| Description |
Chelerythrine is a benzophenanthridine alkaloid that elicits a wide range of biological responses. It was initially reported to be a potent PKC inhibitor (IC 50 = 660 nM) through interaction with the catalytic domain, competitive with respect to the phosphate acceptor, noncompetitive with respect to ATP (1), and is often used in research as a means to inhibit PKC activation (2-4). However, subsequent studies have shown that chelerythrine is not a potent PKC inhibitor and its effects are independent of PKC inhibition (5,6). Researchers have demonstrated that chelerythrine activates JNK and p38 through an oxidative stress mechanism (6), inhibits Bcl-xL by preventing Bcl-xL-Bak BH3 peptide binding (IC 50 = 1.5 μM) and disrupting the interaction between Bcl-xL and Bax (7), and induces apoptosis (6-8).
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Western blot analysis of extracts from HeLa cells, serum-starved overnight and untreated or treated with Chelerythrine Chloride (2 hr) at the indicated concentrations, using Phospho-SAPK/JNK (Thr183/Tyr185) (81E11) Rabbit mAb #4668 (upper) or SAPK/JNK (56G8) Rabbit mAb #9258 (lower).
Chemical structure of chelerythrine chloride.