Chelerythrine Chloride #11916
Inquiry Info. # 11916
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Product Information
Product Usage Information
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.
Storage
Store lyophilized or in solution at -20ºC, desiccated. Protect from light. In lyophilized form, the chemical is stable for 24 months. Once in solution, use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.
Product Description
| Molecular Weight | 383.82 g/mol |
| Purity | >99% |
| Molecular Formula | C21H18NO4Cl |
| CAS | 3895-92-9 |
| Solubility | Soluble in DMSO and H2O at 5mg/ml. |
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).
- Herbert, J.M. et al. (1990) Biochem Biophys Res Commun 172, 993-9.
- Chao, M.D. et al. (1998) Planta Med 64, 662-3.
- Nakai, M. et al. (1999) J Neurochem 72, 1179-86.
- Iwabu, A. et al. (2004) J Biol Chem 279, 14551-60.
- Lee, S.K. et al. (1998) J Biol Chem 273, 19829-33.
- Yu, R. et al. (2000) J Biol Chem 275, 9612-9.
- Chan, S.L. et al. (2003) J Biol Chem 278, 20453-6.
- Chmura, S.J. et al. (2000) Clin Cancer Res 6, 737-42.
Alternate Names
apoptosis; Bax; Bcl-xL inhibitor; JNK; oxidative; p38
限制使用
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For Research Use Only. Not for Use in Diagnostic Procedures.
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