PARP

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PARP Inhibitors (14)

water-soluble

Cat.No. Product Name Information Product Citations Customer Reviews
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 1/2.
  • 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 1/2.
  • Cancer Res, 2011, 71(14):4944-54
  • Nucleic Acids Res, 2013, 41(7):4080-92
  • Clin Cancer Res, 2012, 18(21):5878-87
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 1/2.
  • Nature, 2011, 470(7334):419-23
  • Clin Cancer Res, 2013, 19(18):5003-15
  • Int J Radiat Oncol Biol Phys, 2013, 88(2):385-94
S1087 Iniparib (BSI-201) BSI-201 (Iniparib, SAR240550) is a PARP1 inhibitor with demonstrated effectiveness in triple-negative breast cancer (TNBC). Phase 3.
  • Nat Methods , 2013, 10(10):981-4
  • Neuroscience, 2010, 171(4):1256-64
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.
  • Nat Methods , 2013, 10(10):981-4
S8038 UPF 1069 UPF 1069 is a selective PARP2 inhibitor with IC50 of 0.3 μM. It is ~27-fold selective against PARP1.
S7048 BMN 673 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 1.
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.
S7438 ME0328 ME0328 is a potent and selective PARP inhibitor with IC50 of 0.89 μM for PARP3, about 7-fold selectivity over PARP1.
S2886 PJ34 PJ-34 is a PARP inhibitor with EC50 of 20 nM and is equally potent to PARP1/2.
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.
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
S2741 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. Phase 3.
  • Oncogene, 2013, 32(47):5377-87