Catalog No.: PC-49499Not For Human Use, Lab Use Only.
G-631 is a potent and selective TNKS1/2 inhibitor with IC50 of 7 nM in biochemical assays of tankyrase auto-PARsylation activity, and cellular potency of 8 nM (HEK293).
G-631 is a potent and selective TNKS1/2 inhibitor with IC50 of 7 nM in biochemical assays of tankyrase auto-PARsylation activity, and cellular potency of 8 nM (HEK293).
G-631 is selective against other PARP family members, with IC50 on PARP1 > 10,000 nM.
G-631 is also highly selective against kinases and secondary pharmacology targets, shows no >50 % inhibition against 220 kinases at 1 uM.
G-631 caused dose-dependent intestinal toxicity in mice while showing modest antitumor effects in a SW403 xenograft model at 100 mg/kg daily oral dosing.
