PARP

Sigaling Pathway Map

Research Area

Inhibitory Selectivity

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Notes:
2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Isoform-specific Inhibitors

Catalog No. Information Product Use Citations Product Validations
S1060

Olaparib (AZD2281, Ku-0059436)

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. Phase 3.

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 in cell-free assays, respectively. It is inactive to SIRT2. Phase 3.

S1098

Rucaparib (AG-014699,PF-01367338)

Rucaparib (AG-014699, PF-01367338) 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. Phase 3.

S1087

Iniparib (BSI-201)

Iniparib (BSI-201) is a PARP1 inhibitor with demonstrated effectiveness in triple-negative breast cancer (TNBC). Phase 3.

S7048

Talazoparib (BMN 673)

Talazoparib (BMN 673) is a novel PARP inhibitor with IC50 of 0.58 nM 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.

S8370New

BGP-15

BGP-15, is a nicotinic amidoxime derivative with PARP inhibitory activity. It has been demonstrated that BGP-15 protects against ischemia-reperfusion injury.

S2741New

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.

S4710New

Picolinamide

Picolinamide is found to be a strong inhibitor of poly (ADP-ribose) synthetase of nuclei from rat pancreatic islet cells.

S4715New

Benzamide

Benzamide, an inhibitor of poly(ADP-ribose) polymerase, is a derivative of benzoic acid.

S7625New

MK-4827(Niraparib) tosylate

MK-4827(Niraparib) tosylate is a selective inhibitor of PARP1/PARP2 with IC50 of 3.8 nM/2.1 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.

S1132

INO-1001 (3-Aminobenzamide)

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.

S2886

PJ34

PJ-34 is a PARP inhibitor with EC50 of 20 nM and is equally potent to PARP1/2.

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.

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.

S7438

ME0328

ME0328 is a potent and selective PARP inhibitor with IC50 of 0.89 μM for PARP3, about 7-fold selectivity over PARP1.

S7730

NU1025

NU1025 is a potent PARP inhibitor with IC50 of 400 nM.

S7239

G007-LK

G007-LK is a potent and selective tankyrase inhibitor with IC50 of 46 nM and 25 nM for TNKS1/2, respectively.

Catalog No. Information Product Use Citations Product Validations
S1060

Olaparib (AZD2281, Ku-0059436)

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. Phase 3.

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 in cell-free assays, respectively. It is inactive to SIRT2. Phase 3.

S1098

Rucaparib (AG-014699,PF-01367338)

Rucaparib (AG-014699, PF-01367338) 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. Phase 3.

S1087

Iniparib (BSI-201)

Iniparib (BSI-201) is a PARP1 inhibitor with demonstrated effectiveness in triple-negative breast cancer (TNBC). Phase 3.

S7048

Talazoparib (BMN 673)

Talazoparib (BMN 673) is a novel PARP inhibitor with IC50 of 0.58 nM 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.

S8370New

BGP-15

BGP-15, is a nicotinic amidoxime derivative with PARP inhibitory activity. It has been demonstrated that BGP-15 protects against ischemia-reperfusion injury.

S2741New

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.

S4710New

Picolinamide

Picolinamide is found to be a strong inhibitor of poly (ADP-ribose) synthetase of nuclei from rat pancreatic islet cells.

S4715New

Benzamide

Benzamide, an inhibitor of poly(ADP-ribose) polymerase, is a derivative of benzoic acid.

S7625New

MK-4827(Niraparib) tosylate

MK-4827(Niraparib) tosylate is a selective inhibitor of PARP1/PARP2 with IC50 of 3.8 nM/2.1 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.

S1132

INO-1001 (3-Aminobenzamide)

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.

S2886

PJ34

PJ-34 is a PARP inhibitor with EC50 of 20 nM and is equally potent to PARP1/2.

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.

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.

S7438

ME0328

ME0328 is a potent and selective PARP inhibitor with IC50 of 0.89 μM for PARP3, about 7-fold selectivity over PARP1.

S7730

NU1025

NU1025 is a potent PARP inhibitor with IC50 of 400 nM.

S7239

G007-LK

G007-LK is a potent and selective tankyrase inhibitor with IC50 of 46 nM and 25 nM for TNKS1/2, respectively.

Tags: PARP inhibition | PARP cancer | PARP inhibitor cancer | PARP signaling | PARP activity | PARP assay | PARP activity | PARP inhibitor trial | PARP activation | PARP inhibitors clinical trials | FDA approval PARP inhibitor | PARP inhibitor drugs | PARP phosphorylation | PARP inhibitor review