ALEXIS Biochemicals: Celastrol

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ALX-350-298

Revised 03-Apr-08

Betulinic acid (~95%)
SYNONYMS	3β-Hydroxy-20(29)-lupaene-28-oic acid
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Natural Products - Antitumor Reagents

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-350-298-M100		100 mg	55.00 USD
ALX-350-298-M500		500 mg	180.00 USD
ALX-350-298-G001		1 g	290.00 USD

Product Specification

FORMULA:	C₃₀H₄₈O₃
MW:	456.7
CAS NUMBER:	472-15-1
SOURCE/HOST:	Isolated from Platanus acerifolia (plane tree) bark.
PURITY:	≥95% (HPLC)
APPEARANCE:	White to off-white powder.
SOLUBILITY:	Soluble in DMSO.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C

Product Description

Antitumor and anti-HIV agent. Induces apoptosis by activating mitochondrial permeability transition (MPT). Inhibits NF-κB activation and NF-κB-regulated gene expression induced by carcinogens and inflammatory stimuli. Decreases expression of Bcl-2 and cyclin D1. Potent proteasome activator.

Product Specific Literature References

Anti-AIDS agents, 11. Betulinic acid and platanic acid as anti-HIV principles from Syzigium claviflorum, and the anti-HIV activity of structurally related triterpenoids: T. Fujioka, et al.; J. Nat. Prod. 57, 243 (1994) Abstract
Discovery of betulinic acid as a selective inhibitor of human melanoma that functions by induction of apoptosis: E. Pisha, et al.; Nat. Med. 1, 1046 (1995) Abstract
Betulinic acid and dihydrobetulinic acid derivatives as potent anti-HIV agents: Y. Kashiwada, et al.; J. Med. Chem. 39, 1016 (1996) Abstract
Betulinic acid triggers CD95 (APO-1/Fas)- and p53-independent apoptosis via activation of caspases in neuroectodermal tumors: S. Fulda, et al.; Cancer Res. 57, 4956 (1997) Abstract
Anti-AIDS agents--XXVII. Synthesis and anti-HIV activity of betulinic acid and dihydrobetulinic acid derivatives: F. Hashimoto, et al.; Bioorg. Med. Chem. 5, 2133 (1997) Abstract
Betulinic acid induces apoptosis in human neuroblastoma cell lines: M.L. Schmidt, et al.; Eur. J. Cancer 33, 2007 (1997) Abstract
Induction of p53 without increase in p21WAF1 in betulinic acid-mediated cell death is preferential for human metastatic melanoma: M. Rieber & M. Strasberg Rieber; DNA Cell Biol. 17, 399 (1998) Abstract
Activation of mitochondria and release of mitochondrial apoptogenic factors by betulinic acid: S. Fulda, et al.; J. Biol. Chem. 273, 33942 (1998) Abstract; Full Text
Betulinic acid inhibits aminopeptidase N activity: M.F. Melzig & H. Bormann; Planta Med. 64, 655 (1998) Abstract
Correspondence re: S. Fulda et al., Betulinic acid triggers CD95 (Apo1/Fas)- and p53-independent apoptosis via activation of caspases in neuroectodermal tumors. Cancer Res., 57: 4956, 1997: M. Rieber & M. Strasberg Rieber; Cancer. Res. 58, 5876 (1998) Abstract
Betulinic acid: a new cytotoxic agent against malignant brain-tumor cells: S. Fulda, et al.; Int. J. Cancer 82, 435 (1999) Abstract
Betulinic acid-induced apoptosis in glioma cells: A sequential requirement for new protein synthesis, formation of reactive oxygen species, and caspase processing: W. Wick, et al.; J Pharmacol. Exp. Ther. 289, 1306 (1999) Abstract; Full Text
Effects of betulinic acid alone and in combination with irradiation in human melanoma cells: E. Selzer, et al.; J. Invest. Dermatol. 114, 935 (2000) Abstract
Betulinic acid suppresses carcinogen-induced NF-kappa B activation through inhibition of I kappa B alpha kinase and p65 phosphorylation: abrogation of cyclooxygenase-2 and matrix metalloprotease-9: Y. Takada & B.B. Aggarwal; J. Immunol. 171, 3278 (2003) Abstract
Chemistry, biological activity, and chemotherapeutic potential of betulinic acid for the prevention and treatment of cancer and HIV infection: R.H. Cichewicz & S.A. Kouzi; Med. Res. Rev. 24, 90 (2004), Review Abstract
Betulinic acid-induced apoptosis in leukemia cells: H. Ehrhardt, et al.; Leukemia 18, 1406 (2004) Abstract
Betulinic acid and its derivatives: a review on their biological properties: P. Yogeeswari & D. Sriram; Curr. Med. Chem. 12, 657 (2005), Review Abstract
Betulinic acid decreases expression of bcl-2 and cyclin D1, inhibits proliferation, migration and induces apoptosis in cancer cells: W. Rzeski, et al.; Naunyn Schmiedebergs Arch. Pharmacol. 374, 11 (2006) Abstract
Activation and inhibition of the proteasome by betulinic acid and its derivatives: L. Huang, et al.; FEBS Lett. 581, 4955 (2007) Abstract

Further Categories Containing This Product:

CDK & Cyclin Inhibitors • Other Natural Products - DNA Regulation / Transcription • Natural Products - NF-kB Pathway Inhibitors • MPTP [Mitochondrial Transition Pore] / Related Products • NF-kB Pathway Inhibitors • Antitumor Agents (Apoptosis Inducers) • Natural Products - Anti-inflammatory Agents • Natural Products - Antiviral / anti-HIV Agents • Ubiquitin & Proteasome Other Products • Natural Products - Apoptosis Inducers & Inhibitors • HIV / AIDS / Related Products

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:

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

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