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Chelerythrine chloride

Catalog #: 1330
17 Citations Datasheet / COA / SDS
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1330/5
Chelerythrine chloride | CAS No. 3895-92-9 | Protein Kinase C Inhibitors
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Description: Cell-permeable protein kinase C inhibitor

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

Purity: ≥98%

Product Details
Citations (17)
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Biological Activity Technical Data Background Product Datasheets Calculators

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

  1. 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.
  2. Identification of chelerythrine as an inhibitor of BclXL function.
    Chan et al.
    J.Biol.Chem., 2003;278:20453
  3. Angoline and chelerythrine, benzophenanthridine alkaloids that do not inhibit protein kinase C.
    Lee et al.
    J.Biol.Chem., 1998;273:19829
  4. Chelerythrine is a potent and specfic inhibitor of protein kinase C.
    Herbert et al.
    Biochem.Biophys.Res.Commun., 1990;172:993
  5. 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

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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

  1. Secreted Amyloid Precursor Protein-Alpha Promotes Arc Protein Synthesis in Hippocampal Neurons.
    Authors: Livingstone Et al.
    Front Mol Neurosci  2019;12:198
  2. Aging Increases Hippocampal DUSP2 by a Membrane Cholesterol Loss-Mediated RTK/p38MAPK Activation Mechanism.
    Authors: Martín-Segura Et al.
    Front Neurol  2019;10:675
  3. 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
  4. 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
  5. 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
  6. Loss of long-term depression in the insular cortex after tail amputation in adult mice.
    Authors: Liu and Zhuo
    Mol Pain  2014;10:1
  7. 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
  8. 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
  9. Pituitary adenylate cyclase-activating polypeptide induces postsynaptically expressed potentiation in the intra-amygdala circuit.
    Authors: Cho Et al.
    J Neurosci  2012;32:14165
  10. 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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