CDK9/10/GSK3β-IN-1

CDK9/10/GSK3β-IN-1 (compound 13c) is a kinase inhibitor (Flavopiridol (HY-10005) analogue) that effectively inhibits HsGSK3β (IC50=59 nM), HsCDK9/CyclinT (IC50=64 nM), HsCDK5/p25 (IC50=1.093 µM) and HsCDK2/CyclinA (IC50=1.725 µM). CDK9/10/GSK3β-IN-1 has anti-cancer cellular activity comparable to or higher than that of Flavopiridol. CDK9/10/GSK3β-IN-1 shows high anti-proliferative activity in vitro against up to seven cancer cell lines[1].

Research Areas >> Cancer

Signaling Pathways >> Others >> Others

IC50: 59 nM (HsGSK3β), 64 nM (HsCDK9/CyclinT), 1.093 µM (HsCDK5/p25), 1.725 µM (HsCDK2/CyclinA)[1].

CDK9/10/GSK3β-IN-1 (series concentration,72 h) exhibits high antiproliferative activity to SKOV3, NCIeN87, SKBR3, PC3, MiaPaCa-2, HCT116, K562 cells[1]. Cell Proliferation Assay[1] Cell Line: SKOV3, NCIeN87, SKBR3, PC3, MiaPaCa-2, HCT116, K562 cells Concentration: Series concentration Incubation Time: 72 h Result: Showed high antiproliferative activity, with an IC50 < 100 nM on 6 cancer cell lines, and up to six times more potent on the pancreatic cancer cells (MiaPaCa-2) than the reference compound, flavopiridol.

[1]. Ibrahim N, et al. Identification of a new series of flavopiridol-like structures as kinase inhibitors with high cytotoxic potency. Eur J Med Chem. 2020 Aug 1;199:112355.