Biochem/physiol Actions

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

Reversible: yes

Primary TargetPKCα, 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.

Cell permeable: yes

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 M 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 M for PDK1, lck, MAPKAP kinase-2, Akt, GSK-3β and PKA, respectively). At higher concentrations (>15 M), 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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

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.

Packaging

Packaged under inert gas

500 µg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Warning

Toxicity: Standard Handling (A)