Celastrol Inhibitor CAS No. 34157-83-0

Cat. No.	Name	Size	Price
KI1002	Celastrol	25 mg	$336
	Celastrol	50 mg	$480
	Celastrol	100 mg	$752

Chemical Characteristic

Product Name	Celastrol
CAS No.	34157-83-0
Molecular Weight	450.61
Formula	C₂₉H₃₈O₄
Chemical Name	(2R,4aS,6aS,12bR,14aS,14bR)-10-hydroxy-2,4a,6a,9,12b,14a-hexamethyl-11-oxo-1,2,3,4,4a,5,6,6a,11,12b,13,14,14a,14b-tetradecahydropicene-2-carboxylic acid
Smiles	C1(=C(CC)C2=CC=C3[C@]4(C)CC[C@@]5(C)CCC(C)(C(=O)O)C[C@@H]5[C@@H]4CC[C@H]3C2=C(C1=O)C)O
Chemical Structure

Biological activities

Celastrol is an active compound extracted from the root bark of the Chinese medicine Tripterygium wilfordii and is used in the treatment of autoimmune diseases, asthma, chronic inflammation, and neurodegenerative disease. Celastrol potently inhibits the chymotrypsin-like activity of a purified rabbit 20S proteasome with an IC50 of 2.5 µM. Celastrol inhibits human prostate cancer 26S proteasome at 1-5 µM. ^[1] Besides, celastrol can inhibit the proliferation of a variety of tumor cells, including those from leukemia, gliomas, and prostate cancer. Celastrol potentiates the apoptosis induced by TNF and chemotherapeutic agents and inhibits invasion, both regulated by NF-κB activation. ^[2] Celastrol exhibits potent antitumor activity against ErB2-overexpressing breast cancer cells (SKBr-3, BT-474, 21ME-1, JIMT-1, MCF-7) with IC50 of 0.13, 0.16, 0.53, 0.48 and 1.56 µM, respectively.^[3] Treatment of PC-3 tumor-bearing nude mice with celastrol (1-3 mg/kg/d, i.p., 1-31 days) results in significant inhibition (65-93%) of the tumor growth.^[1]

Protocols

Celastrol is dissolved in DMSO at a stock concentration of 50 mM, aliquoted, and stored at -20°C.^[1]

References

[1] Yang H, et al. Celastrol, a triterpene extracted from the Chinese "Thunder of God Vine," is a potent proteasome inhibitor and suppresses human prostate cancer growth in nude mice. Cancer Res. 2006, 66 (9): 4758-4765. [2] Sethi G, et al. Celastrol, a novel triterpene, potentiates TNF-induced apoptosis and suppresses invasion of tumor cells by inhibiting NF-kB-regulated gene products and TAK1-mediated NF-kB activation. Blood. 2007, 109 (7): 2727-2735. [3] Raja SM, et al. Anticancer activity of Celastrol in combination with ErbB2-targeted therapeutics for treatment of ErbB2-overexpressing breast cancers. Cancer Biol Ther. 2011, 11 (2): 263-276.

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