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Submit ReviewChelerythrine chloride
Description: Cell-permeable protein kinase C inhibitor
Chemical Name: 1,2-Dimethoxy-12-methyl[1,3]benzodioxolo[5,6-c]phenanthridinium chloride
Purity: ≥98% (HPLC)
Biological Activity for Chelerythrine chloride
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 for Chelerythrine chloride
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Chelerythrine chloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 3.84 | 10 | |
| DMSO | 3.84 | 10 |
Preparing Stock Solutions for Chelerythrine chloride
The following data is based on the product molecular weight 383.83. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 26.05 mL | 130.27 mL | 260.53 mL |
| 0.5 mM | 5.21 mL | 26.05 mL | 52.11 mL |
| 1 mM | 2.61 mL | 13.03 mL | 26.05 mL |
| 5 mM | 0.52 mL | 2.61 mL | 5.21 mL |
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Product Datasheets for Chelerythrine chloride
References for Chelerythrine chloride
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for Chelerythrine chloride, please let us know.
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Keywords: Chelerythrine chloride, Chelerythrine chloride supplier, Potent, protein, kinase, C, inhibitors, inhibits, PKC, Kinases, Protein, Kinase, 1330, Tocris Bioscience
17 Citations for Chelerythrine chloride
Citations are publications that use Tocris products. Selected citations for Chelerythrine chloride include:
Cho et al (2012) Pituitary adenylate cyclase-activating polypeptide induces postsynaptically expressed potentiation in the intra-amygdala circuit. J Neurosci 32 14165 PMID: 23055486
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 mor. tolerance at spinal levels of rats. Autophagy 1 122 PMID: 22778820
Livingstone et al (2019) Secreted Amyloid Precursor Protein-Alpha Promotes Arc Protein Synthesis in Hippocampal Neurons. Front Mol Neurosci 12 198 PMID: 31474829
Martín-Segura et al (2019) Aging Increases Hippocampal DUSP2 by a Membrane Cholesterol Loss-Mediated RTK/p38MAPK Activation Mechanism. Front Neurol 10 675 PMID: 31293510
Liu and Zhuo (2014) Loss of long-term depression in the insular cortex after tail amputation in adult mice. Mol Pain 10 1 PMID: 24398034
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
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
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
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
Ortinski et al (2015) Cocaine-seeking is associated with PKC-dependent reduction of excitatory signaling in accumbens shell D2 DA receptor-expressing neurons. Neuropharmacology 92 80 PMID: 25596492
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
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
Chen et al (2011) mGluR5 positive modulators both potentiate activation and restore inhibition in NMDA receptors by PKC dependent pathway. J Biomed Sci 18 19 PMID: 21342491
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 (2010) The effects of sympathetic outflow on upregulation of vanilloid receptors TRPV(1) in primary afferent neurons evoked by intradermal capsaicin. Exp Neurol 222 93 PMID: 20036240
Li (2017) Involvement of galanin and galanin receptor 1 in nociceptive modulation in the central nucleus of amygdala in normal and neuropathic rats. Sci Rep 7 15317 PMID: 29127424
Do you know of a great paper that uses Chelerythrine chloride from Tocris? Please let us know.
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