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Celastrol

CAS No. : 34157-83-0

MCE 国际站：Celastrol

产品活性：Celastrol (Tripterine;Tripterin) 是一种蛋白酶体抑制剂，有效且优先抑制20S 蛋白酶体的胰凝乳蛋白酶样活性，IC₅₀ 为2.5 μM。

研究领域：Metabolic Enzyme/Protease  |  Autophagy  |  Apoptosis

作用靶点：Proteasome  |  Autophagy  |  Mitophagy  |  Apoptosis  |  Endogenous Metabolite

结构分类：萜类  |  三萜  |  结构分类

来源：植物  |  卫矛科  |  雷公藤

In Vitro: Celastrol (Tripterine;Tripterin) significantly inhibits the proteasomal chymotrypsin activity in PC-3 cells in a concentration-dependent manner; at 2.5 μM it reaches ~55% inhibition, comparable to its potency to a purified 20S proteasome (IC₅₀=2.5 μM). Furthermore, increased levels of IκB-α, Bax, and p27 are observed, three well known target proteins of the proteasome in PC-3 cells treated with Celastrol.

In Vivo: 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. Following treatment with 3 and 6 mg/kg Celastrol, the levels of malondialdehyde (MDA) are significantly decreased by 35.2 and 36.7% (P<0.05), respectively. Treatment with 3 and 6 mg/kg Celastrol markedly restores the GSH level (P<0.05) to almost normal levels.

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