| Cat.No. | Name | Information |
|---|---|---|
| M1732 | Talazoparib (BMN-673) | Talazoparib (BMN-673) is a highly potent, orally active PARP1/2 inhibitor.Talazoparib inhibits PARP1 and PARP2 enzyme activity with Kis of 1.2 nM and 0.87 nM, respectively. Talazoparib has antitumor activity. |
| M3932 | NVP-TNKS656 | NVP-TNKS656 is a highly potent, selective, and orally active TNKS2 inhibitor with IC50 of 6 nM; > 300 fold selectivity against PARP1 and PARP2. |
| M4931 | Rucaparib | 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. |
| M1664 | AZD2281 (Olaparib) | AZD 2281 (Olaparib, KU-0059436) is a potent PARP (poly ADP-ribose polymerase) inhibitorwith IC50 of 5 and 1 nM for PARP-1and PARP-2 respectively. Olaparib is an autophagy and mitophagy activator. |
| M2215 | Niraparib (MK-4827) | MK-4827 (Niraparib) is a selective PARP1/2 inhibitor with an IC50 value of 3.8 nM/2.1 nM that increases the formation of PARP-DNA complexes through inhibition of PARPase activity, leading to DNA damage, apoptosis, PARP-1-dependent cell death (parthanatos) and cell death. Strong effector activity when acting on cancer cells harboring mutant BRCA-1 and BRCA-2. It is more than 330-fold more selective than PARP3, V-PARP and Tank1. |
| M1785 | INO-1001 | INO-1001 is a novel poly(ADP-ribose) polymerase (PARP) inhibitor with an IC50 of 3 nM. |
| M13713 | RK-287107 | RK-287107 is a potent and specific tankyrase inhibitor with IC50s of 14.3 and 10.6 nM for tankyrase-1 and tankyrase-2, respectively. RK-287107 blocks colorectal cancer cell growth. |
| M41573 | Lerzeparib | Lerzeparib is an (ADP-ribose) polymerase (PARP) inhibitor, with antineoplastic activity. |
| M41572 | PARP-1-IN-3 | PARP-1-IN-3, a benzamide derivative, is a potent PARP-1 inhibitor with IC50 values of 0.25 nM and 2.34 nM for PARP-1 and PARP-2, respectively. |
| M41571 | Tankyrase-IN-5 | Tankyrase-IN-5, an analogue of MSC2504877, is a tankyrase TNKS1 and TNKS2 inhibitor with IC50s of 2.3 nM and 7.9 nM, respectively. |
| M41360 | PARP-1/2-IN-2 | PARP-1/2-IN-2-IN-1 is a PARP1/2/CDK12 inhibitor (IC50: 34, 30 and 285 nM respectively). |
| M30901 | CEP-9722 | CEP-9722, the proagent of CEP-8983, is a selective and orally active PARP-1 and PARP-2 inhibitor with IC50s of 20 nM and 6 nM, respectively. CEP-9722 has anticancer effects. |
| M30856 | COH34 | COH34 is a potent and specific poly(ADP-ribose) glycohydrolase (PARG) inhibitor with an IC50 of 0.37 nM. COH34 binds to the catalytic domain of PARG (Kd=0.547 μM), thereby prolonging PARylation at DNA lesions and trapping DNA repair factors. |
| M30842 | E7016 | E7016 (GPI 21016) is an orally available PARP inhibitor. E7016 can enhance tumor cell radiosensitivity in vitro and in vivo through the inhibition of DNA repair. E7016 acts as a potential anticancer agent. |
| M30744 | TC-E 5001 | TC-E 5001 is an inhibitor of Wnt pathway that inhibits tankyrase 1/2 (TNKS1/2) via novel adenosine pocket binding, with Kds of 79 nM and 28 nM, respectively. TC-E 5001 also inhibits Axin2 and STF, with IC50s of 0.709 μM and 0.215 μM, respectively. |
| M30210 | Verminoside | Verminoside is an iridoid isolated from Kigelia africana, exhibits anti-inflammatory and remarkable antioxidant activity with a radical-scavenging activity of 2.5 μg/mL. The genotoxicity of Verminoside on human lymphocytes is associated with elevated levels of PARP-1 and p53 proteins. |
| M29690 | SK-575-NEG | SK-575-NEG (compound 28), a methylation counterpart of SK-575, is synthesized by methylation of the amino group of piperidine-2,6-dione in SK-575 as an control compound. SK-575-NEG is strongly bound to PARP1, with an IC50 of 2.64 nM. SK-575-NEG was completely ineffective in inducing PARP1 degradation in MDA-MB-436 and Capan-1 cells at concentrations up to 1 μM. |
| M29689 | SK-575 | SK-575 is a highly potent and specific proteolysis-targeting chimera (PROTAC) degrader of PARP1, with an IC50 of 2.30 nM. SK-575 potently inhibits the growth of cancer cells bearing BRCA1/2 mutations. |
| M29595 | OM-1700 | OM-1700 is a potent tankyrase inhibitor with IC50s of 127 and 14 nM for tankyrase 1 and tankyrase 2, respectively. OM-1700 reduces cell growth in the colon cancer cell line COLO 320DM (GI50=650 nM). |
| M29181 | PARP14 inhibitor H10 | PARP14 inhibitor H10, compound H 10, is a selective inhibitor against PARP14 (IC50=490 nM), over other PARPs (≈24 fold over PARP1). PARP14 inhibitor H10 induces caspase-3/7-mediated cell apoptosis. |
| M29141 | Nesuparib | Nesuparib is a potent inhibitor of PARP. Nesuparib is useful for the research of neuropathic pain, neurodegenerative disease, and cardiovascular disease. |
| M29049 | PDD00017238 | PDD00017238 is a potent inhibitor of Poly(ADP-ribose) Glycohydrolase (PARG), with EC50 values of 40 nM and 55 nM in biochemical assay and cell POM, respectively. |
| M29041 | PDD00017272 | PDD00017272 (34f) is a potent inhibitor of Poly(ADP-ribose) Glycohydrolase (PARG), with EC50 of 4.8 nM and 9.2 nM in biochemical assay and cell POM, respectively. |
| M28932 | AZ9482 | AZ9482 is a triple PARP1/2/6 inhibitor, with IC50 values of 1 nM, 1 nM and 640 nM for PARP1, PARP2 and PARP6, respectively. |
| M28804 | Venadaparib | Venadaparib (IDX-1197) is a potent, selective and orally active PARP inhibitor with IC50s of 1.4 nM and 1.0 nM for PARP1 and PARP2, respectively. Venadaparib does not sensitive to PARP-5. Venadaparib prevents the repair of DNA single-strand breaks (SSB) and can be used for solid tumors research. |
| M28629 | TNKS-IN-2 | TNKS-IN-2 (compound 40) is a potent and selective tankyrase (TNKS) inhibitor with pIC50 values of 8.1, 7.0 for TANKS and Wnt, respectively. |
| M28495 | MSC2504877 | MSC2504877 (M2912) is a potent and orally active tankyrase inhibitor with IC50s of 0.0007, 0.0008, 0.54 µM for TNKS, TNKS2, PARP1, respectively. MSC2504877 increases the expression of AXIN2 and TNKS protein levels and decreases β-catenin levels. MSC2504877 shows anti-tumor activity. |
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