雷公藤红素 T3028

Product Introduction
Bioactivity


英文名: Tripterin

描述: Tripterin (Celastrol) 属于天然产物，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=2.5 μM)。Tripterin 具有抗炎、抗感染和免疫调节的作用。

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)

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.

体外活性: 方法：人前列腺癌细胞 PC-3 用 Tripterin (0.5-5 µM) 处理 12 h，使用 Z-GGL-AMC 检测蛋白酶体糜蛋白酶样活性。结果：Tripterin 以浓度依赖的方式显著抑制 PC-3 细胞中蛋白酶体糜蛋白酶的活性，在 2.5 µM 时，达到约 55% 的抑制作用。[1]方法：人慢性髓白血病细胞 KBM-5 用 Tripterin (2.5 µM) 孵育 6 h，随后用 TNF (1 nM) 处理 6-24 h，使用 Western Blot 检测靶点蛋白表达水平。结果：TNF 以时间依赖的方式诱导抗凋亡蛋白 IAP1、IAP2、Bcl-2、Bcl-XL、c-FLIP 和 survivin 的表达，Tripterin 抑制了表达。[2]

体内活性: 方法：为检测体内抗肿瘤活性，将 Tripterin (1-3 mg/kg，10% DMSO+70% Cremophor/ethanol (3:1)+20% PBS) 腹腔注射给携带人前列腺癌肿瘤 PC-3 的 nude immunodeficient 小鼠，每天一次，持续十六天。结果：Tripterin 治疗显著抑制前列腺癌症异种移植物的生长，并抑制体内蛋白酶体活性和诱导细胞凋亡。[1]方法：为检测体内抗肿瘤活性，将 Tripterin (1.25 mg/kg) 腹腔注射给携带前庭神经鞘瘤 SC4 的 BALB/c (nu/nu) 小鼠，每三天一次，持续两周。结果：Tripterin 显著抑制肿瘤生长而不显示毒性。[3]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 60 mg/mL (133.15 mM)
5% DMSO+95% Saline : 2.26 mg/mL (5 mM, suspension)
Ethanol : 33.8 mg/mL (75 mM)


关键字: inhibit | Mitophagy | Tripterin | Endogenous Metabolite | Proteasome | Mitochondrial Autophagy | Autophagy | Apoptosis | Inhibitor

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相关库: Antioxidant Compound Library | Bioactive Lipid Compound Library | Mitochondria-Targeted Compound Library | Anti-Metabolism Disease Compound Library | Ubiquitination Compound Library | Inhibitor Library | Traditional Chinese Medicine Monomer Library | Anti-Cancer Active Compound Library | NO PAINS Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途