A cell-permeable and reversible lyso-sphingolipid protein kinase C (PKC) inhibitor that competitively interacts at the regulatory phorbol binding domain of PKC. Inhibits enzymatic activity and ³H-phorbol dibutyrate binding of purified rat brain PKC (IC₅₀ = 37.5 µM and 31 µM, respectively). Inhibits human PKC_α, the major overexpressed isoenzyme in MCF-7 DOXR cells (IC₅₀ = 40 µM). Enhances the cytotoxic effect of the chemotherapeutic agent Mitomycin C (MMC; Cat. Nos. 47589 and 475820) in gastric cancer cells by promoting drug-induced apoptosis.

Cell permeable: yes

Primary Target
Enzymatic activity and 3H-phorbol dibutyrate binding of purified rat brain PKC

Product does not compete with ATP.

Reversible: yes

Target IC₅₀: 37.5 µM and 31 µM, inhibiting enzymatic activity and 3H-phorbol dibutyrate binding of purified rat brain PKC, respectively

Following initial thaw, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Kedderis, L.B., et al. 1995. Fundam. Appl. Toxicol.25, 201.
Sachs, C.W., et al. 1995. J. Biol. Chem. 270, 26639.
Schwartz, G.K., et al. 1995. J. Natl. Cancer Inst.87,1394.

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

Toxicity: Irritant (B)