Chelerythrine chloride

Chelerythrine chloride

An Inhibitor of Protein Kinase C, SERCA Pump, and P2X7 Receptor
Cat #: C-400
Sizes: 1 mg, 5 x 1 mg, 5 mg
Source: Natural
MW: 383.84 Da.
Target: PKC, SERCA pumps, P2X7 receptor

Chelerythrine is a potent, cell-permeable inhibitor of protein kinase C (IC₅₀ = 660 nM) 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-3.⁶Furthermore, 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

Chelerythrine inhibits SERCA pumps with an IC₅₀ of 1.5 µM⁸. It also antagonizes P2X7 receptors; it inhibits ATP-induced ⁸⁶Rb⁺ efflux with an IC₅₀ of 5.6 µM⁹.

Alomone Labs is pleased to offer Chelerythrine chloride (#C-400), isolated and purified from Macleaya Cordata.

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. and Wang, Ca. (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.
8. Vieira, S.M. et al. (2015) Arch. Biochem. Biophys. 570, 58.
9. Shemon, A.N. et al. (2004) Br. J. Pharmacol. 142, 1015.

For a list of product citations in the literature, see product citations tab below. If you know of additional relevant citations for this product, please let us know.

• Our Bioassay
• Specifications
• Citations
• Related Products

Our bioassay

Alomone Labs Chelerythrine chloride inhibits NGF-mediated survival of serum-deprived PC12 cells.
Dose response curve of Chelerythrine chloride (#C-400) inhibition of the 100 ng/ml mouse NGF 2.5S (>95%) (#N-100) mediated survival of serum-deprived PC12 cells. IC₅₀ was determined at 8.3 µM.

Alomone Labs Chelerythrine chloride inhibits PKC in NIH-3T3 cells.
Cells were incubated with different concentrations of Chelerythrine chloride (#C-400) for 30 min and then stimulated with PMA (#P-800), (3 ng/ml) for 20 min. Cell proteins were resolved by SDS-PAGE and probed with anti-phospho (ser)-MARCKS (myristoylated alanin-rich protein kinase C substrate).
OriginAlkaloid isolated from Macleaya Cordata plant.
Purity>99%.
Effective concentration1-5 µM.
Chemical name1,2-Dimethozk-12-methyl[1,3]benzodioxolo[5,6-c]phenanthridinium chloride.
Molecular formulaC₂₁H₁₈ClNO₄.
CAS number3895-92-9.
Activity

Chelerythrine chloride is a potent, cell-permeable inhibitor of
protein kinase C (PKC). It is at least 100-fold more selective for PKCs than for other kinases^1,2.

Storage before reconstitutionLyophilized powder can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
ReconstitutionWater or DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
Storage after reconstitutionUp to two weeks at 4°C or six months at -20°C.
Product citations

1. Libster, A.M. et al. (2015) J. Neurophysiol. 114, 3339.
2. De Chiara, V. et al. (2013) Neuroscience 250, 232.