval PARP inhibitor | PARP inhibitor drugs | PARP phosphorylation | PARP inhibitor review