Naturally occurring alkaloid. Cell-permeable, selective inhibitor of protein kinase C (IC₅₀ = 660 nM). Acts on the catalytic domain irrespective of the attachment of the regulatory domain. Material is a competitive inhibitor with respect to the phosphate acceptor and a non-competitive inhibitor with respect to ATP. Over ten-fold more potent than H-7, HCl (Cat. No. 371955). Inhibits thromboxane formation and phosphoinositide metabolism in platelets. Also induces apoptotic DNA fragmentation and cell death in HL-60 human promyelocytic leukemia cells.

Naturally-occurring alkaloid. Potent, selective, and cell-permeable inhibitor of protein kinase C (IC₅₀ = 660 nM). Acts on the catalytic domain of PKC. A competitive inhibitor with respect to the phosphate acceptor and a non-competitive inhibitor with respect to ATP. Over ten-fold more potent than H-7, HCl (Cat. No. 371955). Inhibits thromboxane formation and phosphoinositide metabolism in platelets. Also induces apoptotic DNA fragmentation and cell death in HL-60 human promyelocytic leukemia cells.

Cell permeable: yes

Primary Target
PKC

Product does not compete with ATP.

Reversible: no

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

Heating to 40-50°C with gentle agitation may be necessary to achieve complete solubilization. Further dilute with buffer just prior to use.

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Herbert, J.M., et al. 1990. Biochem. Biophys. Res. Commun.172, 993.
Ko, F., et al. 1990. Biochim. Biophys. Acta1052, 360.
Walterova, D., et al. J. Med. Chem.24, 1100.

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

Toxicity: Harmful (C)