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DNA Regulation / Transcription
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ALX-480-027 Revised 25-Jun-08
8-Bromoguanosine 3',5'-cyclic Monophosphothioate, Sp-Isomer . sodium salt (high purity)
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SYNONYMS Sp-8-Br-cGMPS . Na
8-Br-cGMPS . Na, Sp-isomer
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY cGMP Derivatives
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-480-027-M001   1 mg 80.00 USD Add To Cart
ALX-480-027-M005   5 mg 320.00 USD Add To Cart
Product Specification
FORMULA: C10H10BrN5O6PS . Na
MW: 439.2 . 23.0
CAS NUMBER: 153660-03-8
PURITY: ≥99% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
IDENTITY: Identity determined by MS, 1H-NMR and UV.

Product Description
Unspecific activator of both cGMP-dependent protein kinase (PKG) 1α and cAMP-dependent protein kinase (PKA). Resistant to cyclic nucleotide phosphodiesterases. Much more lipophilic and membrane permeant as compared to cyclic GMP (Prod. No. ALX-480-059) or Sp-cGMPS (Prod. No. ALX-480-073).
Product Specific Literature References
Evidence for two intracellular calcium pools in Dictyostelium: the cAMP- induced calcium influx is directed into a NBD-Cl- and 2,5-di-(tert- butyl)1,4-hydroquinone-sensitive pool: H. Flaadt, et al.; J. Cell Sci. 105, 1131 (1993) Abstract
Further Categories Containing This Product:
PKG ActivatorsPKA Activators
 
 
ALX-350-246 Revised 07-Mar-08
Butein
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SYNONYMS 2',3,4,4'-Tetrahydroxychalcone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-246-M010   10 mg 190.00 USD Add To Cart
Product Specification
FORMULA: C15H12O5
MW: 272.3
CAS NUMBER: 487-52-5
PURITY: ≥98% (HPLC)
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO (>50mg/ml) or methanol; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light. Keep cool and dry under inert gas.
IDENTITY: Identity determined by 1H-NMR, 13C-NMR and MS.

Product Description
Plant polyphenol that acts as a specific tyrosine kinase inhibitor. Potently inhibits the tyrosine kinase activity of the EGF receptor and p60c-src. Potent antioxidant and anti-inflammatory agent. Inhibits glutathione reductase and rat liver glutathione S-transferase. Activator of human deacetylase SIRT1. Inhibits aromatase, showing chemopreventive properties. Directly inhibits IKK.
Product Specific Literature References
Inhibition of 12-O-tetradecanoylphorbol-13-acetate-mediated epidermal ornithine decarboxylase induction and skin tumor promotion by new lipoxygenase inhibitors lacking protein kinase C inhibitory effects: E. Aizu, et al.; Carcinogenesis 7, 1809 (1986) Abstract
Protective effects of hydroxychalcones on free radical-induced cell damage: S. Sogawa, et al.; Biol. Pharm. Bull. 17, 251 (1994) Abstract
Cytotoxic effect of butein on human colon adenocarcinoma cell proliferation: C.C. Yit & N.P. Das; Cancer Lett. 82, 65 (1994) Abstract
Inhibitory effects of plant polyphenols on rat liver glutathione S-transferase: K. Zhang & N.P. Das; Biochem. Pharmacol. 47, 2063 (1994) Abstract
Endothelium-dependent relaxation of rat aorta by butein, a novel cyclic AMP-specific phosphodiesterase inhibitor: S.M. Yu, et al.; Eur. J. Pharmacol. 280, 69 (1995) Abstract
Butein (3,4,2',4'-tetrahydroxychalcone) ameliorates experimantal anti-glomerular basement membrane antibody-associated glomerulonephritis (3): K. Hayashi, et al.; Eur. J. Pharmacol. 316, 297 (1996) Abstract
Inhibition of glutathione reductase by plant polyphenols: K. Zhang, et al.; Biochem. Pharmacol 54, 1047 (1997) Abstract
Butein, a specific protein tyrosine kinase inhibitor: E.-B. Yang, et al.; BBRC 245, 435 (1998) Abstract
Antioxidant properties of butein isolated from Dalbergia odorifera: Z.J. Cheng, et al.; Biochim. Biophys. Acta 1392, 291 (1998) Abstract
Flavonoids inhibit cell growth and induce apoptosis in B16 melanoma 4A5 cells: K. Iwashita, et al.; Biosci. Biotechnol. Biochem. 64, 1813 (2000) Abstract
Butein, a plant polyphenol, induces apoptosis concomitant with increased caspase-3 activity, decreased Bcl-2 expression and increased Bax expression in HL-60 cells: N.Y. Kim, et al.; Pharmacol. Toxicol. 88, 261 (2001) Abstract
Small molecule activators of sirtuins extend Saccharomyces cerevisiae lifespan: K.T. Howitz, et al.; Nature 425, 191 (2003) Abstract
The plant polyphenol butein inhibits testosterone-induced proliferation in breast cancer cells expressing aromatase: Y. Wang, et al.; Life Sci. 77, 39 (2005) Abstract
Butein, a tetrahydroxychalcone, inhibits nuclear factor (NF)-kappaB and NF-kappaB-regulated gene expression through direct inhibition of IkappaBalpha kinase beta on cysteine 179 residue: M.K. Pandey, et al.; J. Biol. Chem. 282, 17340 (2007) Abstract
 
 
ALX-270-411 Revised 01-Apr-08
Butyrolactone 3
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SYNONYMS Gcn5 Inhibitor 1
MB-3
3-Methylene-4-hydroxycarbonyl-5-(1-propyl)-tetrahydrofuran-2-one
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY Histone Acetyl- & Methyl-Transferases/Related Products
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ALX-270-411-M005   5 mg 190.00 USD Add To Cart
Product Specification
FORMULA: C9H12O4
MW: 184.2
CAS NUMBER: 778649-18-6
SOURCE/HOST: Synthetic.
PURITY: ≥95% (1H-NMR)
APPEARANCE: White solid.
SOLUBILITY: Soluble in DMSO or methanol.
SHIPPING: AMBIENT
SHORT TERM STORAGE: +4°C
LONG TERM STORAGE: -20°C
USE/STABILITY: Stock solutions in DMSO are stable for at least 2 months when stored at -20°C.

Product Description
Racemic. Inhibitor of human histone acetyltransferase Gcn5.
Product Specific Literature References
Design, synthesis, and biological evaluation of a small-molecule inhibitor of the histone acetyltransferase Gcn5: M. Biel, et al.; Angew. Chem. Int. Ed. Engl. 43, 3974 (2004) Abstract
 
 
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-270-480 Revised 10-Mar-08 New product
Caffeic acid ethyl ester
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SYNONYMS CAEE
Ethyl caffeate
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Anti-inflammatory Agents
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ALX-270-480-M050   50 mg 20.00 USD Add To Cart
ALX-270-480-M250   250 mg 60.00 USD Add To Cart
Product Specification
FORMULA: C11H12O4
MW: 208.2
CAS NUMBER: 66648-50-8
SOURCE/HOST: Synthetic.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least one year after receipt when stored at -20°C.
HANDLING: Protect from light and moisture.

Product Description
Shows anti-carcinogenic, anti-inflammatory and immunomodulatory properties. Suppresses lipopolysaccharide (LPS)-induced nitric oxide (NO) production (IC50=5.5µg/ml). Potent and specific inhibitor of NF-κB and its downstream inflammatory mediators inducible nitric oxide synthase (iNOS; NOS II), prostaglandin E2 (PGE2) and cyclooxygenase-2 (COX-2). Prevents DNA single-strand breaks caused by H2O2.
Product Specific Literature References
Inhibitory effects of caffeic acid ethyl ester on H2O2-induced cytotoxicity and DNA single-strand breaks in Chinese hamster V79 cells: T. Nakayama, et al.; Biosci. Biotechnol. Biochem. 60, 316 (1996) Abstract
Ethyl caffeate suppresses NF-kappaB activation and its downstream inflammatory mediators, iNOS, COX-2, and PGE2 in vitro or in mouse skin: Y.M. Chiang, et al.; Br. J. Pharmacol. 146, 352 (2005) Abstract
Antitumor activity of some natural flavonoids and synthetic derivatives on various human and murine cancer cell lines: M. Cardenas, et al.; Bioorg. Med. Chem. 14, 2966 (2006) Abstract
Drastic effect of several caffeic acid derivatives on the induction of heme oxygenase-1 expression revealed by quantitative real-time RT-PCR: K. Suzuki, et al.; Biofactors 28, 151 (2006) Abstract
 
 
ALX-350-278 Revised 08-Apr-08
Caffeic acid n-octyl ester
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SYNONYMS n-Octylcaffeate
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - NF-kB Pathway Inhibitors
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ALX-350-278-M005   5 mg 25.00 USD Add To Cart
ALX-350-278-M025   25 mg 100.00 USD Add To Cart
Product Specification
FORMULA: C17H24O4
MW: 292.2
PURITY: ≥99%
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
More potent analog than CAPE (Prod. No. ALX-270-244). Suppressor of inducible nitric oxide synthase (iNOS; NOS II). Induces apoptosis.
Product Specific Literature References
Mechanism of toxicity of esters of caffeic and dihydrocaffeic acids: B. Etzenhouser, et al.; Bioorg. Med. Chem. 9, 199 (2001) Abstract
A novel antioxidant, octyl caffeate, suppression of LPS/IFN-gamma-induced inducible nitric oxide synthase gene expression in rat aortic smooth muscle cells: G. Hsiao, et al.; Biochem. Pharmacol. 65, 1383 (2003) Abstract
Caffeic acid derivatives: in vitro and in vivo anti-inflammatory properties: F.M. da Cunha, et al.; Free Radic. Res. 38, 1241 (2004) Abstract
Octylcaffeate induced apoptosis in human leukemia U937 cells: M. Ujibe, et al.; Biol. Pharm. Bull. 28, 2338 (2005) Abstract
General Information
Octylcaffeate significantly ameliorates circulatory failure of endotoxemia by suppression of iNOS (NOS II) expression through inactivation of mitogen-activated protein kinases.
 
 
ALX-270-244 Revised 03-Apr-08
Caffeic acid phenylethyl ester
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SYNONYMS CAPE
Phenethyl caffeiate
Caffeic acid phenethyl ester
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Anti-inflammatory Agents
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ALX-270-244-M010   10 mg 20.00 USD Add To Cart
ALX-270-244-M050   50 mg 60.00 USD Add To Cart
Product Specification
FORMULA: C17H16O4
MW: 284.3
CAS NUMBER: 115610-29-2
SOURCE/HOST: Synthetic.
PURITY: ≥97% (HPLC)
APPEARANCE: White to off-white crystalline solid.
SOLUBILITY: Soluble in DMSO, 100% ethanol, methanol, acetone or acetonitrile; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least one year after receipt when stored at –20°C.
HANDLING: Protect from light and moisture.
HAZARD: IRRITANT.

Product Description
Active component of propolis from honeybee hives, known to have anti-mitogenic, anti-carcinogenic, anti-inflammatory, and immunomodulatory properties. Potent and specific inhibitor of NF-κB activation, induced by TNF-α (Prod. No. ALX-522-008 (human) or Prod. No. ALX-522-009 (mouse)), PMA (Prod. No. ALX-445-004) and other inflammatory agents. Exhibits inhibitory activity against HIV-1 integrase (IC50=7µM). Suppresses lipid peroxidation and inhibits ornithine decarboxylase, protein tyrosine kinase and lipoxygenase activities. Induces apoptosis.
Product Specific Literature References
Hydroxylated aromatic inhibitors of HIV-1 integrase: T.R. Burke Jr., et al.; J. Med. Chem. 38, 4171 (1995) Abstract
Apoptosis and altered redox state induced by caffeic acid phenethyl ester (CAPE) in transformed rat fibroblast cells: C. Chiao, et al.; Cancer Res. 55, 3576 (1995) Abstract
Caffeic acid phenethyl ester is a potent and specific inhibitor of activation of nuclear transcription factor NF-kappa B: K. Natarajan, et al.; PNAS 93, 9090 (1996) Abstract
Inhibitory effects of caffeic acid phenethyl ester on the activity and expression of cyclooxygenase-2 in human oral epithelial cells and in a rat model of inflammation: P. Michaluart, et al.; Cancer Res. 59, 2347 (1999) Abstract
Caffeic acid phenethyl ester induces leukocyte apoptosis, modulates nuclear factor-kappa B and suppresses acute inflammation: Z. Orban, et al.; Neuroimmunomodulation 7, 99 (2000) Abstract
Caffeic acid phenethyl ester inhibits T-cell activation by targeting both nuclear factor of activated T-cells and NF-kappaB transcription factors: N. Marquez, et al.; J. Pharmacol. Exp. Ther. 308, 993 (2004) Abstract
Caffeic acid derivatives: in vitro and in vivo anti-inflammatory properties: F.M. da Cunha, et al.; Free Radic. Res. 38, 1241 (2004) Abstract
Drastic effect of several caffeic acid derivatives on the induction of heme oxygenase-1 expression revealed by quantitative real-time RT-PCR: K. Suzuki, et al.; Biofactors 28, 151 (2006) Abstract
 
 
ALX-550-322 Revised 29-Oct-07
Caffeine
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SYNONYMS 1,3,7-Trimethylxanthine
3,7-Dihydro-1,3,7-trimethyl-1H-purine-2,6-dione
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products for Neurological Research
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ALX-550-322-G005   5 g 10.00 USD Add To Cart
Product Specification
FORMULA: C8H10N4O2
MW: 194.2
CAS NUMBER: 58-08-2
MERCK INDEX: 14: 1636
SOURCE/HOST: Found in tea leaves, coffee beans, cocoa beans, maté leaves, guarana paste and kola nuts.
PURITY: ≥99%
APPEARANCE: White powder.
SOLUBILITY: Soluble in chloroform, 100% alcohol or hot water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
HAZARD: TOXIC.

Product Description
CNS stimulant. Blocks adenosine A1 and A2A receptors. cAMP phosphodiesterase inhibitor. Interferes with the uptake and storage of Ca2+ by the sarcoplasmic reticulum in skeletal muscle. Prevents apoptosis and cell cycle effects induced by various chemicals. Inhibits cellular DNA repair mechanisms. Anti-inflammatory.
Product Specific Literature References
Analogues of caffeine and theophylline: effect of structural alterations on affinity at adenosine receptors: J.W. Daly, et al.; J. Med. Chem. 29, 1305 (1986) Abstract
Caffeine as an analgesic adjuvant: a review of pharmacology and mechanisms of action: J. Sawynok & T.L. Yaksh; Pharmacol. Rev. 45, 43 (1993) Abstract
Caffeine prevents apoptosis and cell cycle effects induced by camptothecin or topotecan in HL-60 cells: F. Traganos, et al.; Cancer Res. 53, 4613 (1993) Abstract
Multiple effects of caffeine on calcium current in rat ventricular myocytes: I. Zahradnik & P. Palade; Pfluegers Arch. 424, 129 (1993) Abstract
Acute effects of caffeine on arterial stiffness, wave reflections, and central aortic pressures: T.G. Papaioannou, et al.; Am. J. Hypertens. 18, 129 (2005), (Review) Abstract
Caffeine and the dopaminergic system: O. Cauli & M. Morelli; Behav. Pharmacol. 16, 63 (2005), (Review) Abstract
Immunomodulatory effects of caffeine: friend or foe: L. A. Horrigan, et al.; Pharmacol. Ther. 111, 877 (2006), (Review) Abstract
Novel neuroprotection by caffeine and adenosine A(2A) receptor antagonists in animal models of Parkinson’s disease: A. Kalda, et al.; J. Neurol. Sc