Description
Chelerythrine is a potent, cell permeable inhibitor of protein kinase C (IC
50 = 660 nM) that does not inhibit tyrosine protein kinases, cAMP-
dependent protein kinase, or calcium/calmodulin-
dependent protein kinase.
1 Chelerythrine also inhibits Bcl-xL function (IC
50 = 1.5 μM) by displacing Bax binding, inducing apoptosis in several cancer cell lines.
2 Chelerythrine can also have PKC-
independent effects, activate p38 MAP kinase and JUNK signaling pathways, and induce apoptosis in cancer cells both
in vitro and
in vivo.
3,4,5,6
References
1. j. m. herbert, j. m. augereau, j. gleye and j. p. maffrand, biochem biophys res commun 1990, 172, 993-999. 2. w. d. jarvis, a. j. turner, l. f. povirk, r. s. traylor and s. grant, cancer res 1994, 54, 1707-1714. 3. j. vrba, p. dolezel, j. vicar, m. modriansky and j. ulrichova, toxicol in vitro 2008, 22, 1008-1017. 4. m. vogler, k. weber, d. dinsdale, i. schmitz, k. schulze-osthoff, m. j. dyer and g. m. cohen, cell death differ 2009, 16, 1030-1039. 5. r. yu, s. mandlekar, t. h. tan and a. n. kong, j biol chem 2000, 275, 9612-9619. 6. s. yamamoto, k. seta, c. morisco, s. f. vatner and j. sadoshima, j mol cell cardiol 2001, 33, 1829-1848.