Biochem/physiol Actions

Reversible: no

Product does not compete with ATP.

Primary TargetPKC

Cell permeable: yes

General description

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.

Legal Information

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

Other Notes

Kandasamy, R.A., et al. 1995. J. Biol. Chem.270 29209.Jarvis, W.D., et al. 1994. Cancer Res.54, 1707.Barg, J., et al. 1992. J. Neurochem.59, 1145.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.

Packaging

5 mg in Plastic ampoule

Preparation Note

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

Reconstitution

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

Warning

Toxicity: Harmful (C)