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Fatty Acid Synthase [FAS] / Related Products
You are here: Product Lines > Obesity & Adipokines > Lipid Metabolism / Related Products > Fatty Acid Synthase [FAS] / Related Products
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ALX-270-286 Revised 18-Sep-07
C75
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SYNONYMS trans-4-Carboxy-5-octyl-3-methylene-butyrolactone
PRODUCT LINE Obesity & Adipokines
PRODUCT CATEGORY Fatty Acid Synthase [FAS] / Related Products
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ALX-270-286-M001   1 mg 65.00 USD Add To Cart
ALX-270-286-M005   5 mg 240.00 USD Add To Cart
Product Specification
FORMULA: C14H22O4
MW: 254.3
CAS NUMBER: 191282-48-1
SOURCE/HOST: Synthetic.
PURITY: ≥98%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in dichloromethane, methanol or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: HARMFUL.

Product Description
Inhibitor of fatty acid synthase (FAS) reducing food intake and body weight in mice. Exhibits irreversible slow-binding biphasic inactivation of fatty acid synthase. Downregulates neuropeptide Y and Agouti-related protein expression. Has been proposed to activate CPT-1 activity in liver and adipose tissue, leading to increased fatty acid oxidation and energy production. Shows significant in vivo antitumor activity in human breast cancer cells. Suppresses DNA replication and induces apoptosis. FAS inhibition by C75 leads to a dramatic accumulation of the CDK inhibitor p27KIP1 from cytosol to cell nuclei.
Product Specific Literature References
Pharmacological inhibitors of mammalian fatty acid synthase suppress DNA replication and induce apoptosis in tumor cell lines: E.S. Pizer, et al.; Cancer Res. 58, 4611 (1998) Abstract
Synthesis and antitumor activity of an inhibitor of fatty acid synthase: F.P. Kuhajda, et al.; PNAS 97, 3450 (2000) Abstract
Reduced food intake and body weight in mice treated with fatty acid synthase inhibitors: T.M. Loftus, et al.; Science 288, 2379 (2000) Abstract
Malonyl-coenzyme-A is a potential mediator of cytotoxicity induced by fatty-acid synthase inhibition in human breast cancer cells and xenografts: E.S. Pizer, et al.; Cancer Res. 60, 213 (2000) Abstract
Increased fatty acid synthase is a therapeutic target in mesothelioma: E.W. Gabrielson, et al.; Clin. Cancer Res. 7, 153 (2001) Abstract
Pharmacological inhibition of fatty acid synthase activity produces both cytostatic and cytotoxic effects modulated by p53: J.N. Li, et al.; Cancer Res. 61, 1493 (2001) Abstract
Green tea epigallocatechin gallate: a natural inhibitor of fatty-acid synthase: X. Wang & W. Tian; BBRC 288, 1200 (2001) Abstract
Comparison of central and peripheral administration of c75 on food intake, body weight, and conditioned taste aversion: D.J. Clegg, et al.; Diabetes 51, 3196 (2002) Abstract
Expression of FAS within hypothalamic neurons: a model for decreased food intake after C75 treatment: E.K. Kim, et al.; Am. J. Physiol. Endocrinol. Metab. 283, E867 (2002) Abstract
Differential effects of a centrally acting fatty acid synthase inhibitor in lean and obese mice: M.V. Kumar, et al.; PNAS 99, 1921 (2002) Abstract; Full Text
Effect of a fatty acid synthase inhibitor on food intake and expression of hypothalamic neuropeptides: T. Shimokawa, et al.; PNAS 99, 66 (2002) Abstract
C75 increases peripheral energy utilization and fatty acid oxidation in diet-induced obesity: J.N. Thupari, et al.; PNAS 99, 9498 (2002) Abstract
Effect of the anorectic fatty acid synthase inhibitor C75 on neuronal activity in the hypothalamus and brainstem: S. Gao and M.D. Lane; PNAS 100, 10 (2003) Abstract
Hypothalamic malonyl-CoA as a mediator of feeding behavior: Z. Hu, et al.; PNAS 100, 12624 (2003) Abstract
C75 inhibits food intake by increasing CNS glucose metabolism: M.D. Wortman, et al.; Nat. Med. 9, 483 (2003) Abstract
Fatty Acid Synthase Inhibition Triggers Apoptosis during S Phase in Human Cancer Cells: W. Zhou, et al.; Cancer Res. 63, 7330 (2003) Abstract
Long-term effects of a fatty acid synthase inhibitor on obese mice: food intake, hypothalamic neuropeptides, and UCP3: S.H. Cha, et al.; BBRC 317, 301 (2004) Abstract
C75, a fatty acid synthase inhibitor, modulates AMP-activated protein kinase to alter neuronal energy metabolism: L.E. Landree, et al.; J. Biol. Chem. 279, 3817 (2004) Abstract
Inhibition of tumor-associated fatty acid synthase activity antagonizes estradiol- and tamoxifen-induced agonist transactivation of estrogen receptor (ER) in human endometrial adenocarcinoma cells: J.A. Menendez, et al.; Oncogene 23, 4945 (2004) Abstract
C75 activates malonyl-CoA sensitive and insensitive components of the CPT system: C. Nicot, et al.; BBRC 325, 660 (2004) Abstract
The anorexigenic fatty acid synthase inhibitor, C75, is a non-specific neuronal activator: K.A. Takahashi, et al.; Endocrinology 145, 184 (2004) Abstract
 
 
ALX-380-053 Revised 19-Jun-08
Cerulenin
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SYNONYMS 2,3-Epoxy-4-oxo-7,10-dodecadienamide
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Apoptosis Inducers & Inhibitors
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ALX-380-053-M005   5 mg 60.00 USD Add To Cart
ALX-380-053-M010   10 mg 110.00 USD Add To Cart
ALX-380-053-M050   50 mg 420.00 USD Add To Cart
Product Specification
FORMULA: C12H17NO3
MW: 223.3
CAS NUMBER: 17397-89-6
MERCK INDEX: 14: 2004
RTECS: JR1670000
SOURCE/HOST: Isolated from Cephalosporium caerulens.
PURITY: ≥98%
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO, dimethyl formamide, dichloromethane, methanol, 100% ethanol or acetone; slighly soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.
HAZARD: HARMFUL.

Product Description
Antibiotic. Fatty acid synthase (FAS) inhibitor reported to bind in equimolar ratio to β-keto-acyl-ACP synthase, thus inhibiting protein acylation. Produces metabolic effects similar to effects of leptin, but through mechanisms that are independent of, or down-stream from, both leptin and melanocortin receptors. Apoptosis inducer. Inhibitor of bacterial fatty acid synthesis (inhibits FabH, FabB and FabF condensation enzymes).
Product Specific Literature References
Studies on cerulenin, 3. Isolation and physico-chemical properties of cerulenin: Y. Sato, et al.; J. Antibiot. (Tokyo) 200, 344 (1967) Abstract
Effect of cerulenin on the synthesis of very-long-chain fatty acids in microsomes from leek seedlings: F. Schneider, et al.; Biochim. Biophys. Acta 1152, 243 (1993) Abstract
Cerulenin-resistant mutants of Saccharomyces cerevisiae with an altered fatty acid synthase gene: J. Inokashi, et al.; Mol. Gen. Genet. 244, 90 (1994) Abstract
Cerulenin mimics effects of leptin on metabolic rate, food intake, and body weight independent of the melanocortin system, but unlike leptin, cerulenin fails to block neuroendocrine effects of fasting: H. Makimura, et al.; Diabetes 50, 733 (2001) Abstract; Full Text
Key role of mitochondria in cerulenin-mediated apoptosis: S.J. Heiligtag, et al.; Cell Death Differ. 9, 1017 (2002) Abstract
Fatty acid synthase inhibitors cerulenin and C75 retard growth and induce caspase-dependent apoptosis in human melanoma A-375 cells: T.S. Ho, et al.; Biomed. Pharmacother. 61, 578 (2007) Abstract
Further Categories Containing This Product:
Fatty Acid Synthase [FAS] / Related Products
 
 
ALX-270-263 Revised 03-Apr-08
(-)-Epigallocatechin gallate
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SYNONYMS EGCG
(2R,3R)-2-(3,4,5-Trihydroxyphenyl)-3,4-dihydro-1[2H]-benzopyran-3,5,7-triol 3-(3,4,5-trihydroxybenzoate)
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antioxidants
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-263-M010   10 mg 20.00 USD Add To Cart
ALX-270-263-M050   50 mg 60.00 USD Add To Cart
Product Specification
FORMULA: C22H18O11
MW: 458.4
CAS NUMBER: 989-51-5
MERCK INDEX: 14: 3526
SOURCE/HOST: Isolated from green tea.
PURITY: ≥98% (HPLC)
APPEARANCE: Off-white to yellow powder.
SOLUBILITY: Soluble in 100% ethanol, dimethyl formamide or DMSO; slightly soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Stock solutions in DMSO are stable for up to 3 months when stored at -20°C.
HANDLING: After reconstitution, prepare aliquots and store at -20°C. Keep under inert gas. Protect from light.

Product Description
Antitumor reagent. Antioxidant. Protects cells from lipid peroxidation and DNA damage induced by reactive free radicals. Inhibits inducible nitric oxide synthase (iNOS; NOS II). Chemopreventive anticancer agent. Induces apoptosis in human cancer cell lines. Inhibits MAP kinase mediated signalling pathways. Inhibits angiogenesis. Inhibits telomerase and DNA methyltransferase. Anti-inflammatory agent.
Product Specific Literature References
Inhibitory effect of topical application of a green tea polyphenol fraction on tumor initiation and promotion in mouse skin: M.T. Huang, et al.; Carcinogenesis 13, 947 (1992) Abstract
Inhibition of 12-O-tetradecanoylphorbol-13-acetate and other skin tumor-promoter-caused induction of epidermal interleukin-1 alpha mRNA and protein expression in SENCAR mice by green tea polyphenols: S.K. Katiyar, et al.; J. Invest. Dermatol. 105, 394 (1995) Abstract
Growth inhibition and regression of human prostate and breast tumors in athymic mice by tea epigallocatechin gallate: S. Liao, et al.; Cancer Lett. 96, 239 (1995) Abstract
Inhibition of N-methyl-N'-nitro-N-nitrosoguanidine-induced carcinogenesis by (-)-epigallocatechin gallate in the rat glandular stomach: T. Yamane, et al.; Cancer Res. 55, 2081 (1995) Abstract
(-)-Epigallocatechin gallate, a polyphenolic tea antioxidant, inhibits peroxynitrite-mediated formation of 8-oxodeoxyguanosine and 3-nitrotyrosine: E.S. Fiala, et al.; Experientia 52, 922 (1996) Abstract
Green tea constituent epigallocatechin-3-gallate and induction of apoptosis and cell cycle arrest in human carcinoma cells: N. Ahmad, et al.; J. Natl. Cancer Inst. 89, 1881 (1997) Abstract
Inhibition of inducible nitric oxide synthase gene expression and enzyme activity by epigallocatechin gallate, a natural product from green tea: M.M. Chan, et al.; Biochem. Pharmacol. 54, 1281 (1997) Abstract
(-)-Epigallocatechin-3-gallate blocks the induction of nitric oxide synthase by down-regulating lipopolysaccharide-induced activity of transcription factor nuclear factor-kappaB: Y.L. Lin & J.K. Lin; Mol. Pharmacol. 52, 465 (1997) Abstract
Telomerase inhibition, telomere shortening, and senescence of cancer cells by tea catechins: I. Naasani, et al.; BBRC 249, 391 (1998) Abstract
Epigallocatechin suppression of proliferation of vascular smooth muscle cells: correlation with c-jun and JNK: L.H. Lu, et al.; Br. J. Pharmacol. 124, 1227 (1998) Abstract
ESR study on the structure-antioxidant activity relationship of tea catechins and their epimers: Q. Guo, et al.; Biochim. Biophys. Acta 1427, 13 (1999) Abstract
Pharmacokinetics of the green tea derivative, EGCG, by the topical route of administration in mouse and human skin: K. Dvorakova, et al.; Cancer Chemother. Pharmacol. 43, 331 (1999) Abstract
Polyphenolic antioxidant (-)-epigallocatechin-3-gallate from green tea reduces UVB-induced inflammatory responses and infiltration of leukocytes in human skin: S.K. Katiyar, et al.; Photochem. Photobiol. 69, 148 (1999) Abstract
Antioxidant chemistry of green tea catechins. Identification of products of the reaction of (-)-epigallocatechin gallate with peroxyl radicals: S. Valcic, et al.; Chem. Res. Toxicol. 12, 382 (1999) Abstract
Antimutagenic and anticarcinogenic activity of tea polyphenols: Y. Kuroda & Y. Hara; Mutat. Res. 436, 69 (1999) Abstract
Inhibitory effect of green and black tea on tumor growth: A.H. Conney, et al.; Proc. Soc. Exp. Biol. Med. 220, 229 (1999) Abstract
Green tea epigallocatechin gallate: a natural inhibitor of fatty-acid synthase: X. Wang & W. Tian; BBRC 288, 1200 (2001) Abstract
Epigallocatechin gallate, a constituent of green tea, represses hepatic glucose production: M.E. Waltner-Law, et al.; J. Biol. Chem. 277, 34933 (2002) Abstract; Full Text
The specificities of protein kinase inhibitors: an update:: J. Bain, et al.; Biochem. J. 371, 199 (2003) Abstract; Full Text
Selective inhibition of ADAMTS-1, -4 and -5 by catechin gallate esters: M.N. Vankemmelbeke, et al.; Eur. J. Biochem. 270, 2394 (2003) Abstract
Epigallocatechin-3-gallate, constituent of green tea, suppresses the LPS-induced phenotypic and functional maturation of murine dendritic cells through inhibition of mitogen-activated protein kinases and NF-kappaB: S.C. Ahn, et al.; BBRC 313, 148 (2004) Abstract
Epigallocatechin-3-gallate inhibits epidermal growth factor receptor signaling pathway. Evidence for direct inhibition of ERK1/2 and AKT kinases: J.F. Sah, et al.; J. Biol. Chem. 279, 12755 (2004) Abstract
Inhibition of c-Jun NH2-terminal kinase activity improves ischemia/reperfusion injury in rat lungs: M. Ishii, et al.; J. Immunol. 172, 2569 (2004) Abstract
A constituent of green tea, epigallocatechin-3-gallate, activates endothelial nitric oxide synthase by a phosphatidylinositol-3-OH-kinase-, cAMP-dependent protein kinase-, and Akt-dependent pathway and leads to endothelial-dependent vasorelaxation: M. Lorenz, et al.; J. Biol. Chem. 279, 6190 (2004) Abstract; Full Text
Green tea polyphenols prevent toxin-induced hepatotoxicity in mice by down-regulating inducible nitric oxide-derived prooxidants: J.H. Chen, et al.; Am. J. Clin. Nutr. 80, 742 (2004) Abstract; Full Text
Neuroprotective effects of (-)-epigallocatechin gallate following hypoxia-ischemia-induced brain damage: novel mechanisms of action: B.A. Sutherland, et al.; FASEB J. 19, 258 (2005) Abstract; Full Text
Tea flavanols inhibit angiotensin-converting enzyme activity and increase nitric oxide production in human endothelial cells: I.A. Persson, et al.; J. Pharm. Pharmacol. 58, 1139 (2006) Abstract
General Literature References
Anticarcinogenic effects of (-)-epigallocatechin gallate: H. Fujiki, et al.; Prev. Med. 21, 503 (1992), (Review) Abstract
Absorption, metabolism and antioxidative effects of tea catechin in humans: T. Miyazawa; Biofactors 13, 55 (2000), (Review) Abstract
Inhibition of tumour invasion and angiogenesis by epigallocatechin gallate (EGCG), a major component of green tea: Y.D. Jung and L.M. Ellis; Int. J. Exp. Pathol. 82, 309 (2001), (Review) Abstract
Anti-invasive effects of green tea polyphenol epigallocatechin-3-gallate (EGCG), a natural inhibitor of metallo and serine proteases: R. Benelli, et al.; Biol. Chem. 383, 101 (2002), (Review) Abstract
 
 
ALX-385-005 Revised 21-May-08
Kaempferol
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SYNONYMS 3,4',5,7-Tetrahydroxyflavone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Flavonols
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ALX-385-005-M010   10 mg 40.00 USD Add To Cart
ALX-385-005-M050   50 mg 120.00 USD Add To Cart
Product Specification
FORMULA: C15H10O6
MW: 286.2
CAS NUMBER: 520-18-3
MERCK INDEX: 14: 5274
RTECS: LK9275200
PURITY: ≥90%
APPEARANCE: Yellow powder.
SOLUBILITY: Soluble in ether or 100% ethanol (hot); slightly soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.
HAZARD: IRRITANT. MAY BE MUTAGENIC.

Product Description
Antioxidant flavonoid. Apoptosis inducer. Reversible inhibitor of fatty acid synthase (FAS).
Product Specific Literature References
Structure-antioxidant activity relationships of flavonoids and phenolic acids: C.A. Rice-Evans, et al.; Free Radical Biol. & Med. 20, 933 (1996), (Review) Abstract
Presence of fatty acid synthase inhibitors in the rhizome of Alpinia officinarum hance: B.H. Li & W.X. Tian; J. Enzyme Inhib. Med. Chem. 18, 349 (2003) Abstract
Pharmacological inhibitors of Fatty Acid Synthase (FASN)--catalyzed endogenous fatty acid biogenesis: a new family of anti-cancer agents?: R. Lupu & J. A. Menendez; Curr. Pharm. Biotechnol. 7, 483 (2006), (Review) Abstract
 
 
ALX-385-007 Revised 07-Oct-08
Luteolin
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SYNONYMS 3',4',5,7-Tetrahydroxyflavone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Flavones
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-385-007-M010   10 mg 15.00 USD Add To Cart
ALX-385-007-M050   50 mg 45.00 USD Add To Cart
Product Specification
FORMULA: C15H10O6
MW: 286.2
CAS NUMBER: 491-70-3
MERCK INDEX: 14: 5614
RTECS: LK9275210
PURITY: ≥90%
APPEARANCE: Yellow powder.
SOLUBILITY: Soluble in methanol, alkaline solutions; slightly soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C

Product Description
Antioxidant flavonoid. Inhibits VEGF-induced angiogenesis. Inhibitor of phosphoinositide 3-kinase (PI(3)K). Inhibitor of fatty acid synthase (FAS). Apoptosis inducer.
Product Specific Literature References
Structure-antioxidant activity relationships of flavonoids and phenolic acids: C.A. Rice-Evans, et al.; Free Radical Biol. & Med. 20, 933 (1996), (Review) Abstract
Luteolin inhibits vascular endothelial growth factor-induced angiogenesis; inhibition of endothelial cell survival and proliferation by targeting phosphatidylinositol 3'-kinase activity: E. Bagli, et al.; Cancer Res. 64, 7936 (2004)
Dietary flavonoids: bioavailability, metabolic effects, and safety: J.A. Ross & C.M. Kasum; Annu. Rev. Nutr. 221, 19 (2002), (Review) Abstract
Pharmacological inhibitors of Fatty Acid Synthase (FASN)--catalyzed endogenous fatty acid biogenesis: a new family of anti-cancer agents?: R. Lupu & J. A. Menendez; Curr. Pharm. Biotechnol. 7, 483 (2006), (Review) Abstract
 
 
ALX-350-152 Revised 20-Jun-08
Orlistat
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SYNONYMS Tetrahydrolipstatin
N-Formyl-L-leucine-(1S)-1-(((2S,3S)-3-hexyl-4-oxo-2-oxetanyl)methyl)dodecyl ester
PRODUCT LINE Obesity & Adipokines
PRODUCT CATEGORY Fatty Acid Synthase [FAS] / Related Products
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-152-M050   50 mg 40.00 USD Add To Cart
ALX-350-152-M250   250 mg 120.00 USD Add To Cart
Product Specification
FORMULA: C29H53NO5
MW: 495.7
CAS NUMBER: 96829-58-2
MERCK INDEX: 14: 6869
SOURCE/HOST: Synthetic. Originally isolated from Streptomyces sp.
PURITY: ≥97%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stock solutions are stable for up to 6 weeks when stored at -20°C.
HANDLING: After reconstitution, prepare aliquots and store at -20°C. Protect from light and moisture.

Product Description
Cell permeable, irreversible inhibitor of gastric and pancreatic lipases. Shows only minimal activity against amylase, trypsin, chymotrypsin, or phospholipase A2 (PLA2). Partially inhibits the hydrolysis of triglycerides and lowers the absorption of dietary fat and promotes weight loss. Anti-obesity drug. Exhibits antitumor activity by inhibition of the thioesterase domain of fatty acid synthase (FAS) both in vitro and in vivo.
Product Specific Literature References
Interactions of lipoprotein lipase with the active-site inhibitor tetrahydrolipstatin (Orlistat): A. Lookene, et al.; Eur. J. Biochem. 222, 395 (1994) Abstract
Degree of in vivo inhibition of human gastric and pancreatic lipases by Orlistat (Tetrahydrolipstatin, THL) in the stomach and small intestine: B. Sternby, et al.; Clin. Nutr. 21, 395 (2002) Abstract
A fatty acid synthase blockade induces tumor cell-cycle arrest by down-regulating Skp2: L.M. Knowles, et al.; J. Biol. Chem. 279, 30540 (2004) Abstract; Full Text
Orlistat is a novel inhibitor of fatty acid synthase with antitumor activity: S.J. Kridel, et al.; Cancer Res. 64, 2070 (2004) Abstract
Antitumoral actions of the anti-obesity drug orlistat (XenicalTM) in breast cancer cells: blockade of cell cycle progression, promotion of apoptotic cell death and PEA3-mediated transcriptional repression of Her2/neu (erbB-2) oncogene: J.A. Menendez, et al.; Ann. Oncol. 16, 1253 (2005) Abstract
Differential uptake of subfractions of triglyceride-rich lipoproteins by THP-1 macrophages: A.M. Palmer, et al.; Atherosclerosis 180, 233 (2005) Abstract
Orlistat and sibutramine beyond weight loss: E. Mannucci, et al.; Nutr. Metab. Cardiovasc. Dis. 70, 1228 (2008) Abstract
Further Categories Containing This Product:
Natural Products - Antitumor ReagentsObesity & Diabetes Other Products
 
 
ALX-385-001 Revised 08-Apr-08
Quercetin . dihydrate
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SYNONYMS 3,3',4',5,7-Pentahydroxyflavone . 2H2O
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Flavonols
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ALX-385-001-G005   5 g 15.00 USD Add To Cart
ALX-385-001-G025   25 g 45.00 USD Add To Cart
Product Specification
FORMULA: C15H10O7 . 2H2O
MW: 302.2 . 36.0
CAS NUMBER: 6151-25-3
MERCK INDEX: 14: 8034
RTECS: LK8950000
SOURCE/HOST: Isolated from Sophora japonica L.
PURITY: ≥95% (HPLC)
APPEARANCE: Yellow powder with a green or brown cast.
SOLUBILITY: Soluble in 100% ethanol or 1M sodium hydroxide; almost insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
HAZARD: MAY BE MUTAGENIC. TOXIC.

Product Description
Antioxidant flavonoid. Inhibitor of mitochondrial ATPase, cAMP- and cGMP-phosphodiesterases. Inhibitor of protein tyrosine kinases and protein kinase C (PKC). Induces apoptosis. Blocks cells at the G0/G1 interface. Activator of human deacetylase SIRT1. Reversible inhibitor of fatty acid synthase (FAS). Inhibits the production of the inflammatory mediators nitric oxide (NO), TNF-α and IL-12 in activated macrophages.
Product Specific Literature References
Effects of quercetin and F1 inhibitor on mitochondrial ATPase and energy-linked reactions in submitochondrial particles: D.R. Lang & E. Racker; Biochim. Biophys. Acta 333, 180 (1974)
Flavonoid compounds are potent inhibitors of cyclic AMP phosphodiesterase: A. Beretz, et al.; Experientia 34, 1054 (1978) Abstract
Flavonoids are selective cyclic GMP phosphodiesterase inhibitors: M. Ruckstuhl, et al.; Biochem. Pharmacol. 28, 535 (1979) Abstract
The effect of quercetin on the phosphorylation activity of the Rous sarcoma virus transforming gene product in vitro and in vivo: Y. Graziani, et al.; Eur. J. Biochem. 135, 583 (1983) Abstract
Inhibition of the calcium- and phospholipid-dependent protein kinase activity from mouse brain cytosol by quercetin: M. Gschwendt, et al.; BBRC 117, 444 (1983) Abstract
Tyrosine protein kinase activity in the DMBA-induced rat mammary tumor: inhibition by quercetin: J. Levy, et al.; BBRC 123, 1227 (1984) Abstract
The phospholipid- and calcium-dependent protein kinase as a target in tumor chemotherapy: H. Grunicke, et al.; Adv. Enzyme Regul. 28, 201 (1989) Abstract
Induction of apoptosis by quercetin: involvement of heat shock protein: Y.Q. Wei, et al.; Cancer Res. 54, 4952 (1994) Abstract
Multiple effects of tyrosine kinase inhibitors on vascular smooth muscle contraction: C.M. Filipeanu, et al.; Eur. J. Pharmacol. 281, 29 (1995) Abstract
Structure-antioxidant activity relationships of flavonoids and phenolic acids: C.A. Rice-Evans, et al.; Free Radical Biol. & Med. 20, 933 (1996), (Review)