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Celastrol

Anti-inflammatory and immunosuppressive
 
ALX-350-332-M005 5 mg 74.00 USD
 
ALX-350-332-M025 25 mg 267.00 USD
 
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 Specification

Alternative Name:Tripterine, 3-Hydroxy-24-nor-2-oxo-1(10),3,5,7-friedelatetraen-29-oic acid
 
Formula:C29H38O4
 
MW:450.6
 
Source:Isolated from the root of Tripterygium sp.
 
CAS:34157-83-0
 
MI:14: 10370
 
Purity:≥98% (HPLC)
 
Appearance:Red cubic crystals.
 
Solubility:Soluble in 100% ethanol, DMSO or dimethyl formamide; insoluble in water.
 
Long Term Storage:-20°C
 
Handling:Protect from light.
 
350-332
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350-332

Product Literature References

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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