PARP
Signaling Pathway Map
Research Area
Inhibitory Selectivity
Isoform-specific Inhibitors
PARP Products
| 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. |
CYREN does not regulate repair of replication-induced DSBs. Representative images of chromosomes.
|
|
| 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. |
Chromosomal single-strand break repair rates in the indicated RPE-1 cell lines following treatment with 50 μM H2O2 in the presence/absence of 10 μM of the PARP inhibitor (PARPi) Veliparib, as measured by alkaline comet assay. Data are the mean tail moment of 100 cells per sample per experiment and are the average (-/+SEM) of three independent experiments. Two-way ANOVA analysis between relevant genotypes is presented (ns= not significant, **= p<0.01, ***= p<0.001).
|
|
| S1098 |
Rucaparib (AG-014699,PF-01367338) phosphateRucaparib (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. |
Representative images for RAD51 and γH2AX foci formation, surrogate DSB markers, in stable shK-H or shSCR 231 cells after rucaparib or vehicle (0.01% DMSO) treatment for 24 hours. DAPI-stained cell nuclei. Scale bars, 10 μm.
|
|
| S1087 |
Iniparib (BSI-201)Iniparib (BSI-201) is a PARP1 inhibitor with demonstrated effectiveness in triple-negative breast cancer (TNBC). Phase 3. |
Immunoblot analysis of
PARylation after treatment with various PARP
inhibitors.The asterisk indicates
a nonspecific band.
|
|
| S7048 |
Talazoparib (BMN 673)Talazoparib (BMN 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. |
DNA damage persists on withdrawal of PARPi in RNASEH2AKO cells. Wild-type and RNASEH2AKO HeLa cells were treated with talazoparib and released into fresh medium for the indicated times before being processed for γ-H2AX immunofluorescence and propidium iodide (PI) staining. The γ-H2AX immunofluorescence (pseudocolor plots) and cell cycle (histograms) FACS profiles shown are representative of three biologically independent experiments.
|
|
| S9360New |
4-Hydroxyquinazoline4-Hydroxyquinazoline is a PARP inhibitor with a high potency for PARP-1 and no effects on enzymes other than PARP. |
||
| S8592New |
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. |
||
| S2178 |
AG-14361AG14361 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. |
Immunoblot analysis of PARylation after treatment with various PARP inhibitors.The asterisk indicates a nonspecific band. |
|
| 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. |
Propofol inhibited the increase of PARP-1׳s expression and activity. Mice (n=6) were injected intraperitoneally with propofol, INO-1001 (a PARP-1 inhibitor) or equal volume of normal saline (NS), and then were trained with objects. Naïve animals were injected with normal saline and trained without objects (the same as habituation). 30 min after acquisition trial, the hippocampal tissues were harvested for determining PARP-1 (A and B) and PAR (C and D) expression by Western blot. Histogram represented the relative level normalized to naïve. *P<0.05, **P<0.01.
|
|
| S2197 |
A-966492A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively. |
Immunoblot analysis of PARylation after treatment with various PARP inhibitors.The asterisk indicates a nonspecific band. |
|
| S7300 |
PJ34 HClPJ34 HCl is the hydrochloride salt of PJ34, which is a PARP inhibitor with EC50 of 20 nM and is equally potent to PARP1/2. |
LN229 GBM cells were treated with PJ34 (20 µM), TRAIL (200 ng/ml) or the combination of both and analyzed for the expression of DR5, caspase-9 (CP9) and cleaved caspase-3 (cCP3). The vertical line on the immunoblot indicates that the first and second samples were noncontiguous, but run on the same gel simultaneously with the other samples.
|
|
| 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. Phase 3. |
Western Blot data testing protein expression after treatment with Olaparib, Niraparib, and Talazoparib on Brca1-deficient cell line in W780 cells.
|
|
| S8038 |
UPF 1069UPF 1069 is a selective PARP2 inhibitor with IC50 of 0.3 μM. It is ~27-fold selective against PARP1. |
||
| S7029 |
AZD2461AZD2461 is a novel PARP inhibitor with low affinity for Pgp than Olaparib. Phase 1. |
(b) Hoechst-positive cell quantification of caspase and PARP inhibitors and their effect on ARPE-19 cells undergoing UOS in the presence and absence of NPD1 (lower panel). Bars represent data averages of three repeats (technical replicas) of three independent experiments (biological replicas). *P<0.05
|
|
| S7438 |
ME0328ME0328 is a potent and selective PARP inhibitor with IC50 of 0.89 μM for PARP3, about 7-fold selectivity over PARP1. |
Colony survival assay in wild-type A549 cells treated with vehicle, 3.0 μM ME0328 or 500 nM KU58948 and pyridostatin.
|
|
| S8370 |
BGP-15 2HClBGP-15, is a nicotinic amidoxime derivative with PARP inhibitory activity. It has been demonstrated that BGP-15 protects against ischemia-reperfusion injury. |
||
| S7625 |
Niraparib (MK-4827) tosylateNiraparib (MK-4827) tosylate is a selective inhibitor of PARP1/PARP2 with IC50 of 3.8 nM/2.1 nM. |
Berberine activates PARP1 in ovarian cancer cells. PAR synthesis is detected by immunofluorescence staining in A2780 and HO8910 treated with different concentration of berberine alone or in combination with niraparib (10 μM) for 48 h. Top: representative examples of immunofluorescence staining of PAR. Scale bar, 20 μm. Bottom: quantification of PAR level in A2780 and HO8910. Immunofluorescence intensities were quantified by ImageJ. *P<0.05, **P<0.01
|
|
| S7730 |
NU1025NU1025 is a potent PARP inhibitor with IC50 of 400 nM. |
||
| S7239 |
G007-LKG007-LK is a potent and selective tankyrase inhibitor with IC50 of 46 nM and 25 nM for TNKS1/2, respectively. |
Western blot analysis of SH3BP2 in WT BMMs after culture for 2 days in the presence of IWR-1 (2 μM), G007-LK (0.1 μM), or ICG001 (2 μM). |
|
| S7238 |
NVP-TNKS656NVP-TNKS656 is a highly potent, selective, and orally active tankyrase inhibitor with IC50 of 6 nM for TNKS2, > 300-fold selectivity against PARP1 and PARP2. |
||
| S8419 |
E7449E7449 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. |
||
| S8363 |
NMS-P118NMS-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). |
||
| S4715 |
BenzamideBenzamide, a derivative of benzoic acid, is an inhibitor of poly(ADP-ribose) polymerase with an IC50 of 3.3 μM. |
||
| S4710 |
PicolinamidePicolinamide is found to be a strong inhibitor of poly (ADP-ribose) synthetase of nuclei from rat pancreatic islet cells. |
| 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. |
CYREN does not regulate repair of replication-induced DSBs. Representative images of chromosomes.
|
|
| 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. |
Chromosomal single-strand break repair rates in the indicated RPE-1 cell lines following treatment with 50 μM H2O2 in the presence/absence of 10 μM of the PARP inhibitor (PARPi) Veliparib, as measured by alkaline comet assay. Data are the mean tail moment of 100 cells per sample per experiment and are the average (-/+SEM) of three independent experiments. Two-way ANOVA analysis between relevant genotypes is presented (ns= not significant, **= p<0.01, ***= p<0.001).
|
|
| S1098 |
Rucaparib (AG-014699,PF-01367338) phosphateRucaparib (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. |
Representative images for RAD51 and γH2AX foci formation, surrogate DSB markers, in stable shK-H or shSCR 231 cells after rucaparib or vehicle (0.01% DMSO) treatment for 24 hours. DAPI-stained cell nuclei. Scale bars, 10 μm.
|
|
| S1087 |
Iniparib (BSI-201)Iniparib (BSI-201) is a PARP1 inhibitor with demonstrated effectiveness in triple-negative breast cancer (TNBC). Phase 3. |
Immunoblot analysis of
PARylation after treatment with various PARP
inhibitors.The asterisk indicates
a nonspecific band.
|
|
| S7048 |
Talazoparib (BMN 673)Talazoparib (BMN 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. |
DNA damage persists on withdrawal of PARPi in RNASEH2AKO cells. Wild-type and RNASEH2AKO HeLa cells were treated with talazoparib and released into fresh medium for the indicated times before being processed for γ-H2AX immunofluorescence and propidium iodide (PI) staining. The γ-H2AX immunofluorescence (pseudocolor plots) and cell cycle (histograms) FACS profiles shown are representative of three biologically independent experiments.
|
|
| S9360New |
4-Hydroxyquinazoline4-Hydroxyquinazoline is a PARP inhibitor with a high potency for PARP-1 and no effects on enzymes other than PARP. |
||
| S8592New |
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. |
||
| S2178 |
AG-14361AG14361 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. |
Immunoblot analysis of PARylation after treatment with various PARP inhibitors.The asterisk indicates a nonspecific band. |
|
| 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. |
Propofol inhibited the increase of PARP-1׳s expression and activity. Mice (n=6) were injected intraperitoneally with propofol, INO-1001 (a PARP-1 inhibitor) or equal volume of normal saline (NS), and then were trained with objects. Naïve animals were injected with normal saline and trained without objects (the same as habituation). 30 min after acquisition trial, the hippocampal tissues were harvested for determining PARP-1 (A and B) and PAR (C and D) expression by Western blot. Histogram represented the relative level normalized to naïve. *P<0.05, **P<0.01.
|
|
| S2197 |
A-966492A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively. |
Immunoblot analysis of PARylation after treatment with various PARP inhibitors.The asterisk indicates a nonspecific band. |
|
| S7300 |
PJ34 HClPJ34 HCl is the hydrochloride salt of PJ34, which is a PARP inhibitor with EC50 of 20 nM and is equally potent to PARP1/2. |
LN229 GBM cells were treated with PJ34 (20 µM), TRAIL (200 ng/ml) or the combination of both and analyzed for the expression of DR5, caspase-9 (CP9) and cleaved caspase-3 (cCP3). The vertical line on the immunoblot indicates that the first and second samples were noncontiguous, but run on the same gel simultaneously with the other samples.
|
|
| 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. Phase 3. |
Western Blot data testing protein expression after treatment with Olaparib, Niraparib, and Talazoparib on Brca1-deficient cell line in W780 cells.
|
|
| S8038 |
UPF 1069UPF 1069 is a selective PARP2 inhibitor with IC50 of 0.3 μM. It is ~27-fold selective against PARP1. |
||
| S7029 |
AZD2461AZD2461 is a novel PARP inhibitor with low affinity for Pgp than Olaparib. Phase 1. |
(b) Hoechst-positive cell quantification of caspase and PARP inhibitors and their effect on ARPE-19 cells undergoing UOS in the presence and absence of NPD1 (lower panel). Bars represent data averages of three repeats (technical replicas) of three independent experiments (biological replicas). *P<0.05
|
|
| S7438 |
ME0328ME0328 is a potent and selective PARP inhibitor with IC50 of 0.89 μM for PARP3, about 7-fold selectivity over PARP1. |
Colony survival assay in wild-type A549 cells treated with vehicle, 3.0 μM ME0328 or 500 nM KU58948 and pyridostatin.
|
|
| S8370 |
BGP-15 2HClBGP-15, is a nicotinic amidoxime derivative with PARP inhibitory activity. It has been demonstrated that BGP-15 protects against ischemia-reperfusion injury. |
||
| S7625 |
Niraparib (MK-4827) tosylateNiraparib (MK-4827) tosylate is a selective inhibitor of PARP1/PARP2 with IC50 of 3.8 nM/2.1 nM. |
Berberine activates PARP1 in ovarian cancer cells. PAR synthesis is detected by immunofluorescence staining in A2780 and HO8910 treated with different concentration of berberine alone or in combination with niraparib (10 μM) for 48 h. Top: representative examples of immunofluorescence staining of PAR. Scale bar, 20 μm. Bottom: quantification of PAR level in A2780 and HO8910. Immunofluorescence intensities were quantified by ImageJ. *P<0.05, **P<0.01
|
|
| S7730 |
NU1025NU1025 is a potent PARP inhibitor with IC50 of 400 nM. |
||
| S7239 |
G007-LKG007-LK is a potent and selective tankyrase inhibitor with IC50 of 46 nM and 25 nM for TNKS1/2, respectively. |
Western blot analysis of SH3BP2 in WT BMMs after culture for 2 days in the presence of IWR-1 (2 μM), G007-LK (0.1 μM), or ICG001 (2 μM). |
|
| S7238 |
NVP-TNKS656NVP-TNKS656 is a highly potent, selective, and orally active tankyrase inhibitor with IC50 of 6 nM for TNKS2, > 300-fold selectivity against PARP1 and PARP2. |
||
| S8419 |
E7449E7449 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. |
||
| S8363 |
NMS-P118NMS-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). |
||
| S4715 |
BenzamideBenzamide, a derivative of benzoic acid, is an inhibitor of poly(ADP-ribose) polymerase with an IC50 of 3.3 μM. |
||
| S4710 |
PicolinamidePicolinamide is found to be a strong inhibitor of poly (ADP-ribose) synthetase of nuclei from rat pancreatic islet cells. |
