Description General description A cell-permeable Staurosporine (Cat. No. 569397) derived anticancer agent that reversibly and ATP-competitively inhibits several protein kinases (IC50 = 29 nM, 34 nM, 30 nM, 590 nM and 530 nM for PKCα, PKCβ, PKCγ, PKCδ and PKCε; IC50 = 7 nM, 27 nM, 50 nM, 50 nM, 150 nM and 1.04 µM for Chk1, Cdc25C-associated protein kinase 1, Cdk1, PAK4, Cdk5/p25 and Chk2; IC50 = 33 nM, 50 nM, 95 nM, 500 nM, 500 nM and 1.0 µM for PDK1, lck, MAPKAP kinase-2, Akt, GSK-3β and PKA, respectively). At higher concentrations (> 15 µM), affects the activities of Src, PIM-1, CKII, DNA-PK, ErK1, ILK-1 and MAPKK1). Reported to suppress thymidylate synthase expression, induce apoptosis with caspase activation, and sensitize tumor cells to a range of DNA-damaging agents. Packaging 500 μg in Plastic ampoule Biochem/physiol Actions Cell permeable: yes IC50 = 29 nM, 34 nM, 30 nM, 590 nM, 530 nM, 7 nM, 27 nM, 50 nM, 50 nM, 150 nM, 1.04 µM, 33 nM, 50 nM, 95 nM, 500 nM, 500 nM and 1.0 µM, respectively for primary targets in the order listed Primary Target PKCα, PKCβ, PKCγ, PKCδ PKCε, Chk1, Cdc25C-associated protein kinase 1, Cdk1, PAK4, Cdk5/p25 and Chk2, PDK1, lck, MAPKAP kinase-2, Akt, GSK-3β and PKA Product competes with ATP. Reversible: yes Packaging Packaged under inert gas Warning Toxicity: Standard Handling (A) Reconstitution Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C. Other Notes Reinhardt, H.C., et al. 2007. Cancer Cell11, 175. Jiang, X., et al. 2004. Mol. Cancer Ther.3, 1221. Sato, S., et al. 2002. Oncogene21, 1727. Patel, V., et al. 2002. Clin. Cancer Res.8, 3549. Leclerc, S., et al. 2001. J. Biol. Chem.276, 251. Busby, E.C., et al. 2000. Cancer Res.60, 2108. Hsueh, C.T., et al. 1998. Clin. Cancer Res.4, 2201. Akiyama, T., et al. 1997. Cancer Res.57, 1495. Seynaeve, C.M., et al. 1994. Mol. Pharmacol.45, 1207. Takahashi, I., et al. 1987, J. Antibiot.40, 1782.