Cdk1/2 Inhibitor III is a cell-permeable triazolo-diamine compound that displays anti-proliferative properties in various human cancer cells (IC50 = 20 nM, 35 nM and 92 nM in HCT-116, HeLa, and A375 cells, respectively). Cdk1/2 Inhibitor III acts as a highly potent, ATP-competitive inhibitor of Cdk1/cyclin B and Cdk2/cyclin A (IC50 = 600 pM and 500 pM, respectively) with selectivity over VEGF-R2 (IC50 = 32 nM), GSK-3b (IC50 = 140 nM), and a panel of eight other kinases (IC50 ≥ 1 µM)
1. Lin, Ronghui., et al., 2005. 1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities. Journal of medicinal chemistry. 48(13): 4208-11. PMID: 15974571
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