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Chelerythrine chloride
Chemical Name:1,2-Dimethoxy-12-methyl[1,3]benzodioxolo[5,6-c]phenanth
ridinium chloride
Biological Activity:
Potent, cell-permeable inhibitor of protein kinase C (IC50
= 660 nM); competitive with respect to the phosphate acceptor and
non-competitive with respect to ATP. Has a wide range of biological activities,
including antiplatelet, anti-inflammatory, antibacterial and antitumour
effects. Activates MAPK pathways, independent of PKC inhibition. Inhibits
binding of BclXL to Bak (IC50 = 1.5 μM) or Bad proteins and stimulates apoptosis.
Herbertet al (1990) Chelerythrine is a potent and specfic
inhibitor of protein kinase C. Biochem.Biophys.Res.Comm. 172 993.
Leeet al (1998) Angoline and chelerythrine, benzophenanthridine
alkaloids that do not inhibit protein kinase C. J.Biol.Chem. 273
19829. Yuet al (2000) Activation of p38 and c-Jun N-terminal
kinase pathways and induction of apoptosis by chelerythrine do not require
inhibition of protein kinase C. J.Biol.Chem. 275 9612. Chanet al (2003) Identification of chelerythrine as an inhibitor of BclXL
function. J.Biol.Chem. 278 20453.