Chelerythrine chloride
- 貨號 Cat. No.
- C-400
- 規格 Size
- 10 x 0.25 mg 1mg 5x1mg 5mg
Description
Chelerythrine chloride
Protein Kinase C Inhibitor
| Product#: | C-400 |
| Sizes: |
| 10 x 0.25 mg |
| 1 mg |
| 5 x 1 mg |
| 5 mg |
| M.W.: | 383.84 |
| CAS No.: | [3895-92-9] |
| Structure: |
| . |
 |
| Purity: | >99% |
| Bioassay: |
The biological activity was tested to confirm the ability of Chelerythrine to inhibit PKC. |
 |
NIH/3T3 cells were incubated with different concentrations of Chelerythrine (0-20 mM) for 30 min and then stimulated with TPA (3ng/ml) for 20 min. Cell extracts were blotted and probed with Phospho-Myristoylated alanin-rich protein kinase C substrate (P-MARCKS) antibody. |
| References: |
1. | Herbert, J.M. et al. (1990) Biochem. Biophys. Res. Commun. 172, 993. |
2. | Chao, M.D. et al. (1998) Planta Med. 64, 662. |
3. | Ko, F.N. et al. (1990) Biochim. Biophys. Acta 1052, 360. |
4. | Le Corvoisier, P. et al. (2002) Fundam. Clin. Pharmacol. 16, 31. |
5. | Shi, L. et al. (1999) Arch. Biochem. Biophys. 368, 40. |
6. | Sweeney, J.F. et al. (2000) Shock 13, 464. |
7. | Chan, S.L. et al. (2003) J Biol. Chem. 278, 20453. |
Chelerythrine is a potent, cell-permeable inhibitor of protein kinase C (IC50 = 660nM) that binds to the catalytic domain of PKC. Chelerythrine is at least 100-fold more selective for PKCs than for other kinases.1,2
In platelets, Chelerythrine inhibits thromboxane formation and phosphoinositide metabolism.3,4 It has an inhibitory effect on ACh-induced current in PC12 cells.5
Chelerythrine induces apoptotic cell death in polymorphonuclear leukocyte through activation of caspase-3.6 Furthermore, Chelerythrine treated cells underwent apoptosis, with features that suggest involvement of the mitochondrial pathway, and through a mechanism that involves inhibition of the anti-apoptotic inhibitor BclXL.7