Chelerythrine chlorideA potent and selective inhibitor of protein kinase C

Chelerythrine chloride (CAS 3895-92-9)

Chelerythrine chloride | CAS 3895-92-9 is rated 5.0 out of 5 by 1.
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Synonym: Toddalin chloride
Application: A potent and selective inhibitor of protein kinase C
CAS Number: 3895-92-9
Purity: ≥98%
Molecular Weight: 383.82
Molecular Formula: C21H18NO4•Cl
* Refer to Certificate of Analysis for lot specific data (including water content).
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Chelerythrine chloride Is an isoquinoline alkaloid isolated from the root of Zanthoxylum simulans, Chelidonium majus L., and other Papaveraceae. It has been reported to be a potent and selective inhibitor of PKC (protein kinase C, IC50=0.66 μM), and an independent activator of MAPK pathways. The compound has been observed to induce apoptosis in HL-60 human promyelocytic leukemia cells. The proposed method of action of apoptotic stimulation is through the inhibition of binding BclXL to Bax or Bad at an IC50 = 1.5 μM. When used in combination with cisplatin (sc-200896) inhibition of cell proliferation of non-small cell lung cancer cells was increased in an additive/synergistic pattern. Also through inhibition of thromboxane formation and phosphoinositide breakdown chelerythrine chloride was demonstrated to inhibit rabbit platelet aggregation and release. Chelerythrine Chloride is an inhibitor of Cox-2.


References

1. Herbert, J.M., et al. 1990. Biochem. Biophys. Res. Commun. 172: 993-999. PMID: 2244923
2. Ko, F.N., et al. 1990. Biochim. Biophys. Acta. 1052: 360-365. PMID: 2162213
3. Jarvis, W.D., et al. 1994. Cancer Res. 54: 1707-1714. PMID: 7511048
4. Freemerman, A.J., et al. 1996. Mol. Pharmacol. 49: 788-795. PMID: 8622627
5. Chao, M.D., et al. 1998. Planta Med. 64: 662-663. PMID: 9810275
6. Hiruma, H., et al. 1999. Brain Res. 826: 135-138. PMID: 10216205
7. Yu, R., et al. 2000. J. Biol. Chem. 275: 9612-9619. PMID: 10734112
8. Lee, S.K., et al. 1998. J. Biol. Chem. 273: 19829-19833. PMID: 9677417

Appearance :
Powder
Physical State :
Solid
Solubility :
Soluble in methanol, 100% ethanol, water(warm) (2 mg/ml), and DMSO (≥10 mg/ml).
Storage :
Store at -20° C
IC50 :
protein kinase C: IC50 = 0.66 µm
Ki Data :
Apoptosis regulator Bcl-W : Ki= 106 µm (human); Apoptosis regulator Bcl-W: Ki= 171 µm (human)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
RTECS :
FL9200000
PubChem CID :
72311
Merck Index :
14: 2051
MDL Number :
MFCD00060717
EC Number :
223-444-9
SMILES :
C[N+]1=C2C(=C3C=CC(=C(C3=C1)OC)OC)C=CC4=CC5=C(C=C42)OCO5.[Cl-]

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Certificate of Analysis

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Chelerythrine chloride  Product Citations

See how others have used Chelerythrine chloride. Click on the entry to view the PubMed entry .

Citations 1 to 10 of 14 total

PMID: # 28399187  He, M. et al. 2017. PLoS ONE. 12: e0175466.

PMID: # 28566491  Silpanisong, J. et al. 2017. Am. J. Physiol., Cell Physiol. 313: C207-C218.

PMID: # 27543462  Sulen, A. et al. 2016. Pharmacol. Res. 113: 216-227.

PMID: # 27222466  2016. MBio. 7:

PMID: # 24265135  2014. J. Neurosci. Res. 92: 24-34.

PMID: # 22537485  2012. Can. J. Physiol. Pharmacol. 90: 637-45.

PMID: # 15764707  Zhang N et al. 2005. Proc. Natl. Acad. Sci. USA. 102(12): 4536-4541.

PMID: # 15632134  Kim, D.J. et al. 2005. J. Biol. Chem. 280: 9519-9527.

PMID: # 15020304  Das, A. et al. 2004. Am. J. Physiol. Heart Circ. Physiol. 286: H1455-H1460.

PMID: # 12801934  Wang, HY. et al. 2003. J. Biol. Chem. 278: 31547-31553.

Citations 1 to 10 of 14 total
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Rated 5 out of 5 by from Wang Wang, et. al. (PubMed ID # 12801934) found that chelerythrine chloride (CAS 3895-92-9) was not effective in knocking down A 42-induced tau phosphorylation at concentrations considered to be safe for cell viability. -SCBT Publication Review
Date published: 2015-03-07
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