TFLLR-NH2, derived from the protease-activated receptor-1 (PAR1), is a selective PAR1 agonist with an EC50 of 1.9 μM.
PJ34 is a novel and potential PARP inhibitor with potential anticancer activity. PJ34 has a high affinity for PARP-1 (IC(50) = 20 nM) .
Olaparib, also known as AZD-2281 or KU-59436, is a small molecule inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase (PARP) with potential chemosensiti...
BSI-201 is a small-molecule prodrug inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase-1 (PARP-1) with potential chemosensitizing, radiosensitizing and...
Rucaparib Phosphate is a selective PARP inhibitor that suppresses the PARP1-mediated DNA repair via binding to PARP1 (Ki = <5 nM). It can be used to sensitize c...
XMD16-5is a novel non-receptor tyrosine kinase TNK2 inhibitor (IC50= 16 nM and 77 nM for D163E and R806Q mutant TNK2, respectively)
A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively
BMN-673 is an orally bioavailable inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase (PARP) with potential antineoplastic activity. PARP inhibitor BMN-...
MK-4827 tosylate is a selective inhibitor of PARP1/PARP2 with IC50 of 3.8 nM/2.1 nM. It has a great activity in cancer cells with mutant BRCA-1 and BRCA-2, >330...
NVP-TNKS656, also known as TNKS656, is a potent and orally active Tankyrase Inhibitor. With an enthalpy-driven thermodynamic signature of binding, highly favor...
Niraparib is an inhibitor of PARP, which was approved by FDA for the maintenance treatment of adult patients with recurrent epithelial ovarian, fallopian tube o...
UPF 1069 is a selective PARP2 inhibitor with IC50 of 0.3 μM. It is ~27-fold selective against PARP1.PARP activity is evaluated by utilizing commercially availab...
AZD2461 is a novel and potent PARP inhibitor with lower affinity to P-glycoprotein. AZD2641 is currently in Phase I clinical study. The study is being conducted...
A novel small-molecule-like BRCA1 inhibitor (IC50= 0.53 μM) (Ki= 0.71 μM)
G007-LK is a potent, "rule of 5" compliant and a metabolically stable TNKS1/2 inhibitor. G007-LK displayed high selectivity toward tankyrases 1 and 2 with bioch...
AG14361 is a PARP-1 inhibitor with Ki < 5 nmol/L. AG14361 is at least 1000-fold more potent than the benzamides. The IC50 for AG14361 is 29 nM in permeabilized ...
AZ0108 is an orally bioavailable, PARP1,2,6 inhibitor that causes a multi-polar spindle phenotype at double digit nM concentrations. AZ0108 has been utilized as...
Veliparib (ABT-888) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM, respectively. In HCT-116 and HT-29 cell lines, the ability of ABT-888...