9-Bromo-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one NSC-664704 Yellow-brown solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A potent cell-permeable inhibitor of glycogen synthase kinase-3b (IC50 = 230 nM), Lck (IC50 = 470 nM), and cyclin-dependent kinases (Cdks). Inhibits Cdk1/cyclin B (IC50 = 400 nM), Cdk2/cyclin A (IC50 = 680 nM), Cdk2/cyclin E (IC50 = 7.5 µM), and Cdk5/p25 (IC50 = 850 nM). Also inhibits other kinases such as c-Src (IC50 = 15 µM), casein kinase II (IC50 = 20 µM), ERK1 (IC50 = 20 µM), and ERK2 (IC50 = 9 µM). Inhibition is competitive with respect to ATP binding. Purity: ≥95% by HPLC. CAS 142273-20-9. Ref.: Bain, J., et al. 2003. Biochem. J. 371, 199. Buolamwini, J.K. 2000. Curr. Pharm. Des. 6, 379. Schultz, C., et al. 1999. J. Med. Chem. 42, 2909. Zaharevitz, D.W., et al. 1999. Cancer Res. 59, 2566. |