Chelerythrine chloride
1 Image
Description: Cell-permeable protein kinase C inhibitor
Chemical Name: 1,2-Dimethoxy-12-methyl[1,3]benzodioxolo[5,6-c]phenanthridinium chloride
Purity: ≥98%
Biological Activity
Chelerythrine chloride is a 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Cross-talk between alpha1D-adrenoceptors and transient receptor potential vanilloid type 1 triggers prostate cancer cell proliferation.
Morelli, Maria Be, Amantini, Consuelo, Nabissi, Massimo, Liberati, Sonia, Cardinali, Claudio, Farfariello, Valerio, Tomassoni, Daniele, Quaglia, Wilma, Piergentili, Alessand, Bonifazi, Alessand, Del Bello, Fabio, Santoni, Matteo, Mammana, Gabriele, Servi, Lucilla, Filosa, Alessand, Gismondi, Angela, Santoni, Giorgio
BMC Cancer, 2014;14(0):921. -
Identification of chelerythrine as an inhibitor of BclXL function.
Chan et al.
J.Biol.Chem., 2003;278:20453 -
Angoline and chelerythrine, benzophenanthridine alkaloids that do not inhibit protein kinase C.
Lee et al.
J.Biol.Chem., 1998;273:19829 -
Chelerythrine is a potent and specfic inhibitor of protein kinase C.
Herbert et al.
Biochem.Biophys.Res.Commun., 1990;172:993 -
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
Product Datasheets
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Citations for Chelerythrine chloride
The citations listed below are publications that use Tocris products. Selected citations for Chelerythrine chloride include:
17 Citations: Showing 1 - 10
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Secreted Amyloid Precursor Protein-Alpha Promotes Arc Protein Synthesis in Hippocampal Neurons.
Authors: Livingstone Et al.
Front Mol Neurosci 2019;12:198
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Aging Increases Hippocampal DUSP2 by a Membrane Cholesterol Loss-Mediated RTK/p38MAPK Activation Mechanism.
Authors: Martín-Segura Et al.
Front Neurol 2019;10:675
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Involvement of galanin and galanin receptor 1 in nociceptive modulation in the central nucleus of amygdala in normal and neuropathic rats.
Authors: Li
Sci Rep 2017;7(1):15317
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Cocaine-seeking is associated with PKC-dependent reduction of excitatory signaling in accumbens shell D2 DA receptor-expressing neurons.
Authors: Ortinski Et al.
Neuropharmacology 2015;92:80
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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
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Loss of long-term depression in the insular cortex after tail amputation in adult mice.
Authors: Liu and Zhuo
Mol Pain 2014;10:1
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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
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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
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Pituitary adenylate cyclase-activating polypeptide induces postsynaptically expressed potentiation in the intra-amygdala circuit.
Authors: Cho Et al.
J Neurosci 2012;32:14165
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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
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mGluR5 positive modulators both potentiate activation and restore inhibition in NMDA receptors by PKC dependent pathway.
Authors: Chen Et al.
J Biomed Sci 2011;18:19
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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
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Distinctions between persistent and reversible group I mGluR-induced epileptiform burst prolongation.
Authors: Fuortes Et al.
Epilepsia 2010;51:1633
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The effects of sympathetic outflow on upregulation of vanilloid receptors TRPV(1) in primary afferent neurons evoked by intradermal capsaicin.
Authors: Xu Et al.
Exp Neurol 2010;222:93
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Involvement of protein kinase C in mor. tolerance at spinal levels of rats.
Authors: Jin and Yu
Autophagy 2010;1:122
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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
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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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