PARP

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Isoform-specific Inhibitors

PARP Products

All (38) PARP Inhibitors (36) PARP Activators (1) PARP Modulators (1)

Catalog No.	Information	Product Use Citations	Product Validations
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.	Mol Cell, 2021, 81(2):340-354.e5 Nucleic Acids Res, 2021, gkaa1290 Free Radic Biol Med, 2021, 164:369-380	Role of PARP and BER in the synergy between PTX and GMX in A549 cells. A) Cells were pre-treated +/- 1 uM olaparib (2h) then sequentially +/- 150nM PTX (24h) then +/- GMX 12nM (48h). Cells were harvested for (left) NAD+ quantification by LC-MS/MS (mean +/-SD of quadruplicates) or (right) viability by CellTiter-Glo (mean +/-SD of duplicates) B) PAR modification of proteins and γ-H2AX levels were measured in extracts treated as in A) by western blotting.
S1004	Veliparib (ABT-888) Veliparib (ABT-888, NSC 737664) is a potent inhibitor of PARP1 and PARP2 with K_i 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.	Mol Med Rep, 2021, 23(1)40 Mol Cell, 2020, S1097-2765(20)30902-3 Mol Cell, 2020, S1097-2765(20)30898-4	Number of foci detected using laser confocal microscopy and fluorescent Fluor 647 anti-H2A.X-phosphorylated (Ser139) antibody. Double-stranded breaks (red) are clearly augmented in cells incubated with 500 nmol/l of ABT-888 and 500 nmol/l of AZD-2281 compared with PBS and 1% dimethyl sulfoxide controls. Image analysis was performed using ImageJ and the ‘analyze particle’ function.
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.	Theranostics, 2021, 11(6):2966-2986 Stem Cells, 2021, 10.1002/stem.3328 Chemosphere, 2021, 263:128125	Fluorescence microscopy of pSuper or Cdo shRNA expressing P19 cells at ITS1 immunostained withβ-tubulin III antibodies. Size bar=100 um. P19/control or P19/Cdo shRNA cells were treated with DMSO or XAV939 in the differentiation medium for 72 h followed by immunostaining.
S1098	Rucaparib (AG-014699) phosphate Rucaparib (AG-014699, PF-01367338) is an inhibitor of PARP with K_i of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. Phase 3.	Cancer Cell, 2020, 37(2):157-167 Cell Rep, 2020, 33(2):108240 Elife, 2020, 9e60637	For anchorage dependent clonogenic assays, HER2+ breast cancer BT474 cells were seeded at low density in 6-well plates and allowed to adhere overnight. The next day, olaparib and rucaparib were added at the indicated concentrations. Media and drugs were replenished every three days. After 10-15 days, depending on cell proliferation rate, cells were fixed and stained with crystal violet. Images and graphs indicate the results compared to control condition. Data are mean ± S.D. n.s.: non-significant, ∗p < 0.05, ∗∗p < 0.01, ∗∗∗p < 0.001.
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.	PLoS Pathog, 2020, 21;16(4):e1008474 Int J Oncol, 2015, 47(1):262-8 J Breast Cancer, 2015, 18(4):329-38	Immunoblot analysis of PARylation after treatment with various PARP inhibitors.The asterisk indicates a nonspecific band.
S9712^New	Fluzoparib (SHR-3162) Fluzoparib (SHR3162, HS10160) is a potent Poly (ADP-ribose) polymerase (PARP) inhibitor that shows anti-tumor activity.
S6899^New	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.
S6882^New	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.
S8992^New	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^New	RBN-2397 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.
S0732^New	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.
S8876^New	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.
S0519^New	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.
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.	Nat Cell Biol, 2021, 10.1038/s41556-020-00624-3 Mol Cell, 2021, 81(2):340-354.e5 Sci Rep, 2021, 11(1):1234	Western blot assessment of effects on PAR, PARP, and dsDNA breaks mediated by IMMU-132 plus PARPi in TNBC tumor lines. Cells were plated overnight in 6-well plates before the addition of chemotherapeutics. After a 24-hour incubation, cells were harvested and cell lysates resolved and transferred for Western analysis as described in Materials and Methods. PAR and FL-PARP levels were determined on the same gel. Assessment of dsDNA breaks (p-H2A.X) was calculated as ratios relative to untreated control (Unt) normalized to b-actin protein loading control (Dp-H2A.X). B, HCC1806 cells exposed to rucaparib (Ruc) and IMMU-132 or to (C) talazoparib (Tala) and IMMU-132.
S2178	AG-14361 AG14361 is a potent inhibitor of PARP1 with K_i of <5 nM in a cell-free assay. It is at least 1000-fold more potent than the benzamides.	J Clin Med, 2020, 30;9(4) Nature, 2019, 572(7768):254-259 PLoS One, 2019, 14(4):e0215277	Immunoblot analysis of PARylation after treatment with various PARP inhibitors.The asterisk indicates a nonspecific band.
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.	Acta Pharm Sin B, 2019, 9(4):782-793 J Cell Biochem, 2017, 118(11):3943-3952 J Biol Chem, 2015, 290(48):28675-82	Effect of DPQ and INO-1001 on ADP-, collagen- or PAR1ap-induced platelet aggregation. Human PRP samples were preincubated with PARP inhibitor (50 μM) or its vehicle and then stimulated with ADP (1.5 to 5 μM; to produce a biphasic aggregation curve), collagen (1 to 2 μg/ml) or PAR1ap (1 to 2 μM). Results are expressed relatively to platelet agonist alone (=vehicle group; normalized to 100%) and presented as the mean±SD (n=5-6).
S2197	A-966492 A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with K_i of 1 nM and 1.5 nM, respectively.	J Clin Med, 2020, 30;9(4) Int J Cance, 2019, 144(2):297-310 Cancer Immunol Res, 2019,	Immunoblot analysis of PARylation after treatment with various PARP inhibitors.The asterisk indicates a nonspecific band.
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.	Nat Commun, 2020, 11(1):3018 Glia, 2020, 10.1002/glia.23790 J Clin Med, 2020, 30;9(4)	LN229 GBM cells were treated with PJ34 (20 µM), TRAIL (200 ng/ml) or the combination of both and analyzed for the expression of DR5, caspase-9 (CP9) and cleaved caspase-3 (cCP3). The vertical line on the immunoblot indicates that the first and second samples were noncontiguous, but run on the same gel simultaneously with the other samples.
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.	J Exp Clin Cancer Res, 2021, 40(1):15 Cancer Cell, 2020, 15 pii: S1535-6108(20)30164-1 Sci Adv, 2020, 6(51)eabb8626	PARP1 silencing rescues PARP1/2 inhibitor sensitivity in the ERCC1-deficient population. Effect of PARP1 knockdown by siRNA on sensitivity of ERCC1-isogenic cell lines to niraparib. Cells were reverse-transfected with PARP1 siRNA and drug was added 48 h after transfection. Cells were exposed to the drug for 5 days. Error bars represent the s.d. from the mean of three independent experiments.
S8038	UPF 1069 UPF 1069 is a selective PARP2 inhibitor with IC50 of 0.3 μM. It is ~27-fold selective against PARP1.	J Clin Med, 2020, 30;9(4) Biochem Pharmacol, 2019, 10.1016/j.bcp.2019.05.007 Mol Med Rep, 2019, 20(4):3609-3616
S7029	AZD2461 AZD2461 is a novel PARP inhibitor with low affinity for Pgp than Olaparib. Phase 1.	Dev Cell, 2020, 20;53(2):240-252 J Clin Med, 2020, 30;9(4) J Cancer Res Clin Oncol, 2019, 145(1):137-152.	(b) Hoechst-positive cell quantification of caspase and PARP inhibitors and their effect on ARPE-19 cells undergoing UOS in the presence and absence of NPD1 (lower panel). Bars represent data averages of three repeats (technical replicas) of three independent experiments (biological replicas). *P<0.05
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	Colony survival assay in wild-type A549 cells treated with vehicle, 3.0 μM ME0328 or 500 nM KU58948 and pyridostatin.
S6739	MN 64 MN-64 is a potent inhibitor of TNKS1 and TNKS2 with IC50 value of 6 and 72 nM, respectively.
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.
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.	Nat Commun, 2020, 22;11(1):2573 Cell Rep, 2020, 31(10):107745 Cancer Discov, 2020, CD-20-0818	Berberine activates PARP1 in ovarian cancer cells. PAR synthesis is detected by immunofluorescence staining in A2780 and HO8910 treated with different concentration of berberine alone or in combination with niraparib (10 μM) for 48 h. Top: representative examples of immunofluorescence staining of PAR. Scale bar, 20 μm. Bottom: quantification of PAR level in A2780 and HO8910. Immunofluorescence intensities were quantified by ImageJ. P<0.05, *P<0.01
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
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.	Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-19-2549
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	Western blot analysis of SH3BP2 in WT BMMs after culture for 2 days in the presence of IWR-1 (2 μM), G007-LK (0.1 μM), or ICG001 (2 μM).
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
S8419	E7449 E7449 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.	J Clin Med, 2020, 30;9(4)
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.
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).	J Clin Med, 2020, 30;9(4) Biochem Pharmacol, 2019, 10.1016/j.bcp.2019.05.007 Mol Med Rep, 2019, 20(4):3609-3616
S7490	WIKI4 WIKI4 is a novel Tankyrase inhibitor with IC50 of 15 nM for TNKS2, and leads to inhibition of Wnt/beta-catenin signaling.	Carcinogenesis, 2020, 41(7):993-1004 Nat Commun, 2019, 10(1):4363
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
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).
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.
S0913^New	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.
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.	Antiviral Res, 2020, 186:105000 Oncol Rep, 2018, 40(3):1525-1532 Shandong University, 2014, Haoran Cui

Catalog No.	Information	Product Use Citations	Product Validations
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.	Mol Cell, 2021, 81(2):340-354.e5 Nucleic Acids Res, 2021, gkaa1290 Free Radic Biol Med, 2021, 164:369-380	Role of PARP and BER in the synergy between PTX and GMX in A549 cells. A) Cells were pre-treated +/- 1 uM olaparib (2h) then sequentially +/- 150nM PTX (24h) then +/- GMX 12nM (48h). Cells were harvested for (left) NAD+ quantification by LC-MS/MS (mean +/-SD of quadruplicates) or (right) viability by CellTiter-Glo (mean +/-SD of duplicates) B) PAR modification of proteins and γ-H2AX levels were measured in extracts treated as in A) by western blotting.
S1004	Veliparib (ABT-888) Veliparib (ABT-888, NSC 737664) is a potent inhibitor of PARP1 and PARP2 with K_i 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.	Mol Med Rep, 2021, 23(1)40 Mol Cell, 2020, S1097-2765(20)30902-3 Mol Cell, 2020, S1097-2765(20)30898-4	Number of foci detected using laser confocal microscopy and fluorescent Fluor 647 anti-H2A.X-phosphorylated (Ser139) antibody. Double-stranded breaks (red) are clearly augmented in cells incubated with 500 nmol/l of ABT-888 and 500 nmol/l of AZD-2281 compared with PBS and 1% dimethyl sulfoxide controls. Image analysis was performed using ImageJ and the ‘analyze particle’ function.
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.	Theranostics, 2021, 11(6):2966-2986 Stem Cells, 2021, 10.1002/stem.3328 Chemosphere, 2021, 263:128125	Fluorescence microscopy of pSuper or Cdo shRNA expressing P19 cells at ITS1 immunostained withβ-tubulin III antibodies. Size bar=100 um. P19/control or P19/Cdo shRNA cells were treated with DMSO or XAV939 in the differentiation medium for 72 h followed by immunostaining.
S1098	Rucaparib (AG-014699) phosphate Rucaparib (AG-014699, PF-01367338) is an inhibitor of PARP with K_i of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. Phase 3.	Cancer Cell, 2020, 37(2):157-167 Cell Rep, 2020, 33(2):108240 Elife, 2020, 9e60637	For anchorage dependent clonogenic assays, HER2+ breast cancer BT474 cells were seeded at low density in 6-well plates and allowed to adhere overnight. The next day, olaparib and rucaparib were added at the indicated concentrations. Media and drugs were replenished every three days. After 10-15 days, depending on cell proliferation rate, cells were fixed and stained with crystal violet. Images and graphs indicate the results compared to control condition. Data are mean ± S.D. n.s.: non-significant, ∗p < 0.05, ∗∗p < 0.01, ∗∗∗p < 0.001.
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.	PLoS Pathog, 2020, 21;16(4):e1008474 Int J Oncol, 2015, 47(1):262-8 J Breast Cancer, 2015, 18(4):329-38	Immunoblot analysis of PARylation after treatment with various PARP inhibitors.The asterisk indicates a nonspecific band.
S9712^New	Fluzoparib (SHR-3162) Fluzoparib (SHR3162, HS10160) is a potent Poly (ADP-ribose) polymerase (PARP) inhibitor that shows anti-tumor activity.
S6899^New	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.
S6882^New	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.
S8992^New	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^New	RBN-2397 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.
S0732^New	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.
S8876^New	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.
S0519^New	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.
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.	Nat Cell Biol, 2021, 10.1038/s41556-020-00624-3 Mol Cell, 2021, 81(2):340-354.e5 Sci Rep, 2021, 11(1):1234	Western blot assessment of effects on PAR, PARP, and dsDNA breaks mediated by IMMU-132 plus PARPi in TNBC tumor lines. Cells were plated overnight in 6-well plates before the addition of chemotherapeutics. After a 24-hour incubation, cells were harvested and cell lysates resolved and transferred for Western analysis as described in Materials and Methods. PAR and FL-PARP levels were determined on the same gel. Assessment of dsDNA breaks (p-H2A.X) was calculated as ratios relative to untreated control (Unt) normalized to b-actin protein loading control (Dp-H2A.X). B, HCC1806 cells exposed to rucaparib (Ruc) and IMMU-132 or to (C) talazoparib (Tala) and IMMU-132.
S2178	AG-14361 AG14361 is a potent inhibitor of PARP1 with K_i of <5 nM in a cell-free assay. It is at least 1000-fold more potent than the benzamides.	J Clin Med, 2020, 30;9(4) Nature, 2019, 572(7768):254-259 PLoS One, 2019, 14(4):e0215277	Immunoblot analysis of PARylation after treatment with various PARP inhibitors.The asterisk indicates a nonspecific band.
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.	Acta Pharm Sin B, 2019, 9(4):782-793 J Cell Biochem, 2017, 118(11):3943-3952 J Biol Chem, 2015, 290(48):28675-82	Effect of DPQ and INO-1001 on ADP-, collagen- or PAR1ap-induced platelet aggregation. Human PRP samples were preincubated with PARP inhibitor (50 μM) or its vehicle and then stimulated with ADP (1.5 to 5 μM; to produce a biphasic aggregation curve), collagen (1 to 2 μg/ml) or PAR1ap (1 to 2 μM). Results are expressed relatively to platelet agonist alone (=vehicle group; normalized to 100%) and presented as the mean±SD (n=5-6).
S2197	A-966492 A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with K_i of 1 nM and 1.5 nM, respectively.	J Clin Med, 2020, 30;9(4) Int J Cance, 2019, 144(2):297-310 Cancer Immunol Res, 2019,	Immunoblot analysis of PARylation after treatment with various PARP inhibitors.The asterisk indicates a nonspecific band.
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.	Nat Commun, 2020, 11(1):3018 Glia, 2020, 10.1002/glia.23790 J Clin Med, 2020, 30;9(4)	LN229 GBM cells were treated with PJ34 (20 µM), TRAIL (200 ng/ml) or the combination of both and analyzed for the expression of DR5, caspase-9 (CP9) and cleaved caspase-3 (cCP3). The vertical line on the immunoblot indicates that the first and second samples were noncontiguous, but run on the same gel simultaneously with the other samples.
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.	J Exp Clin Cancer Res, 2021, 40(1):15 Cancer Cell, 2020, 15 pii: S1535-6108(20)30164-1 Sci Adv, 2020, 6(51)eabb8626	PARP1 silencing rescues PARP1/2 inhibitor sensitivity in the ERCC1-deficient population. Effect of PARP1 knockdown by siRNA on sensitivity of ERCC1-isogenic cell lines to niraparib. Cells were reverse-transfected with PARP1 siRNA and drug was added 48 h after transfection. Cells were exposed to the drug for 5 days. Error bars represent the s.d. from the mean of three independent experiments.
S8038	UPF 1069 UPF 1069 is a selective PARP2 inhibitor with IC50 of 0.3 μM. It is ~27-fold selective against PARP1.	J Clin Med, 2020, 30;9(4) Biochem Pharmacol, 2019, 10.1016/j.bcp.2019.05.007 Mol Med Rep, 2019, 20(4):3609-3616
S7029	AZD2461 AZD2461 is a novel PARP inhibitor with low affinity for Pgp than Olaparib. Phase 1.	Dev Cell, 2020, 20;53(2):240-252 J Clin Med, 2020, 30;9(4) J Cancer Res Clin Oncol, 2019, 145(1):137-152.	(b) Hoechst-positive cell quantification of caspase and PARP inhibitors and their effect on ARPE-19 cells undergoing UOS in the presence and absence of NPD1 (lower panel). Bars represent data averages of three repeats (technical replicas) of three independent experiments (biological replicas). *P<0.05
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	Colony survival assay in wild-type A549 cells treated with vehicle, 3.0 μM ME0328 or 500 nM KU58948 and pyridostatin.
S6739	MN 64 MN-64 is a potent inhibitor of TNKS1 and TNKS2 with IC50 value of 6 and 72 nM, respectively.
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.
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.	Nat Commun, 2020, 22;11(1):2573 Cell Rep, 2020, 31(10):107745 Cancer Discov, 2020, CD-20-0818	Berberine activates PARP1 in ovarian cancer cells. PAR synthesis is detected by immunofluorescence staining in A2780 and HO8910 treated with different concentration of berberine alone or in combination with niraparib (10 μM) for 48 h. Top: representative examples of immunofluorescence staining of PAR. Scale bar, 20 μm. Bottom: quantification of PAR level in A2780 and HO8910. Immunofluorescence intensities were quantified by ImageJ. P<0.05, *P<0.01
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
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.	Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-19-2549
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	Western blot analysis of SH3BP2 in WT BMMs after culture for 2 days in the presence of IWR-1 (2 μM), G007-LK (0.1 μM), or ICG001 (2 μM).
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
S8419	E7449 E7449 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.	J Clin Med, 2020, 30;9(4)
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.
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).	J Clin Med, 2020, 30;9(4) Biochem Pharmacol, 2019, 10.1016/j.bcp.2019.05.007 Mol Med Rep, 2019, 20(4):3609-3616
S7490	WIKI4 WIKI4 is a novel Tankyrase inhibitor with IC50 of 15 nM for TNKS2, and leads to inhibition of Wnt/beta-catenin signaling.	Carcinogenesis, 2020, 41(7):993-1004 Nat Commun, 2019, 10(1):4363
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
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).
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.

Catalog No.	Information	Product Use Citations	Product Validations
S0913^New	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.

Catalog No.

Information

Product Use Citations

Product Validations

S0913^New

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.

Catalog No.	Information	Product Use Citations	Product Validations
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.	Antiviral Res, 2020, 186:105000 Oncol Rep, 2018, 40(3):1525-1532 Shandong University, 2014, Haoran Cui

Catalog No.

Information

Product Use Citations

Product Validations

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.

Antiviral Res, 2020, 186:105000

Oncol Rep, 2018, 40(3):1525-1532

Shandong University, 2014, Haoran Cui