PARP Inhibitor

EXQ-2d is the inhibitor for tankyrase and inhibits TNKS1 and TNKS2 with an IC₅₀ of 48.8 nM and 13.8 nM (pIC₅₀=7.31 and 7.86). EXQ-2d inhibits WNT/β-catenin signaling pathway with IC₅₀ of 515 nM. EXQ-2d exhibits anti-proliferative activity in cancer cells COLO 320DM and RKO with GI₅₀ of 4.9 μM and 77 μM.

5-AIQ (5-Aminoisoquinolin-1-one) is a PARP-1 inhibitor. 5-AIQ is an important functional group in various drugs. 5-AIQ reduces the tissue injury associated with ischemia-reperfusion of the liver, it can be used for the research of the research conditions associated with ischemia-reperfusion of the liver.

Tubulin/PARP-IN-1 (compound 14) is a dual PARP-tubulin inhibitor with activity against endometrial cancer. Tubulin/PARP-IN-1 inhibits PARP and tubulin with IC₅₀s of 74 nM (PARP1), 109 nM (PARP2), and 1.4 μM (Microtubule/Tubulin), respectively. Tubulin/PARP-IN-1 can induce apoptosis and autophagy and cause cell cycle arrest in the G2/M phase.

BRCA1-IN-1 is a novel small-molecule-like BRCA1 inhibitor with IC₅₀ and K_i of 0.53 μM and 0.71 μM, respecrively.

WD2000-012547 is a selective poly(ADP-ribose)-polymerase (PARP-1) inhibitor with a pK_i of 8.221.