Tripterin

SKU: orb1304608

Description

Tripterin

Research Area

Cell Biology, Metabolism Research, Protein Biochemistry

Key Properties

• CAS Number: 34157-83-0
• MW: 450.61
• Purity: 99.74%
• Formula: C₂₉H₃₈O₄
• SMILES: CC1=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
• Target: Proteasome,Autophagy,Endogenous Metabolite,Apoptosis,Mitophagy
• Solubility: Ethanol:33.8 mg/mL (75.01 mM);DMSO:250 mg/mL (554.8 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4.51 mg/mL (10.01 mM)

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 inhibite 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 induce 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 b the MTT uptake method. Briefly, × 0^3 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 ℃, an the optical density is then measured at 570 nM using a Tecan plate reader.(Only for Reference)

Storage & Handling

• Storage: keep away from direct sunlight,keep away from moisture,The compound is unstable in solution. Please use soon | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

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

Compound Identifiers

PubChem CID

122724