BYK204165 is a novel, potent and selective poly(ADP-ribose) polymerase (PARP)-1 inhibitor with pIC50of 5.38 and 7.35 for PARP-2 and PARP-1 respectively.
RK-287107 is a potent TNKS/TNKS2 inhibitor (IC50 = 14.4 nM) with >7000-fold selectivity against the PARP1 enzyme, which inhibits WNT-responsive TCF reporter activity and proliferation of human colorectal cancer cell line COLO-320DM.
JW 55 is a potent and selective small molecule inhibitor of β-catenin signaling pathway, it functions via inhibition of the PARP domain of tankyrase 1 and tankyrase 2 (TNKS1/2) which are regulators of the β-catenin destruction complex.
Pamiparib (also known as BGB-290; trade name in China: Baihuize) is a novel, potent and selective inhibitor of PARP1/2 approved in China for cancer treatment. It inhibits PARP1/2 with IC50 values of 0.83 and 0.11 nM, respectively in enzymatic assays. It kills tumor cells via the so-called synthetic lethality. Pamiparib diaplays high selectivity over other […]
BGP-15 HCl is a potent and novel PARP inhibitor that can protect against heart failure and atrial fibrillation in mice. BGP-15 (200 μM) prevents the imatinib mesylate-induced oxidative damages, attenuates the depletion of high-energy phosphates, alters the signaling effect of imatinib mesylate by preventing p38 MAP kinase and JNK activation, and induced the phosphorylation of […]
Stenoparib (formerly E-7449; 2X-121) is a novel, potent and orally bioavailable dual inhibitor of PARP1/2 [nuclear enzymes poly (ADP-ribose) polymerase] and tankyrases (TNKS1/2) with anticancer activity.
Iniparib (SAR-240550; BSI-201; NSC-746045; IND-71677) is a novel, potent, and irreversible inhibitor of PARP1 [poly(ADP-ribose) polymerase-1] with potential anticancer activity.
Niraparib tosylate hydrate (also known as MK-4827; MK4827; Zejula), the tosylate salt and hydrated form of niraparib, is a selective inhibitor of PARP1/2 (IC50 = 3.8 nM and 2.1nM) that was approved by FDA for the treatment of recurrent epithelial ovarian, fallopian tube, or primary peritoneal cancer.
AZD0156 is a novel, orally bioactive, potent and selective inhibitor of ATM (ataxia telangiectasia mutated) kinase with an IC50 of 0.58 nM and with potential chemo-/radio-sensitizing and antineoplastic activities.
PJ34 HCl, the hydrochloride of PJ34, is a novel, potent and selective inhibitor of poly(ADP-ribose) polymerase (PARP) with potential anticancer and neuro-protective activities.