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Celastrol


CAS Number: 34157-83-0

Mol. Formula: C29H38O4

Melting Point: 180-185°C

Mol. Weight: 450.61

Solubility: Soluble in 100% ethanol, DMSO or dimethyl formamide; insoluble in water.

Synonyms:
3-Hydroxy-2-oxo-24-nor-D:A-friedooleana-1(10),3,5,7-tetraen-29-oic Acid; Tripterin; (9β,13α,14β,20α)-3-Hydroxy-9,13-dimethyl-2-oxo-24,25,26-trinoroleana-1(10),3,5,7-tetraen-29-oic Acid; 

Appearance:
Orange Red Solid

Application:

A cell-permeable dienone-phenolic triterpene compound that exhibits antioxidant and anti-inflammatory properties. It suppresses LPS-induced pro-inflammatory cytokines release in macrophages and monocytes (IC50 = 40 nM for IL-1β and IL-1α, 80 nM for IL-6, 110 nM for PGE2, and 210 nM for IL-8 and TNF-α), as well as LPS-induced NF-κB activation (IC50 = 270 nM) and NO production (IC50 = 230 nM) in RAW264.7 cells. Preferentially inhibits chymotrypsin-like activity of 20S proteasome with an IC50 of 2.5 µM. Has also been shown to inhibit lipid peroxidation induced by ADP and Fe2+ in rat liver mitochondria (IC50 = 7 µM). Significantly improves the performance in memory, learning, and psychomotor activity in rats. May be useful to minimize inflammation in Alzheimer′s disease (AD).

Reference:

1.The triterpene celastrol as a very potent inhibitor of lipid peroxidation in mitochondria: H. Sassa, et al.; BBRC 172, 890 (1990), Abstract;

2.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;

3.Novel cytokine release inhibitors. Part III: Truncated analogs of tripterine: W. He, et al.; Bioorg. Med. Chem. Lett. 8, 3659 (1998), Abstract;

4.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;

5.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;

6.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

7.Celastrol inhibits pro-inflammatory cytokine secretion in Crohn’s disease biopsies: G.F. Pinna, et al.; BBRC 322, 778 (2004), Abstract;

8.Celastrols as inducers of the heat shock response and cytoprotection: S.D. Westerheide, et al.; J. Biol. Chem. 279, 56053 (2004), Abstract; Full Text

9.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;

10.Celastrol protects against MPTP- and 3-nitropropionic acid-induced neurotoxicity: C. Cleren, et al.; J. Neurochem. 94, 995 (2005), Abstract;

11.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

12.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;

13.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;

The product is only for R&D purpose,not for human use.We will not take any responsibility for illegal use.

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