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PARP1-selektive Inhibitors

  • PARP1
  • PARP2
  • PARP3
  • Tankyrase-1
Kat.-Nr. Produktname Informationen Selektiv / Pan IC50 / Ki
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. Selective PARP1, Ki: <5 nM
S1087 Iniparib (BSI-201) Iniparib (BSI-201) is a PARP1 inhibitor with demonstrated effectiveness in triple-negative breast cancer (TNBC). Phase 3. Selective
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. Pan PARP1, EC50: 1 nM; PARP1, Ki: 1 nM
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. Pan PARP1, IC50: 5 nM
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. Pan PARP1, Ki: 5.2 nM
S7438 ME0328 ME0328 is a potent and selective PARP inhibitor with IC50 of 0.89 μM for PARP3, about 7-fold selectivity over PARP1. Pan PARP1, IC50: 6.3 μM
S8038 UPF 1069 UPF 1069 is a selective PARP2 inhibitor with IC50 of 0.3 μM. It is ~27-fold selective against PARP1. Pan PARP1, IC50: 8.0 μM