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Tripterin

Catalog No. T3028 CAS 34157-83-0

Synonyms: Celastrol, Tripterine

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.

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Tripterin, CAS 34157-83-0

Pack Size	Availability	Price/USD
5 mg	In stock	$ 46.00
10 mg	In stock	$ 72.00
25 mg	In stock	$ 100.00
50 mg	In stock	$ 126.00
100 mg	In stock	$ 171.00
1 mL * 10 mM (in DMSO)	In stock	$ 56.00

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Purity: 99.8%

Purity: 99.58%

Purity: 99.48%

Biological Description

Chemical Properties

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Description	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.
Targets&IC50	20S proteasome:2.5 μM
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. [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]
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. [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]
Kinase Assay	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.
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)
Source	Natural Products > Celastraceae > Celastrus

Synonyms	Celastrol, Tripterine
Molecular Weight	450.61
Formula	C29H38O4
CAS No.	34157-83-0

Storage

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

Solubility Information

DMSO: 45.1 mg/mL (100 mM)

Ethanol: 33.8 mg/mL (75 mM)

References and Literature

1. Yang H, et al. Celastrol, a triterpene extracted from the Chinese "Thunder of God Vine," is a potent proteasome inhibitor and suppresses human prostate cancer growth in nude mice. Cancer Res. 2006 May 1;66(9):4758-65. 2. Sethi G, et al. Celastrol, a novel triterpene, potentiates TNF-induced apoptosis and suppresses invasion of tumor cells by inhibiting NF-kappaB-regulated gene products and TAK1-mediated NF-kappaB activation. Blood. 2007 Apr 1;109(7):2727-35. 3. Kim NH, et al. Celastrol suppresses the growth of vestibular schwannoma in mice by promoting the degradation of β-catenin. Acta Pharmacol Sin. 2022 Nov;43(11):2993-3001. 4. Kannaiyan R, et al. Apoptosis, 2011, 16(10), 1028-1041. 5. Liu Q, Yue Y, Wang S, et al. Celastrol Attenuates the Remodeling of Pulmonary Vascular and Right Ventricular in Monocrotaline-Induced Pulmonary Arterial Hypertension in Rats[J]. 2021 6. Jiang X, Chen S, Zhang Q, et al. Celastrol is a novel selective agonist of cannabinoid receptor 2 with anti-inflammatory and anti-fibrotic activity in a mouse model of systemic sclerosis[J]. Phytomedicine. 2019: 153160.

Citations

1. Qing T, Yan L, Wang S, et al.Celastrol alleviates oxidative stress induced by multi-walled carbon nanotubes through the Keap1/Nrf2/HO-1 signaling pathway.Ecotoxicology and Environmental Safety.2023, 252: 114623. 2. Zhang H, Cai J, Li C, et al.Wogonin inhibits latent HIV-1 reactivation by downregulating histone crotonylation.Phytomedicine.2023: 154855. 3. Zhao W, Xu C, Peng L, et al.cAMP/PKA signaling promotes AKT deactivation by reducing CIP2A expression, thereby facilitating decidualization.Molecular and Cellular Endocrinology.2023: 111946. 4. Li S, Hao L, Hu X, et al.A systematic study on the treatment of hepatitis B-related hepatocellular carcinoma with drugs based on bioinformatics and key target reverse network pharmacology and experimental verification.Infectious Agents and Cancer.2023, 18(1): 41. 5. Liu X, Hu Q, Wang W, et al. A protein-fragment complementation assay reveals that celastrol and gambogic acid suppress ERα mutants in breast cancer. Biochemical Pharmacology. 2021, 188: 114583. 6. Jiang X, Chen S, Zhang Q, et al. Celastrol is a novel selective agonist of cannabinoid receptor 2 with anti-inflammatory and anti-fibrotic activity in a mouse model of systemic sclerosis. Phytomedicine. 2019: 153160 7. Liu Q, Yue Y, Wang S, et al. Celastrol Attenuates the Remodeling of Pulmonary Vascular and Right Ventricular in Monocrotaline-Induced Pulmonary Arterial Hypertension in Rats. Cardiovascular Diagnosis and Therapy. 2022 Feb;12(1):88-102. doi: 10.21037/cdt-21-360.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Traditional Chinese Medicine Monomer Library Inhibitor Library Oxidation-Reduction Compound Library Toxic Compound Library Mitochondria-Targeted Compound Library Anti-Fibrosis Compound Library Autophagy Compound Library Anti-Metabolism Disease Compound Library Natural Product Library

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Keywords

Tripterin 34157-83-0 Apoptosis Autophagy Proteases/Proteasome Ubiquitination Mitophagy Proteasome Celastrol inhibit Tripterine Endogenous Metabolite Mitochondrial Autophagy Inhibitor inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.