Celastrol 是一种蛋白酶体抑制剂，抑制20S 蛋白酶体的胰凝乳蛋白酶样活性，IC50为2.5 μM。

Celastrol is an effective proteasome inhibitor for the chymotrypsin-like activity of a purified 20S proteasome(IC50=2.5 μM) with antioxidant and anti-inflammatory activity.

在携带PC-3肿瘤的雄性裸鼠中, Celastrol（3 mg/kg）显著抑制肿瘤的生长,诱导肿瘤细胞凋亡,并提高p27水平和Bax水平.在携带C4-2B肿瘤的裸鼠中,Celastrol（3 mg/kg）抑制肿瘤的生长,降低蛋白酶体活性,也降低AR蛋白表达.在大鼠中, Celastrol（0.2 mg/kg）能够明显改善记忆和学习能力.

在RPMI-8226 细胞中,Celastrol（1 μM）抑制Akt通路,激活JNK激酶。在KBM-5细胞中, Celastrol（2.5 μM）加强TNF和化疗药物诱导的细胞凋亡,且抑制入侵。在脂多糖诱导的小胶质细胞中,Celastrol（100 nM）降低的Ⅱ类MHC分子。在脂多糖诱导的人体单核细胞和巨噬细胞中,Celastrol（300 nM）抑制TNF-α和IL-1β的生产。在巨噬细胞中（IC50=200 nM）,Celastro强抑制脂多糖和IFN-γ诱导的NO产生。在血管内皮细胞中（IC50为200 nM）,Celastrol强抑制TNF-α和IFN-γ诱导的NO产生。

Inhibition of purified 20S proteasome activity: A purified rabbit 20S proteasome (0.1 μg) is incubated with 40 μM of various fluorogenic peptide substrates in 100 μL assay buffer (20 mM Tris-HCl (pH 7.5)), in the presence of Celastrol at different concentrations or in the solvent DMSO for 2 hours at 37 ℃, followed by measurement of inhibition of each proteasomal activity.

The anti-proliferative effect of celastrol on various human tumor cell lines is determined by the MTT uptake method. Briefly, 5×103 cells are incubated with Celastrol in triplicate in a 96-well plate at 37 ℃. MTT solution is then added to each well. After a 2 hours incubation at 37 ℃, extraction buffer (20% SDS, 50% dimethylformamide) is added, cells are incubated overnight at 37 ℃, and the optical density is then measured at 570 nm using a Tecan plate reader.(Only for Reference)

34157-83-0

C29H38O4

450.619

Celastrol;雷公藤红素;Tripterine

DMSO:45.1 mg/mL (100 mM)
Ethanol:33.8 mg/mL (75 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years