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Tripterin
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Tripterin图片
CAS NO:34157-83-0
包装与价格:
包装价格(元)
20 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
Celastrol
雷公藤红素
Tripterine
产品介绍
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。

产品描述

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.

体外活性

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.

体内活性

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。

激酶实验

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.

细胞实验

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)

Cas No.

34157-83-0

分子式

C29H38O4

分子量

450.619

别名

Celastrol;雷公藤红素;Tripterine

储存和溶解度

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