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Celastrol

SKU: orb1304608

Description

Tripterin

Research Area

Cell Biology, Epigenetics & Chromatin, Neuroscience, Protein Biochemistry

Images & Validation

Key Properties

CAS Number34157-83-0
MW450.62
Purity>98%
FormulaC29H38O4
SMILESCC1=C(O)C(=O)C=C2C1=CC=C1[C@@]2(C)CC[C@@]2(C)[C@@H]3C[C@@](C)(CC[C@]3(C)CC[C@]12C)C(O)=O
TargetProteasome
SolubilitySoluble in DMSO (up to 45 mg/ml) or in Ethanol (up to 30 mg/ml).

Bioactivity

Target IC50
1A9 cells:0.091 μg/mL (ED50)|A172 cells:2.31 μM|20S proteasome:2.5 μM
In Vivo
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. 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.
In Vitro
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. 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.
Cell Research
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)

Storage & Handling

Storage-20°C
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

Tripterin, Tripterine, Proteasome, inhibit, Mitochondrial Autophagy, Mitophagy, Endogenous Metabolite, Inhibitor, 20S proteasome, Autophagy, Apoptosis, Celastrol

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Key Properties

No computed properties available.

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Celastrol (orb1304608)

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5 mg
¥ 2,210.00
25 mg
¥ 4,550.00
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