PHA-767491, also known as CAY10572, is a potent, ATP-competitive dual cdc7/cdk9 inhibitor (IC50 values are 10 and 34 nM respectively) that prevents initiation of DNA replication. PHA-767491 Suppresses Hepatocarcinoma Synergistically with 5-Fluorouracil. PHA-767491 in combination with 5-FU exhibited much stronger cytotoxicity and induced significant apoptosis manifested by remarkably increased caspase 3 activation and poly(ADP-Ribose) polymerase fragmentation in HCC cells. PHA-767491 directly counteracted the 5-FU-induced phosphorylation of Chk1, a substrate of Cdc7; and decreased the expression of the anti-apoptotic protein myeloid leukemia cell 1, a downstream target of Cdk9.
Related Prodcuts:
GW9662; TAS-103; TAS-103 dihydrochloride; BRD73954; PU-WS13; L189; SCR7; Ispinesib; Dasabuvir; Ellipticine; Rucaparib; Rucaparib phosphate; Rucaparib camsylate; CB-5083; Maytansinoid DM 1; Mirin; Dasabuvir sodium; Dexrazoxane Hydrochloride; Nedaplatin