Biochem/physiol Actions
Target Ki: 1.35 nM for protein kinase C
Cell permeable: no
Reversible: no
Primary TargetProtein kinase C
Product does not compete with ATP.
General description
A macrocyclic lactone with antitumor properties. Potently activates protein kinase C and exhibits a high binding affinity (Ki = 1.35 nM). Effectively translocates and down-regulates PKC isozymes α, δ, and ε. Induces a biphasic activation of PKD through a PKC-dependent pathway in intact cells. Also shown to activate Ras in Jurkat T cells and in rat2 cells.
A macrocyclic lactone that exhibits anti-tumor properties. Potently activates protein kinase C and exhibits high binding affinity (Ki = 1.35 nM). Effectively translocates protein kinase C (PKC) isozymes α, β, and ε and induces a biphasic, concentration-dependent, down-regulation of PKC δ. Reported to compete with phorbol esters in binding to PKC. Stimulates protein kinase D (PKD) activity in a biphasic, PKC-dependent manner in intact cells. Also activates Ras in Jurkat T cells and in rat2 cells.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Other Notes
Clamp, A., and Jayson, G. 2002. Anticancer Drugs13, 673.Lorenzo, P.S., et al. 1999. Cancer Res.59, 6137.Wang, Q.J., et al. 1999. J. Biol. Chem.274, 37233.Wender, P.A., et al. 1998. Proc. Natl. Acad. Sci. USA95, 6624.Matthews, S.A., et al. 1997. J. Biol. Chem.272, 20245.Szallasi, Z., et al. 1994. Mol. Pharmacol.46, 840.Berkow, R.L., and Kratt, A.S. 1985. Biochem. Biophys. Res. Commun.3, 1109.
Packaging
10 µg in Plastic ampoule
Reconstitution
Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Warning
Toxicity: Standard Handling (A)
This product has met the following criteria: