PARP

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PARP Inhibitors (14)

water-soluble

Cat.No. Product Name Information Product Use Citation Customer Product Validation
S1060 Olaparib (AZD2281, Ku-0059436) Olaparib (AZD2281, KU0059436) is a selective inhibitor of PARP1/2 with IC50 of 5 nM/1 nM, 300-times less effective against tankyrase-1. Phase 3.
  • Cell, 2011, 145(4):529-42
  • Science, 2013, 339(6120):700-4
  • Nat Methods , 2013, 10(10):981-4
S1004 Veliparib (ABT-888) Veliparib (ABT-888) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM, respectively. It is inactive to SIRT2. Phase 3.
  • Oncogene, 2014, 8.559
  • Cell Metab, 2014, 19(6):1034-41
  • J Cell Biol, 2014, 206(4):493-507
S1098 Rucaparib (AG-014699,PF-01367338) Rucaparib (AG-014699, PF-01367338) is an inhibitor of PARP with Ki of 1.4 nM for PARP1, also showing binding affinity to eight other PARP domains. Phase 3.
  • Nature, 2015, 518(7538):254-7
  • Nature, 2011, 470(7334):419-23
  • Nat Commun, 2014, 5:3361
S1087 Iniparib (BSI-201) Iniparib (BSI-201) is a PARP1 inhibitor with demonstrated effectiveness in triple-negative breast cancer (TNBC). Phase 3.
  • Nat Methods , 2013, 10(10):981-4
  • Cell Metab, 2014, 19(6):1034-41
  • Clin Cancer Res, 2013, 12(7):529-34
S7048 Talazoparib (BMN 673) Talazoparib (BMN 673) is a novel PARP inhibitor with IC50 of 0.58 nM. It is also a potent inhibitor of PARP-2, but does not inhibit PARG and is highly sensitive to PTEN mutation. Phase 3.
  • DNA Repair, 2015, 10.1016/j.dnarep.2015.02.004
  • Frontiers in Oncology, 2015, 4:368
S4273 3-Aminobenzamide 3-Aminobenzamide is a competitive PARP inhibitor with Ki of 1.8 μM.
S2178 AG-14361 AG14361 is a potent inhibitor of PARP1 with Ki of <5 nM. It is at least 1000-fold more potent than the benzamides.
  • Nature, 2015, 519(7543):370-3
  • Nat Methods , 2013, 10(10):981-4
  • Nucleic Acids Res, 2015, 43(2):875-92
S1132 INO-1001 INO-1001 is a potent inhibitor of PARP with IC50 of <50 nM in CHO cells and a mediator of oxidant-induced myocyte dysfunction during reperfusion. Phase 2.
S8038 UPF 1069 UPF 1069 is a selective PARP2 inhibitor with IC50 of 0.3 μM. It is ~27-fold selective against PARP1.
S7029 AZD2461 AZD2461 is a novel PARP inhibitor with low affinity for Pgp than Olaparib. Phase 1.
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.
  • Mol Cancer Ther, 2014, 13(6):1645-54
S7438 ME0328 ME0328 is a potent and selective PARP inhibitor with IC50 of 0.89 μM for PARP3, about 7-fold selectivity over PARP1.
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 Methods , 2013, 10(10):981-4
S2886 PJ34 PJ-34 is a PARP inhibitor with EC50 of 20 nM and is equally potent to PARP1/2.
  • PLoS One, 2014, 9(12):e114583

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Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
S1060 Olaparib (AZD2281, Ku-0059436) 0.002 mg/mL 86 mg/mL <1 mg/mL
S1004 Veliparib (ABT-888) <1 mg/mL 17 mg/mL <1 mg/mL
S1098 Rucaparib (AG-014699,PF-01367338) <1 mg/mL 84 mg/mL <1 mg/mL
S1087 Iniparib (BSI-201) <1 mg/mL 58 mg/mL 28 mg/mL
S7048 Talazoparib (BMN 673) <1 mg/mL 76 mg/mL <1 mg/mL
S4273 3-Aminobenzamide 6 mg/mL 27 mg/mL 10 mg/mL
S2178 AG-14361 <1 mg/mL 12 mg/mL <1 mg/mL
S1132 INO-1001 <1 mg/mL 27 mg/mL 27 mg/mL
S8038 UPF 1069 <1 mg/mL 56 mg/mL <1 mg/mL
S7029 AZD2461 <1 mg/mL 79 mg/mL 31 mg/mL
S7300 PJ34 HCl 66 mg/mL 66 mg/mL <1 mg/mL
S7438 ME0328 <1 mg/mL 64 mg/mL <1 mg/mL
S2197 A-966492 <1 mg/mL 64 mg/mL <1 mg/mL
S2886 PJ34 <1 mg/mL 28 mg/mL <1 mg/mL
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