Catalog Number: 1330
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:
  • Formula:
  • Solubility:
    Soluble to 10 mM in water and to 10 mM in DMSO
  • Purity:
  • Storage:
    Desiccate at -20°C
  • CAS No:
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.
Background References
  1. Identification of chelerythrine as an inhibitor of BclXL function.
    Chan et al.
    J.Biol.Chem., 2003;278:20453
  2. Chelerythrine is a potent and specfic inhibitor of protein kinase C.
    Herbert et al.
    Biochem.Biophys.Res.Commun., 1990;172:993
  3. Angoline and chelerythrine, benzophenanthridine alkaloids that do not inhibit protein kinase C.
    Lee et al.
    J.Biol.Chem., 1998;273:19829
  4. Activation of p38 and c-Jun N-terminal kinase pathways and induction of apoptosis by chelerythrine do not require inhibition of protein kinase C.
    Yu et al.
    J.Biol.Chem., 2000;275:9612

The citations listed below are publications that use Tocris products. Selected citations for Chelerythrine chloride include:

10 Citations: Showing 1 - 10
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  1. Cross-talk between alpha1D-adrenoceptors and transient receptor potential vanilloid type 1 triggers prostate cancer cell proliferation.
    Authors: Morelli Et al.
    BMC Cancer 2014;14:921
  2. Extracellular microvesicles from astrocytes contain functional glutamate transporters: regulation by protein kinase C and cell activation.
    Authors: Gosselin Et al.
    Front Cell Neurosci 2013;7:251
  3. S100A1 deficiency impairs postischemic angiogenesis via compromised proangiogenic endothelial cell function and nitric oxide synthase regulation.
    Authors: Most Et al.
    Circ Res 2013;112:66
  4. Pituitary adenylate cyclase-activating polypeptide induces postsynaptically expressed potentiation in the intra-amygdala circuit.
    Authors: Cho Et al.
    J Neurosci 2012;32:14165
  5. Calcium/calmodulin-dependent protein kinase II mediates group I metabotropic glutamate receptor-dependent protein synthesis and long-term depression in rat hippocampus.
    Authors: Mockett Et al.
    J Neurosci 2011;31:7380
  6. Involvement of protein kinase C-CPI-17 in androgen modulation of angiotensin II-renal vasoconstriction.
    Authors: Song Et al.
    ACS Chem Neurosci 2010;85:614
  7. Distinctions between persistent and reversible group I mGluR-induced epileptiform burst prolongation.
    Authors: Fuortes Et al.
    Epilepsia 2010;51:1633
  8. Involvement of protein kinase C in morphine tolerance at spinal levels of rats.
    Authors: Jin and Yu
    Autophagy 2010;1:122
  9. 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.
    Authors: Xu Et al.
    Cardiovasc Res 2009;87:482
  10. Ablation of transient receptor potential vanilloid 1 abolishes endothelin-induced increases in afferent renal nerve activity: mechanisms and functional significance.
    Authors: Xie and Wang
    Hypertension 2009;54:1298

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