Biological Activity
Cell-permeable inhibitor of protein kinase C (IC50 = 660 nM); competitive with respect to the phosphate acceptor and non-competitive with respect to ATP. Has a wide range of biological activities, including antiplatelet, anti-inflammatory, antibacterial and antitumor effects. Activates MAPK pathways, independent of PKC inhibition. Inhibits binding of BclXL to Bak (IC50 = 1.5 μM) or Bad proteins and stimulates apoptosis.
Technical Data
| M. Wt | 383.83 |
| Formula | C21H18ClNO4 |
| Storage | Desiccate at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 3895-92-9 |
| PubChem ID | 72311 |
| InChI Key | WEEFNMFMNMASJY-UHFFFAOYSA-M |
| Smiles | C[N+](C3=C2C=CC4=C3C=C(OCO5)C5=C4)=CC1=C2C=CC(OC)=C1OC.[Cl-] |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 3.84 | 10 | |
| water | 3.84 | 10 |
Preparing Stock Solutions
The following data is based on the product molecular weight 383.83. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.61 mL | 13.03 mL | 26.05 mL |
| 5 mM | 0.52 mL | 2.61 mL | 5.21 mL |
| 10 mM | 0.26 mL | 1.3 mL | 2.61 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.52 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Chan et al (2003) Identification of chelerythrine as an inhibitor of BclXL function. J.Biol.Chem. 278 20453 PMID: 12702731
Herbert et al (1990) Chelerythrine is a potent and specfic inhibitor of protein kinase C. Biochem.Biophys.Res.Commun. 172 993 PMID: 2244923
Lee et al (1998) Angoline and chelerythrine, benzophenanthridine alkaloids that do not inhibit protein kinase C. J.Biol.Chem. 273 19829 PMID: 9677417
Yu et al (2000) Activation of p38 and c-Jun N-terminal kinase pathways and induction of apoptosis by chelerythrine do not require inhibition of protein kinase C. J.Biol.Chem. 275 9612 PMID: 10734112
Keywords: Chelerythrine chloride, supplier, Potent, protein, kinase, C, inhibitors, inhibits, PKC, Kinases, Protein, Kinase, C, Protein, Kinase, C, Tocris Bioscience
