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). Acts as a highly potent, reversible, 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-3β (IC50 = 140 nM), and a panel of eight other kinases (IC50 ≥ 1 µM).
1 mg in Plastic ampoule
Packaged under inert gas
Cell permeable: yes
Target IC50: 20 nM, 35 nM and 92 nM for anti-proliferative properties in HCT-116, HeLa, and A375 cells, respectively; 600 pM and 500 pM, against Cdk1/cyclin B and Cdk2/cyclin A, respectively
Cdk1/cyclin B, Cdk2/cyclin A
Product competes with ATP.
Toxicity: Harmful (C)
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Lin, R., et al. 2005.J. Med. Chem.48, 4208.
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany