Cell permeable triterpenoid; anti-inflammatory and immunosuppressive compound. Antioxidant. Suppresses LPS-induced cytokine release in macrophages and monocytes (IC50=40nM for IL-1β and IL-1α, 80nM for IL-6, 110nM for prostaglandin E2 and 210nM for IL-8 and TNF-α). Suppresses nitric oxide (NO) production (IC50=230nM) and LPS-induced NF-κB activation (IC50=270nM). Inhibits chymotrypsin-like activity of 20S proteasome (IC50=2.5µM). Inhibits lipid peroxidation induced by ADP and Fe2+ in rat liver mitochondria (IC50=7µM). Induces expression of a wider set of heat shock proteins. Inhibits topoisomerase II.
Product Details
| Alternative Name: | Tripterine, 3-Hydroxy-24-nor-2-oxo-1(10),3,5,7-friedelatetraen-29-oic acid |
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| Formula: | C29H38O4 |
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| MW: | 450.6 |
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| Source: | Isolated from the root of Tripterygium sp. |
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| CAS: | 34157-83-0 |
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| MI: | 14: 10370 |
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| Purity: | ≥98% (HPLC) |
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| Appearance: | Red cubic crystals. |
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| Solubility: | Soluble in 100% ethanol, DMSO or dimethyl formamide; insoluble in water. |
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| Shipping: | Ambient Temperature |
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| Long Term Storage: | -20°C |
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| Handling: | Protect from light. |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
Cannabis sativa Extract Induces Apoptosis in Human Pancreatic 3D Cancer Models: Importance of Major Antioxidant Molecules Present Therein: F. Emhemmed, et al.; Molecules
27, 1214 (2022),
Abstract;
Phenotype-specific apoptosis induced by three new triterpenoid saponins from Albizia glaberrima (Schumach. & Thonn.) Benth: O.P. Noté, et al.; Fitoterapia
109, 80 (2015),
Application(s): Used as a positive control,
Abstract;
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: G. Sethi, et al.; Blood
109, 2727 (2007),
Abstract;
Induction of heat shock proteins in differentiated human and rodent neurons by celastrol: A.M. Chow & I.R. Brown; Cell Stress Chaperones
12, 237 (2007),
Abstract;
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: H. Yang, et al.; Cancer Res.
66, 4758 (2006),
Abstract;
Full Text
Tripterine inhibits the expression of adhesion molecules in activated endothelial cells: D. H. Zhang, et al.; J. Leukoc. Biol.
80, 309 (2006),
Abstract;
Full Text
Celastrol blocks neuronal cell death and extends life in transgenic mouse model of amyotrophic lateral sclerosis: M. Kiaei, et al.; Neurodegener. Dis.
2, 246 (2005),
Abstract;
Celastrol protects against MPTP- and 3-nitropropionic acid-induced neurotoxicity: C. Cleren, et al.; J. Neurochem.
94, 995 (2005),
Abstract;
Celastrol inhibits pro-inflammatory cytokine secretion in Crohn’s disease biopsies: G.F. Pinna, et al.; BBRC
322, 778 (2004),
Abstract;
Celastrols as inducers of the heat shock response and cytoprotection: S.D. Westerheide, et al.; J. Biol. Chem.
279, 56053 (2004),
Abstract;
Full Text
Apoptosis induction in HL-60 cells and inhibition of topoisomerase II by triterpene celastrol: M. Nagase, et al.; Biosci. Biotechnol. Biochem.
67, 1883 (2003),
Abstract;
Full Text
Antiinflammatory constituents of Celastrus orbiculatus inhibit the NF-kappaB activation and NO production: H.Z. Jin, et al.; J. Nat. Prod.
65, 89 (2002),
Abstract;
Celastrol, a potent antioxidant and anti-inflammatory drug, as a possible treatment for Alzheimer’s disease: A.C. Allison, et al.; Prog. Neuropsychopharmacol. Biol. Psychiatry
25, 1341 (2001),
Abstract;
Novel cytokine release inhibitors. Part III: Truncated analogs of tripterine: W. He, et al.; Bioorg. Med. Chem. Lett.
8, 3659 (1998),
Abstract;
Structural basis of potent antiperoxidation activity of the triterpene celastrol in mitochondria: effect of negative membrane surface charge on lipid peroxidation: H. Sassa, et al.; Free Radic. Biol. Med.
17, 201 (1994),
Abstract;
The triterpene celastrol as a very potent inhibitor of lipid peroxidation in mitochondria: H. Sassa, et al.; BBRC
172, 890 (1990),
Abstract;
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