Celastrol, Celastrus scandens, a compound originally purified from Tripterygium wilfordii, has been shown to be an anti-peroxidative and anti-angiogenic agent. Mechanistic studies suggest that Celastrol suppresses levels of VEGF and Flk-1 receptors, VEGFR-1 and VEGFR-2, which may reduce signal transduction between the two growth factors. Additionally, Celastrol has demonstrated the ability to disrupt critical interaction of Glu33 (Hsp90) and Arg167 (Cdc37) in the superchaperone complex which causes anti-proliferative activity in vitro and inhibit Topo II (topoisomerase II) activity in vitro (IC50 = 7.41 μM). Celastrol, Celastrus scandens is an inhibitor of Hsp90.
1. Sassa, H., et al. 1990. Biochem. Biophys. Res. Commun. 172: 890-897. PMID: 2241977 2. Huang, Y., et al. 2008. Cancer Lett. 264: 101-106. PMID: 18343027 3. Zhang, T., et al. 2008. Mol. Cancer Ther. 7: 162-170. PMID: 18202019
Soluble in DMSO (>10 mg/ml), ethanol, DMF:PBS(pH 7.2)(1:10), and DMF. Insoluble in water.
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TrottTrott, A. et al. (PubMed 18199679) studied the biological effects of Celastrol (Celastrus scandens), a compound that displays anti-peroxidative, anti-angiogenic, and anti-proliferative properties. They found that Celastrol inhibited glucocoritcoid receptor activity and that its effects could be blocked by the addition of excess free thiol. -SCBT Publication Review
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