Cell Signaling Technology

Product Pathways - Ca / cAMP / Lipid Signaling

Chelerythrine Chloride #11916

Molecular Formula:
C21H18NO4Cl
Molecular Weight:
383.82 g/mol
Purity:
>99%

Directions for Use

Chelerythrine Chloride is supplied as a lyophilized powder. For a 10 mM stock, reconstitute the 5 mg in 1.30 ml DMSO. Working concentrations and length of treatment can vary depending on the desired effect, but it is typically used at 1-20 µM either as a pretreatment for 15 min-1 hr prior to treating with a stimulator or used alone with varying treatment times lasting up to 24 hr.

Western Blotting

Western Blotting

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).

Structure

Structure

Chemical structure of chelerythrine chloride.

Background

Chelerythrine is a benzophenanthridine alkaloid that elicits a wide range of biological responses. It was initially reported to be a potent PKC inhibitor (IC50 = 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 (IC50 = 1.5 μM) and disrupting the interaction between Bcl-xL and Bax (7), and induces apoptosis (6-8).

  1. Herbert, J.M. et al. (1990) Biochem Biophys Res Commun 172, 993-9.
  2. Chao, M.D. et al. (1998) Planta Med 64, 662-3.
  3. Nakai, M. et al. (1999) J Neurochem 72, 1179-86.
  4. Iwabu, A. et al. (2004) J Biol Chem 279, 14551-60.
  5. Lee, S.K. et al. (1998) J Biol Chem 273, 19829-33.
  6. Yu, R. et al. (2000) J Biol Chem 275, 9612-9.
  7. Chan, S.L. et al. (2003) J Biol Chem 278, 20453-6.
  8. Chmura, S.J. et al. (2000) Clin Cancer Res 6, 737-42.

Application References

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For Research Use Only. Not For Use In Diagnostic Procedures.

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