Chelerythrine chloride

Cat. No. 1330

Chelerythrine chloride C21H18ClNO4 [3895-92-9]

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Chemical Name: 1,2-Dimethoxy-12-methyl[1,3]benzodioxolo[5,6-c]phenanthridinium chloride

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
Solubility:
Soluble to 10 mM in water and to 10 mM in DMSO
Purity:
>98 %
Storage:
Desiccate at -20°C
CAS No:
3895-92-9

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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

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.

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.

Lee et al (1998) Angoline and chelerythrine, benzophenanthridine alkaloids that do not inhibit protein kinase C. J.Biol.Chem. 273 19829. PMID: 9677417.

Herbert et al (1990) Chelerythrine is a potent and specfic inhibitor of protein kinase C. Biochem.Biophys.Res.Commun. 172 993. PMID: 2244923.

If you know of a relevant reference for Chelerythrine chloride please let us know.

Citations are publications that use Tocris products. Selected citations for Chelerythrine chloride include:

Morelli et al (2014) Cross-talk between alpha1D-adrenoceptors and transient receptor potential vanilloid type 1 triggers prostate cancer cell proliferation. BMC Cancer 14 921. PMID: 25481381.

Gosselin et al (2013) Extracellular microvesicles from astrocytes contain functional glutamate transporters: regulation by protein kinase C and cell activation. Front Cell Neurosci 7 251. PMID: 24368897.

Most et al (2013) S100A1 deficiency impairs postischemic angiogenesis via compromised proangiogenic endothelial cell function and nitric oxide synthase regulation. Circ Res 112 66. PMID: 23048072.

Cho et al (2012) Pituitary adenylate cyclase-activating polypeptide induces postsynaptically expressed potentiation in the intra-amygdala circuit. J Neurosci 32 14165. PMID: 23055486.

Mockett et al (2011) Calcium/calmodulin-dependent protein kinase II mediates group I metabotropic glutamate receptor-dependent protein synthesis and long-term depression in rat hippocampus. J Neurosci 31 7380. PMID: 21593322.

Fuortes et al (2010) Distinctions between persistent and reversible group I mGluR-induced epileptiform burst prolongation. Epilepsia 51 1633. PMID: 20659148.

Jin and Yu (2010) Involvement of protein kinase C in morphine tolerance at spinal levels of rats. Autophagy 1 122. PMID: 22778820.

Song et al (2010) Involvement of protein kinase C-CPI-17 in androgen modulation of angiotensin II-renal vasoconstriction. ACS Chem Neurosci 85 614. PMID: 19797427.

Xie and Wang (2009) Ablation of transient receptor potential vanilloid 1 abolishes endothelin-induced increases in afferent renal nerve activity: mechanisms and functional significance. Hypertension 54 1298. PMID: 19858408.

Xu et al (2009) Increases in transient receptor potential vanilloid-1 mRNA and protein in primary afferent neurons stimulated by protein kinase C and their possible role in neurogenic inflammation. Cardiovasc Res 87 482. PMID: 18752301.

Do you know of a great paper that uses Chelerythrine chloride from Tocris? If so please let us know.show all ▼show less ▲

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Keywords: Chelerythrine chloride, supplier, Potent, protein, kinase, C, inhibitors, inhibits, PKC, Kinases, Tocris Bioscience, Protein Kinase C Inhibitor products

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