Celastrol | CAS:34157-83-0

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Name:Celastrol; Tripterin
Cat. No. :CS-0409
CAS No. :34157-83-0
Formula:C29H38O4
M. Wt. : 450.61
Solubility:10 mM in DMSO

Celastrol is a proteasome inhibitor, potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome (IC50=2.5 μM). IC50 & Target: IC50: 2.5 μM (20S proteasome)[1]In Vitro: Celastrol 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[1].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[1]. Following treatment with 3 and 6 mg/kg Celastrol, the levels of malondialdehyde (MDA) are significantly decreased by 35.2 and 36.7% (P[2].

Guan Y, et al. Celastrol attenuates oxidative stress in the skeletal muscle of diabetic rats by regulating the AMPK-PGC1α-SIRT3 signaling pathway. Int J Mol Med. 2016 May;37(5):1229-38. 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 May 1;66(9):4758-65.