ALEXIS Biochemicals: Celastrol

ALX-350-332

Revised 03-Apr-08

Celastrol
SYNONYMS	Tripterine 3-Hydroxy-24-nor-2-oxo-1(10),3,5,7-friedelatetraen-29-oic acid
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Natural Products - Anti-inflammatory Agents

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-350-332-M005		5 mg	65.00 USD
ALX-350-332-M025		25 mg	260.00 USD

Product Specification

FORMULA:	C₂₉H₃₈O₄
MW:	450.6
CAS NUMBER:	34157-83-0
SOURCE/HOST:	Isolated from the root of Tripterygium sp.
PURITY:	≥98% (HPLC)
APPEARANCE:	Red cubic crystals.
SOLUBILITY:	Soluble in 100% ethanol, DMSO or dimethyl formamide; insoluble in water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Protect from light.

Product Description

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 topoisomerse II.

Product Specific Literature References

The triterpene celastrol as a very potent inhibitor of lipid peroxidation in mitochondria: H. Sassa, et al.; BBRC 172, 890 (1990) 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
Novel cytokine release inhibitors. Part III: Truncated analogs of tripterine: W. He, et al.; Bioorg. Med. Chem. Lett. 8, 3659 (1998) 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
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
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
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
Celastrol protects against MPTP- and 3-nitropropionic acid-induced neurotoxicity: C. Cleren, et al.; J. Neurochem. 94, 995 (2005) Abstract
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, 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
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

Further Categories Containing This Product:

NF-kB Pathway Inhibitors • Natural Products - Nitric Oxide Pathway Modulators • Stress & Heat Shock Proteins Other Products • Natural Products - Immunomodulators • Natural Products - Topoisomerase Inhibitors • Ubiquitin & Proteasome Other Products • Natural Products - Antioxidants