Rottlerin

Biochem/physiol Actions

Target IC₅₀: 3-6 µM against PKCδ; 5.3 µM against CaM kinase III

Reversible: yes

Product does not compete with ATP.

Primary TargetPKCδ

Cell permeable: yes

General description

A cell-permeable and reversible protein kinase C inhibitor that exhibits greater selectivity for PKC_δ (IC₅₀ = 3-6 µM) and PKC_θ. Inhibits the PKC_α, PKC_β, and PKC_γ isoforms, but with significantly reduced potency (IC₅₀ = 30-42 µM). Has reduced inhibitory activity on PKC_ε, PKC_η, and PKC_ζ (IC₅₀ = 80-100 µM). Also known to inhibit CaM kinase III (IC₅₀ = 5.3 µM).

Legal Information

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

Other Notes

Villalba, M., et al. 1999. J. Immunol. 163, 5813.Gschwendt, M., et al. 1994. Biochem. Biophys. Res. Commun. 199, 93.Gschwendt, M., et al. 1994. FEBS Lett.338, 85.Gschwendt, M., et al. 1984. Cancer Lett.25, 177.

Packaging

10 mg 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)