Merck, 220285-5MG, Chelerythrine Chloride

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.
Biochem/physiol Actions
Product does not compete with ATP.
Reversible: no
Primary Target
PKC
Cell permeable: yes
Preparation Note
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.
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Harmful (C)