Biochem/physiol Actions

Target K_i: 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 (K_i = 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 (K_i = 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)