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ALX-270-313 Revised 03-Mar-05
BPIQ-I
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SYNONYMS 8-[(3-Bromophenyl)amino]-3-methyl-3H-imidazo[4,5-γ]-quinazoline
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY EGFR Kinase Inhibitors
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ALX-270-313-M001   1 mg 140.00 USD Add To Cart
Product Specification
FORMULA: C16H12BrN5
MW: 354.2
PURITY: ≥95%
APPEARANCE: Off white to yellow solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light. Keep under inert gas.

Product Description
Potent and specific inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR) (IC50=25 pM).
Product Specific Literature References
Tyrosine kinase inhibitors. 9. Synthesis and evaluation of fused tricyclic quinazoline analogues as ATP site inhibitors of the tyrosine kinase activity of the epidermal growth factor receptor: G.W. Rewcastle, et al.; J. Med. Chem. 39, 918 (1996) Abstract
Further Categories Containing This Product:
Tyrosine Kinase Inhibitors
 
 
ALX-270-338 Revised 03-Mar-05
BPIQ-II
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SYNONYMS 8-[(3-Bromophenyl)amino]-1H-imidazo[4,5-γ]-quinazoline
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY EGFR Kinase Inhibitors
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ALX-270-338-M001   1 mg 140.00 USD Add To Cart
Product Specification
FORMULA: C15H10BrN5
MW: 340.2
PURITY: ≥98%
APPEARANCE: Pale pink solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light. Keep under inert gas.

Product Description
Potent and specific inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR) (IC50=8pM).
Product Specific Literature References
Tyrosine kinase inhibitors. 9. Synthesis and evaluation of fused tricyclic quinazoline analogues as ATP site inhibitors of the tyrosine kinase activity of the epidermal growth factor receptor: G.W. Rewcastle, et al.; J. Med. Chem. 39, 918 (1996) Abstract
Further Categories Containing This Product:
Tyrosine Kinase Inhibitors
 
 
ALX-350-019 Revised 17-Apr-08
(+)-Brefeldin A
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SYNONYMS BFA
Ascotoxin
Decumbin
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Apoptosis Inducers & Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-019-M005   5 mg 80.00 USD Add To Cart
ALX-350-019-M010   10 mg 130.00 USD Add To Cart
ALX-350-019-M025   25 mg 270.00 USD Add To Cart
ALX-350-019-M050   50 mg 420.00 USD Add To Cart
Product Specification
FORMULA: C16H24O4
MW: 280.4
CAS NUMBER: 20350-15-6
MERCK INDEX: 14: 1369
SOURCE/HOST: Isolated from Eupenicillium brefeldianum.
PURITY: ≥97%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in methylene chloride or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: TOXIC.

Product Description
Inhibitor of intracellular protein transport and protein secretion, interfering with trafficking in the trans-Golgi network, leading to the accumulation of cycling proteins in ERGIC clusters. Blocks ADP-ribosylation factor (Arf) in an inactive GDP-bound conformation and thereby prevents binding of COPI coats to ERGIC and Golgi membranes. Upon brefeldin A treatment the Golgi rapidly tubulates and fuses with the ER by an energy-, temperature-, and microtubule-dependent process. In contrast, the drug has little effect on the ERGIC, which keeps its identity, although the ERGIC clusters become larger and more uniformly distributed in the cytoplasm of the cells. Inhibits intracellular collagen degradation. Also inhibits apical Na+ channels in epithelia. Induces apoptosis.
Product Specific Literature References
Decumbin, a new compound from a species of Penicillium: V.L. Singleton, et al.; Nature 181, 1072 (1958)
Über die Isolierung neuer Stoffwechselprodukte aus Penicillium brefeldianum Dodge.: E. Harri, et al.; Helv. Chim. Acta 46, 1235 (1963)
Novel blockade by brefeldin A of intracellular transport of secretory proteins in cultured rat hepatocytes: Y. Misumi, et al.; J. Biol. Chem. 261, 11398 (1986) Abstract; Full Text
Brefeldin A causes disassembly of the Golgi complex and accumulation of secretory proteins in the endoplasmic reticulum: T. Fujiwara, et al.; J. Biol. Chem. 263, 18545 (1988) Abstract; Full Text
Brefeldin A, thapsigargin, and AIF4- stimulate the accumulation of GRP78 mRNA in a cycloheximide dependent manner, whilst induction by hypoxia is independent of protein synthesis: B.D. Price, et al.; J. Cell. Physiol. 152, 545 (1992) Abstract
Brefeldin A and the endocytic pathway. Possible implications for membrane traffic and sorting: W. Hunziker, et al.; FEBS Lett. 307, 93 (1992), (Review) Abstract
Brefeldin A inhibits degradation as well as production and secretion of collagen in human lung fibroblasts: C.R. Ripley, et al.; J. Biol. Chem. 268, 3677 (1993) Abstract
Brefeldin A is a potent inducer of apoptosis in human cancer cells independently of p53: R.G. Shao, et al.; Exp. Cell Res. 227, 190 (1996) Abstract
Brefeldin A inhibition of apical Na+ channels in epithelia: R.S. Fisher, et al.; Am. J. Physiol. 270, C138 (1996) Abstract
Brefeldin A: deciphering an enigmatic inhibitor of secretion: A. Nebenfuhr, et al.; Plant Physiol. 130, 1102 (2002), Review Abstract
NKT cells provide help for dendritic cell-dependent priming of MHC class I-restricted CD8+ T cells in vivo: D. Stober, et al.; J. Immunol. 170, 2540 (2003) Abstract; Full Text
Interaction of BIG2, a brefeldin A-inhibited guanine nucleotide-exchange protein, with exocyst protein Exo70: K.F. Xu, et al.; PNAS 102, 2784 (2005) Abstract
 
 
ALX-385-029 Revised 08-Apr-08
4’-Bromoflavone
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SYNONYMS 4’-Bromo-2-phenylbenzopyran
4’-Bromo-2-phenyl-4H-1-benzopyran-4-one
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Flavonoids/Related Products
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ALX-385-029-G001   1 g 90.00 USD Add To Cart
Product Specification
FORMULA: C15H9BrO2
MW: 301.1
SOURCE/HOST: Synthetic.
PURITY: ≥98%
APPEARANCE: White to off-white solid.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: IRRITANT.

Product Description
Chemopreventive compound. Potent inducer of phase II detoxifying enzymes. Quininone reductase and glutathione S-transferase in cell culture and different tissues of rats. Aryl hydrocarbon hydroxylase inducer.
Product Specific Literature References
Simple vs. complex inheritance of inducible aryl hydrocarbon hydroxylase in mouse tissues: K. Burki, et al.; Biochem. Genet. 13, 417 (1975) Abstract
Cancer chemopreventive activity mediated by 4’-bromoflavone, a potent inducer of phase II detoxification enzymes: L.L. Song, et al.; Cancer Res. 59, 578 (1999) Abstract
Further Categories Containing This Product:
Respiratory Chain Other ProductsNatural Products - Chemopreventive Agents
 
 
ALX-350-005 Revised 02-Oct-07
Bryostatin 1
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Other Signal Transduction Pathway Modulators
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ALX-350-005-C010   10 µg 85.00 USD Add To Cart
Product Specification
FORMULA: C47H68O17
MW: 905.0
CAS NUMBER: 83314-01-6
MERCK INDEX: 14: 1457
PURITY: ≥97%
APPEARANCE: Colorless oil.
SOLUBILITY: 25mg/ml soluble in 100% ethanol or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Store tightly sealed. Binds to glass and plastic surfaces in aqueous solutions.

Product Description
Binds to and activates protein kinase C (PKC). Antineoplastic.
Product Specific Literature References
Isolation and structure of Bryostatin 1: G.R. Pettit, et al.; J. Am. Chem. Soc. 104, 6846 (1982)
Bryostatin 1: differentiating agent from the depths: R.M. Stone; Leuk. Res. 21, 399 (1997) Abstract
Chemistry and clinical biology of the bryostatins: R. Mutter & M. Wills; Bioorg. Med. Chem. 8, 1841 (2000), (Review) Abstract
The clinical development of the bryostatins: A. Clamp and G.C. Jayson; Anticancer Drugs 13, 673 (2002) Abstract
The chemistry and biology of the bryostatin antitumour macrolides: K.J. Hale, et al.; Nat. Prod. Rep. 19, 413 (2002), Review Abstract
Bryostatin-1: pharmacology and therapeutic potential as a CNS drug: M.K. Sun & D.L. Alkon; CNS Drug Rev. 12, 1 (2006), Review Abstract
 
 
ALX-400-048 Revised 06-Dec-07
Busulfan
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SYNONYMS 1,4-Butanediol dimethanesulfonate
PRODUCT LINE Cancer
PRODUCT CATEGORY Antitumor Agents (DNA Interaction & Gene Regulation)
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ALX-400-048-G010   10 g 20.00 USD Add To Cart
Product Specification
FORMULA: C6H14O6S2
MW: 246.3
CAS NUMBER: 55-98-1
MERCK INDEX: 14: 1505
RTECS: EK1750000
SOURCE/HOST: Synthetic.
PURITY: ≥98%
APPEARANCE: White to off-white crystalline powder.
SOLUBILITY: Soluble in acetone, 100% ethanol or DMSO; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: MAY BE CARCINOGENIC. VERY TOXIC. MAY BE TERATOGENIC.

Product Description
Antineoplastic bifunctional, DNA alkylating agent that causes DNA damage by cross-linking DNA and proteins. Causes double-base lesions mainly at 5’-GA-3’ and, to a lesser extent, at 5’-GG-3’ sequences. Forms an intrastrand cross-link at the 5’-GA-3’ sequence, in addition to monoalkylation. Selectively induces normal human fibroblast senescence through Erk and p38 pathways.
Product Specific Literature References
DNA intrastrand cross-link at the 5’-GA-3’ sequence formed by busulfan and its role in the cytotoxic effect: T. Iwamoto, et al.; Cancer Sci. 95, 454 (2004) Abstract
Kinetic of genotoxic expression in the pharmacodynamics of busulfan: P. Morales-Ramirez, et al.; Arch. Med. Res. 37, 316 (2006) Abstract
Busulfan-induced senescence is dependent on ROS production upstream of the MAPK pathway: V. Probin, et al.; Free Radic. Biol. Med. 42, 1858 (2007) Abstract
 
 
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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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-270-286 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-260-017 Revised 07-Jul-08
CA-074
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SYNONYMS N-[L-3-trans-Propylcarbamoyloxirane-2-carbonyl]-Ile-Pro-OH
PRODUCT LINE Cancer
PRODUCT CATEGORY Cathepsin Inhibitors
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ALX-260-017-M001   1 mg 210.00 USD Add To Cart
Product Specification
FORMULA: C18H29N3O6
MW: 383.5
CAS NUMBER: 134448-10-5
PURITY: