Hypericin was originally isolated from Hypericum perforatum L. (St. John's Wort). Can be additionally isolated via irradiation of oxypenicilliopsin produced by Penicilliopsis clavariaeformis. A potent and selective inhibitor of PKC (protein kinase C) and additionally reported to inhibit Casein Kinase II (CKII), MAP Kinase, Insulin R, EGFR, PI-3 Kinase. Hypericin is also noted to possess antiviral activity and is of interest in HIV studies. Hypericin is of interest in studies investigating photodynamic treatment of tumors and has been reported to be cytotoxic to some tumor cell lines when Hypericin is photoactivated. Hypericin is an inhibitor of EGFR.
1. Meruelo, D., et al. 1988. Proc. Natl. Acad. Sci. U.S.A. 85: 5230-5234. PMID: 2839837 2. Takahashi, I., et al. 1989. Biochem. Biophys. Res. Commun. 165: 1207-1212. PMID: 2558652 3. Solár, P., et al. 2011. Radiat. Res. 175: 51-56. PMID: 21175347
Soluble in DMSO (25 mg/mL), ethanol (10 mM), methanol, acetone, ethylmethylketone, pyridine or other organic solvents, bases, and 1 M NaOH (10 mg/mL). Insoluble in water.
Store at 4° C
1020.33° C at 760 mmHg
tyrosine kinases: IC50 = 7.5 µM; casein kinase II : IC50 = 6 nM; protein kinase C: IC50 = 3.3 µM; MAP kinase : IC50 = 4 nM; the protein tyrosine activities of the insulin receptor : IC50 = 20-29 nM; the epidermal growth factor receptor: IC50 = 35 nM; apoptosis: IC50 = 0.1 µM (neuroblastoma cells)
Dopamine D3 receptor: Ki= 34.5 nM (human)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
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Rated 5 out of
Rajendra etRajendra et. al. (PubMed ID 15556948) used Hypericin (CAS 548-04-9) to inhibit the activity of ERK-2/MAPK in the course of determining whether the phosphorylation by MAPK regulates simian immunodeficiency virus Vpx protein nuclear import and virus infectivity. -SCBT QC
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