NVP-TNKS656(TNKS-656) is a highly potent, selective, and orally active TNKS2 inhibitor with IC50 of 6 nM; > 300 fold selectivity against PARP1 and PARP2.

MK-4827 is an inhibitor of poly (ADP-ribose) polymerase (PARP) with potential antineoplastic activity.

ME0328 is an inhibitor of PARP3 (IC50 = 0.89 µM), which is a regulator of DNA repair and mitotic progression.

JW 55 is an inhibitor of the PARP domain of tankyrase 1 and 2 (TNKS1/2). JW55 decreased auto-PARsylation of TNKS1/2 in vitro with IC50 values of 1.9 uM and 830 nM respectively.

GeA-69(GeA69) is a potent, selective, allosteric, cell-active PARP14 macrodomain 2 (MD2) inhibitor with Kd of 0.86 uM in ITC assays.

G007-LK is a potent, "rule of 5" compliant and a metabolically stable TNKS1/2 inhibitor.

E7449 is an orally bioavailable, potent, small molecule inhibitor of PARP1 and PARP2; enhances the efficacy of radiotherapy and chemotherapy and has potent single agent anticancer activity in BRCA-deficient tumors.

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

AZ6102 is a potent TNKS1/2 inhibitor that has 100-fold selectivity against other PARP family enzymes and shows 5 nM Wnt pathway inhibition in DLD-1 cells.

AG14361 is a potent inhibitor of PARP1 with Ki of <5 nM. It is at least 1000-fold more potent than the benzamides.

Picolinamide (2-Picolinamide) is an inhibitor of Poly(ADP-ribose) synthetase of nuclei from rat pancreatic islet cells.

TIQ-A is a potent TNKS (poly-ART, PARP) inhibitor, with an IC50 of 24 nM for TNKS2. TIQ-A is a potential anti-ischemic agent.

Basroparib is a potent poly (ADP-ribose) polymerase (PARP) inhibitor, with antineoplastic activity.

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.

DPQ is a potent PARP-1 inhibitor. DPQ can reduce the N-methyl-d-aspartate (NMDA)-induced PARP activation, restoring ATP to near control levels and significantly attenuating neuronal injury in the severe NMDA exposure model. DPQ can be used for researching neuroprotection.

MN-64 is a inhibitor of tankyrases, showed 6 nM potency against tankyrase 1, isoenzyme selectivity, and Wnt signaling inhibition.

NMS-P118 is a potent, orally available, and highly selective PARP-1 inhibitor with excellent ADME and pharmacokinetic profiles and high efficacy in vivo.

NU 1025 is an inhibitor of poly(ADP-ribose) polymerases (PARP) (IC50 = 400 nM).

4-Aminonaphthalimide is a potent PARP inhibitor and potentiates the cytotoxicity of γ-radiation in cancer cells.

Rucaparib (AG-014699, PF-01367338) is an inhibitor of PARP with Ki of 1.4 nM with binding affinity to nine PARP domains. Phase 1/2.

Rucaparib inactivates PARP activity in cells with homologous recombination DNA repair pathway mutations at LC50 values ranging from 1.3-5.5 μM.

Veliparib (ABT-888) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM, respectively.

RP12146 (RP12146) is a novel, selective, and potent small molecule inhibitor of PARP1/2 with IC50 of 0.6/0.5 nM, with several fold selectivity over other isoforms.RP12146 inhibited cell growth in both BRCA mutant and non-BRCA mutant cancer cell lines with a GI50 range of 0.043 to 19.83 µM in a dose dependent manner.RP12146 demonstrated anti-tumor activities in both tumor size and tumor weight in OVCAR3 xenograft model.

PARPYnD is the first cell-active photoaffinity probe (AfBP) for PARP protein class, based on triple PARP1/2/6 inhibitor AZ9482.PARPYnD is a robust tool for profiling PARP1/2 and is used to profile clinical PARP inhibitor olaparib, identifying several novel off-target proteins.PARPYnD can enrich recombinant PARP6 spiked into cellular lysates and inhibits PARP6 in cell-free assays, it does not label PARP6 in intact cells.PARPYnD inhibits PARP1/2/6 with IC50 of 38/6/230 nM, respectively.

AMXI-5001 Hcl (AMXI 5001) is a novel, highly potent, orally active dual PARP1/2 (IC50 5/0.05 nM) and microtubule polymerization inhibitor, inhibits intracellular PAR formation with IC50 of 7 nM.AMXI-5001 binds to the catalytic domain of human PARP1 and is a weak tankyrase inhibitor (800-fold lower than IC50 towards either PARP1 or PARP2 enzymes).AMXI-5001 inhibited tubulin polymerization in a dose-dependent manner.AMXI-5001 exhibited selective antitumor cytotoxicity across a wide variety of human cancer cells with much lower IC50s than existing clinical PARP1/2 inhibitors.AMXI-5001 is highly active in both BRCA mutated and wild type cancers.AMXI-5001 elicited a remarkable In vivo preclinical anti-tumor activity in a BRCA mutated TNBC model induced complete regression of established tumors, including exceedingly large tumors, demonstrated superior anti-tumor effects compared to either single agent (PARP or microtubule) inhibitor or combination with both agents.

PARP-1-IN-1 is a high selective and orally active PARP-1 inhibitor (IC50=0.96 nM). PARP-1-IN-1 has well tolerance and remarkable single dose activity in the MDA-MB-436 xenotransplantation model.

AZ3391 is a potent inhibitor of PARP. AZ3391 is a quinoxaline derivative. PARP family of enzymes play an important role in a number of cellular processes, such as replication, recombination, chromatin remodeling, and DNA damage repair. AZ3391 has the potential for the research of diseases and conditions occurring in tissues in the central nervous system, such as the brain and spinal cord (extracted from patent WO2021260092A1, compound 23).

NCT-TFP is PARP probe used to identifying Poly(ADP-ribose) polymerases (PARP) inhibitors (extracted from patent US20190331688A1).

AZ9482, a potent and selective PARP inhibitor featuring an amide linkage to a 2-piperazinyl-3-cyano-pyridine.

OM-153 is a potent tankyrase inhibitor with IC50s of 13 and 2 nM for tankyrase 1 and tankyrase 2, respectively. OM-153 shows inhibition of WNT/β-catenin signaling and proliferation in COLO 320DM.