PARP1 Selective Inhibitors

Catalog No. Product Name Information Selective / Pan IC50 / Ki
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.

Selective PARP1, IC50: 0.57 nM
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.

Selective PARP1, Ki: 1.4 nM
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.

Selective PARP1, Ki: 1.4 nM
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.

Selective PARP1, Ki: <5 nM
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).

Selective PARP1, Kd: 0.009 μM
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.

Selective hPARP-1, pKi: 7.05; hPARP-1, pIC50: 7.35
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.

Selective PARP1, IC50: 9.5 μM; PARP1, IC50: 9.5 μM; PARP1, IC50: 9.5 μM; PARP1, IC50: 9.5 μM; PARP1, IC50: 9.5 μM; PARP1, IC50: 9.5 μM; PARP1, IC50: 9.5 μM; PARP1, IC50: 9.5 μM; PARP1, IC50: 9.5 μM
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.

Selective
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.

Pan PARP1, IC50: 0.83 nM
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.

Pan PARP1, IC50: 1 nM
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
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.

Pan PARP1, IC50: 3.8 nM
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.

Pan PARP1, IC50: 3.8 nM
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.

Pan PARP1, IC50: 5 nM
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.

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