| 名称 | Tripterin |
| 描述 | Tripterin (Celastrol) is a natural product, a proteasome inhibitor that inhibits the pancreatic rennet-like activity of the 20S proteasome (IC50=2.5 μM). Tripterin has anti-inflammatory, anti-infectious, and immunomodulatory properties. |
| 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 | METHODS: Human prostate cancer cells PC-3 were treated with Tripterin (0.5-5 µM) for 12 h. Proteasomal chymotrypsin-like activity was assayed using Z-GGL-AMC.
RESULTS: Tripterin significantly inhibited proteasomal chymotrypsin-like activity in PC-3 cells in a concentration-dependent manner, reaching about 55% inhibition at 2.5 µM. [1]
METHODS: Human chronic myeloid leukemia cells KBM-5 were incubated with Tripterin (2.5 µM) for 6 h, followed by treatment with TNF (1 nM) for 6-24 h. Target protein expression levels were detected using Western Blot.
RESULTS: TNF induced the expression of anti-apoptotic proteins IAP1, IAP2, Bcl-2, Bcl-XL, c-FLIP and survivin in a time-dependent manner, which was inhibited by Tripterin. [2] |
| 体内活性 | METHODS: To detect anti-tumor activity in vivo, Tripterin (1-3 mg/kg, 10% DMSO+70% Cremophor/ethanol (3:1)+20% PBS) was injected intraperitoneally once daily for sixteen days into nude immunodeficient mice bearing human prostate cancer tumor PC-3.
RESULTS: Tripterin treatment significantly inhibited the growth of prostate cancer xenografts and suppressed proteasome activity and induced apoptosis in vivo. [1]
METHODS: To detect anti-tumor activity in vivo, Tripterin (1.25 mg/kg) was intraperitoneally injected into BALB/c (nu/nu) mice bearing vestibular nerve sheath tumor SC4 every three days for two weeks.
RESULTS: Tripterin significantly inhibited tumor growth without showing toxicity. [3] |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4.51 mg/mL (10.01 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
DMSO : 60 mg/mL (133.15 mM)
Ethanol : 33.8 mg/mL (75 mM)
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| 关键字 | inhibit | Mitophagy | Tripterin | Endogenous Metabolite | Proteasome | Mitochondrial Autophagy | Autophagy | Apoptosis | Inhibitor |
| 相关产品 | Stavudine | Dextran sulfate sodium salt (MW 4500-5500) | Sodium 4-phenylbutyrate | L-Ascorbic acid | Hydroxychloroquine | Guanidine hydrochloride | Tributyrin | Valproic Acid | Paeonol | Naringin | Gefitinib | Oleic acid |
| 相关库 | 抗癌天然产物库 | 经典已知活性库 | 中药单体化合物库 | 植物来源化合物库 | 天然产物库 | 抑制剂库 | 抗衰老化合物库 | 抗癌活性化合物库 |
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