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ALX-350-280 Revised 07-Oct-08
Xanthohumol
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Other Natural Products - DNA Regulation / Transcription
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ALX-350-280-M005   5 mg 135.00 USD Add To Cart
Product Specification
FORMULA: C21H22O5
MW: 354.4
CAS NUMBER: 569-83-5, 6754-58-1
SOURCE/HOST: Isolated from hops (Humulus lupulus).
PURITY: ≥98% (HPLC)
APPEARANCE: Yellow to orange powder.
SOLUBILITY: Soluble in DMSO (25mg/ml), methanol (10mg/ml) or 100% ethanol; soluble in aqueous buffers up to 20μM.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Stable as powder for at least 6 months when stored at +4°C in the dark. Stock solution made in DMSO should not be stored for longer than one month. Working solution is stable for 24 hours at 37°C and up to one week when stored at +4°C. Unstable in acidic (pH < 4.5) and alkaline (pH > 7.5) systems.
IDENTITY: Identity determined by NMR.

Product Description
Prenylated chalcone found in beer. Potent inhibitor of diacylglycerol acetyltransferase (DGAT). Inhibits DNA polymerase and induces cell differentiation. Has antiproliferative and cytotoxic effects in human cancer cell lines. Inhibits human P450 enzymes. Induces quinone reductase. Inhibits the expression of HIF-1α and VEGF under hypoxic conditions. Induces apoptosis in mature adipocytes.
Product Specific Literature References
Xanthohumols, diacylglycerol acyltransferase inhibitors, from Humulus lupulus: N. Tabata, et al.; Phytochemistry 46, 683 (1997) Abstract
Antiproliferative and cytotoxic effects of prenylated flavonoids from hops (Humulus lupulus) in human cancer cell lines: C.L. Miranda, et al.; Food Chem. Toxicol. 37, 271 (1999) Abstract
In vitro inhibition of human P450 enzymes by prenylated flavonoids from hops, Humulus lupulus: M.C. Henderson, et al.; Xenobiotica 30, 235 (2000) Abstract
Prenylated chalcones and flavanones as inducers of quinone reductase in mouse Hepa 1c1c7 cells: C.L. Miranda, et al.; Cancer Lett. 149, 21 (2000) Abstract
Cancer chemopreventive activity of Xanthohumol, a natural product derived from hop: C. Gerhauser, et al.; Mol. Cancer Ther. 1, 959 (2002) Abstract
Xanthohumol and related prenylflavonoids from hops and beer: to your good health!: J.F. Stevens & J.E. Page; Phytochemistry 65, 1317 (2004), (Review) Abstract
Effect of xanthohumol and isoxanthohumol on 3T3-L1 cell apoptosis and adipogenesis: J.Y. Yang, et al.; Apoptosis 12, 1953 (2007) Abstract
 
 
ALX-380-201 Revised 27-Jun-08
Echinomycin
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SYNONYMS Quinomycin A
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - DNA Replication Inhibitors
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ALX-380-201-M001   1 mg 80.00 USD Add To Cart
ALX-380-201-M005   5 mg 320.00 USD Add To Cart
Product Specification
FORMULA: C51H64N12O12S2
MW: 1101.3
CAS NUMBER: 512-64-1
MERCK INDEX: 14: 3497
RTECS: JW5250000
SOURCE/HOST: Isolated from Streptomyces echinatus (DSM 40013).
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in 100% ethanol, dimethyl formamide or DMSO; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Hygroscopic.
HAZARD: TOXIC. MAY BE MUTAGENIC.
IDENTITY: Identity determined by 1H-NMR.

Product Description
Antitumor antibiotic. Powerful, selective inhibitor of nucleic acid synthesis in vitro. Potent inhibitor of hypoxia-inducible factor 1 (HIF-1) DNA binding activity. Induces apoptosis. Displays antibacterial, antifungal and antiviral activities.
Product Specific Literature References
A “quinoxaline antibiotic” similar to the triostins, q.v.: I. Kuroya, et al.; J. Antibiot. 14A, 324 (1961)
Identity of levomycin and quinomycin A (echimomycin): K. Katagiri, et al.; J. Antibiot. 15, 273 (1962) Abstract
The mode of action of quinoxaline antibiotics. Interaction of quinomycin A with deoxyribonucleic acid: K. Sato, et al.; J. Antibiot. 20, 270 (1967) Abstract
The binding of echinomycin to deoxyribonucleic acid: S.P. Wakelin & M.J. Waring; Biochem. J. 157, 721 (1976) Abstract; Full Text
Bifunctional intercalation and sequence specificity in the binding of quinomycin and triostin antibiotics to deoxyribonucleic acid: J.S. Lee & M.J. Waring; Biochem. J. 173, 115 (1978) Abstract; Full Text
Kinetics of the interaction between echinomycin and deoxyribonucleic acid: K.R. Fox, et al.; Biochemistry 20, 5768 (1981) Abstract
Sequence-specific binding of echinomycin to DNA: evidence for conformational changes affecting flanking sequences: C.M. Low, et al.; Nucl. Acids Res. 12, 4865 (1984) Abstract; Full Text
Echinomycin binding sites on DNA: M.M. Van Dyke & P.B. Dervan; Science 225, 1122 (1984) Abstract
Kinetic evidence that echinomycin migrates between potential DNA binding sites: K.R. Fox & M.J. Waring; Nucl. Acids Res. 13, 595 (1985) Abstract; Full Text
Effect of echinomycin on DNA methylation: R.L. Adams & A. Rinaldi; FEBS Lett. 215, 266 (1987) Abstract
Interaction of echinomycin with An.Tn. and (AT)n regions flanking its CG binding site: K. Waterloh & K.R. Fox; Nucl. Acids Res. 19, 6719 (1991) Abstract; Full Text
Localized chemical reactivity in DNA associated with the sequence-specific bisintercalation of echinomycin: C. Bailly, et al.; Biochem. J. 300, 165 (1994) Abstract; Full Text
Energetics of echinomycin binding to DNA: F. Leng, et al.; Nucl. Acids Res. 31, 6191 (2003) Abstract; Full Text
Echinomycin inhibits chromosomal DNA replication and embryonic development in vertebrates: L.G. May, et al.; Nucl. Acids Res. 32, 65 (2004) Abstract; Full Text
Echinomycin and a novel analogue induce apoptosis of HT-29 cells via the activation of MAP kinases pathway: J.Y. Park, et al.; Pharmacol. Res. 50, 201 (2004) Abstract
Echinomycin, a small-molecule inhibitor of hypoxia-inducible factor-1 DNA-binding activity: D. Kong, et al.; Cancer Res. 65, 9047 (2005) Abstract; Full Text
Molecular signaling cascade in DNA bisintercalator, echinomycin-induced apoptosis of HT-29 cells: evidence of the apoptotic process via activation of the cytochrome c-ERK-caspase-3 pathway: J.Y. Park, et al.; Int. J. Biochem. Cell Biol. 38, 244 (2006) Abstract
Synergistic effects of CoCl(2) and ROCK inhibition on mesenchymal stem cell differentiation into neuron-like cells: E. Pacary, et al.; J. Cell Sci. 119, 2667 (2006) Abstract; Full Text
Metabolic targeting of hypoxia and HIF1 in solid tumors can enhance cytotoxic chemotherapy: R.A. Cairns, et al.; PNAS 104, 9445 (2007) Abstract
 
 
ALX-385-008 Revised 13-Mar-08
Apigenin
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SYNONYMS 4',5,7-Trihydroxyflavone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Flavones
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ALX-385-008-M010   10 mg 35.00 USD Add To Cart
ALX-385-008-M050   50 mg 105.00 USD Add To Cart
Product Specification
FORMULA: C15H10O5
MW: 270.2
CAS NUMBER: 520-36-5
MERCK INDEX: 14: 730
SOURCE/HOST: Synthetic.
PURITY: ≥90% (HPLC)
APPEARANCE: Light yellow to slightly brown powder.
SOLUBILITY: Soluble in diluted potassium hydroxide or DMSO; slightly soluble in 100% ethanol (hot). Insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HAZARD: IRRITANT.

Product Description
Antioxidant flavonoid. Has chemopreventive and antitumor properties. Induces apoptosis. Inhibits the proliferation of malignant tumor cells by G2/M arrest. MAP kinase (MAPK/ERK) inhibitor. Inhibits hypoxia-inducible factor-1 (HIF-1) and vascular endothelial growth factor (VEGF) expression.
Product Specific Literature References
Apigenin and tangeretin enhance gap junctional intercellular communication in rat liver epithelial cells: C. Chaumontet, et al.; Carcinogenesis 15, 2325 (1994) Abstract
Apigenin induces morphological differentiation and G2-M arrest in rat neuronal cells: F. Sato, et al.; BBRC 204, 578 (1994) Abstract
Reversion of v-H-ras-transformed NIH 3T3 cells by apigenin through inhibiting mitogen activated protein kinase and its downstream oncogenes: M.L. Kuo and N.C. Yang; BBRC 212, 767 (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) Abstract
Apigenin inhibits endothelial-cell proliferation in G(2)/M phase whereas it stimulates smooth-muscle cells by inhibiting P21 and P27 expression: V. Trochon, et al.; Int. J. Cancer 85, 691 (2000) Abstract
Induction of caspase-dependent, p53-mediated apoptosis by apigenin in human neuroblastoma: R. Torkin, et al.; Mol. Cancer Ther. 4, 1 (2005) Abstract
Apigenin and cancer chemoprevention: progress, potential and promise: D. Patel, et al.; Int. J. Oncol. 30, 233 (2007), (Review) Abstract
Apigenin inhibits tumor angiogenesis through decreasing HIF-1alpha and VEGF expression: J. Fang, et al.; Carcinogenesis 28, 858 (2007) Abstract
Apigenin-induced cell cycle arrest is mediated by modulation of MAPK, PI3K-Akt, and loss of cyclin D1 associated retinoblastoma dephosphorylation in human prostate cancer cells: S. Shukla & S. Gupta; Cell Cycle 6, 1102 (2007) Abstract
Apigenin blocks lipopolysaccharide-induced lethality in vivo and proinflammatory cytokines expression by inactivating NF-kappaB through the suppression of p65 phosphorylation: C. Nicholas, et al.; J. Immunol. 179, 7121 (2007) Abstract
 
 
ALX-385-009 Revised 03-Apr-08
Chrysin
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SYNONYMS 5,7-Dihydroxyflavone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Flavones
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ALX-385-009-G001   1 g 15.00 USD Add To Cart
Product Specification
FORMULA: C15H10O4
MW: 254.2
CAS NUMBER: 480-40-0
MERCK INDEX: 14: 2256
RTECS: LK8329050
PURITY: ≥96%
APPEARANCE: Yellow to tan solid.
SOLUBILITY: Soluble in pyridine or alkaline solutions; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C

Product Description
Antioxidant flavonoid. Shows anti-inflammatory and antitumor properties. Inhibits hypoxia-inducible factor-1α (HIF-1α). Induces apoptosis.
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
Chrysin-induced apoptosis is mediated through caspase activation and Akt inactivation in U937 leukemia cells: K.J. Woo, et al.; Biochem. Biophys. Res. Commun. 325, 1215 (2004) Abstract
Chrysin induces G1 phase cell cycle arrest in C6 glioma cells through inducing p21Waf1/Cip1 expression: involvement of p38 mitogen-activated protein kinase: M.S. Weng, et al.; Biochem. Pharmacol. 69, 1815 (2005) Abstract
Dietary flavonoids: effects on xenobiotic and carcinogen metabolism:: Y.J. Moon, et al.; Toxicol. In Vitro 20, 187 (2006), (Review) Abstract
Chrysin inhibits expression of hypoxia-inducible factor-1alpha through reducing hypoxia-inducible factor-1alpha stability and inhibiting its protein synthesis: B. Fu, et al.; Mol. Cancer Ther. 6, 220 (2007) Abstract
 
 
ALX-420-025 Revised 26-Jun-08
YC-1
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SYNONYMS 3-(5'-Hydroxymethyl-2'-furyl)-1-benzylindazole
PRODUCT LINE Nitric Oxide Pathway
PRODUCT CATEGORY Guanylyl Cyclases, Guanosine Phosphate Metabolism / Related Products
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ALX-420-025-M001   1 mg 20.00 USD Add To Cart
ALX-420-025-M005   5 mg 65.00 USD Add To Cart
ALX-420-025-M025   25 mg 260.00 USD Add To Cart
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Product Specification
FORMULA: C19H16N2O2
MW: 304.4
CAS NUMBER: 170632-47-0
PURITY: ≥98% (HPLC)
APPEARANCE: White to pale yellow powder.
SOLUBILITY: Soluble in DMSO, methanol or dichloromethane.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.
IDENTITY: Identity determined by 1H-NMR.

Product Description

Nitric oxide (NO) independent, superoxide-sensitive stimulator of soluble guanylyl cyclase (sGC). Inhibits platelet adhesion to collagen. Non-specific phosphodiesterase inhibitor. YC-1 inhibits HIF-α activity in tumors resulting in blocked angiogenesis and an inhibition of tumor growth.
Inhibits Na+ channel.
Binds to [3H]BW202W92.

Product Specific Literature References
YC-1, a novel activator of platelet guanylate cyclase: F.N. Ko, et al.; Blood 84, 4226 (1994) Abstract
YC-1 inhibited human platelet aggregation through NO-independent activation of soluble guanylate cyclase: C.C. Wu, et al.; Br. J. Pharmacol 116, 1973 (1995) Abstract
Effect of YC-1, an NO-independent, superoxide-sensitive stimulator of soluble guanylyl cyclase, on smooth muscle responsiveness to nitrovasodilators: A. Mülsch, et al.; Br. J. Pharmacol. 120, 681 (1997) Abstract
Activation of soluble guanylyl cyclase by YC-1 in aortic smooth muscle but not in ventricular myocardium from rat: J.W. Wegener, et al.; Br. J. Pharmacol. 122, 1523 (1997) Abstract
Differential effects of isoliquiritigenin and YC-1 in rat aortic smooth muscle: J.W. Wegener & H. Nawrath; Eur. J. Pharmacol. 323, 89 (1997) Abstract
Inhibition of platelet adhesion to collagen by cGMP-elevating agents: C.-C. Wu, et al.; BBRC 231, 412 (1997) Abstract
Mechanism of YC-1-induced activation of soluble guanylyl cyclase: A. Friebe & D. Koesling; Mol. Pharmacol. 53, 123 (1998) Abstract; Full Text
Nitric oxide-sensitive guanylyl cyclase inhibits acetylcholine release and excitatory motor transmission in the guinea-pig ileum: K. Hebeiss & H. Kilbinger; Neuroscience 82, 623 (1998) Abstract
Synergistic activation of soluble guanylate cyclase by YC-1 and carbon monoxide: implications for the role of cleavage of the iron-histidine bond during activation by nitric oxide: J.R. Stone & M.A. Marletta; Chem. Biol. 5, 255 (1998) Abstract
Generation and characterization of a stable soluble guanylate cyclase-overexpressing CHO cell line: E.M. Becker, et al.; Nitric Oxide 3, 55 (1999) Abstract
Soluble guanylyl cyclase activator YC-1 protects white matter axons from nitric oxide toxicity and metabolic stress, probably through Na(+) channel inhibition: G. Garthwaite, et al.; Mol. Pharmacol. 61, 97 (2002) Abstract
A Novel Drug Binding Site on Voltage-Gated Sodium Channels in Rat Brain: D. R. Riddall, et al.; Mol. Pharmacol. 69, 278 (2006) Abstract
General Literature References
[1] YC-1: a potential anticancer drug targeting hypoxia-inducible factor 1: E.J. Yeo, et al.; J. Natl. Cancer Inst. 95, 516 (2003) Abstract
 
 
ALX-270-434 Revised 18-Apr-06
Tie-2 Inhibitor 13
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SYNONYMS (1Z)-5-Fluoro-2-methyl-1-(3-thienylmethylene)-1H-indene-3-acetic acid
PRODUCT LINE Cancer
PRODUCT CATEGORY Angiopoietins & Tie Receptors / Related Products
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ALX-270-434-M001   1 mg 110.00 USD Add To Cart
Product Specification
FORMULA: C17H13FO2S
MW: 300.6
CAS NUMBER: 857250-95-4
PURITY: ≥95%
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least 6 months when stored at -20°C in the dark.
HANDLING: Protect from light.
IDENTITY: Identity determined by 1H-NMR, 13C-NMR and MS.

Product Description
Potent and cell permeable Tie-2 inhibitor (IC50=600nm).
Product Specific Literature References
Inhibition of angiogenesis-relevant receptor tyrosine kinases by sulindac analogues: E. Gourzoulidou, et al.; Chembiochem. 6, 527 (2005) Abstract
Endothelial survival factors and spatial completion, but not pericyte coverage of retinal capillaries determine vessel plasticity: J. Hoffmann, et al.; FASEB J. 19, 2035 (2005) Abstract
 
 
ALX-270-086 Revised 07-May-08
Indomethacin
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PRODUCT LINE Inflammation
PRODUCT CATEGORY Non-Steroidal Anti-Inflammatory Drugs [NSAIDS]
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ALX-270-086-G005   5 g 30.00 USD Add To Cart
ALX-270-086-G025   25 g 80.00 USD Add To Cart
Product Specification
FORMULA: C19H16ClNO4
MW: 357.8
CAS NUMBER: 53-86-1
MERCK INDEX: 14: 4968
PURITY: ≥98%
APPEARANCE: Off-white solid.
SOLUBILITY: Soluble in acetone or methanol; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
HAZARD: VERY TOXIC.

Product Description
Non-steroidal anti-inflammatory and analgesic agent. Inhibits prostaglandin synthesis. Far more potent for inhibition of cyclooxygenases (COX) than for inhibition of lipoxygenases.
Product Specific Literature References
Chemical and biological studies on indomethacin, sulindac and their analogs: T.Y. Shen, et al.; Adv. Drug Res. 12, 90 (1977) Abstract
Comparative effects of indomethacin, acetylenic acids, 15-HETE, nordihydroguaiaretic acid and BW755C on the metabolism of arachidonic acid in human leukocytes and platelets: H. Salari, et al.; Prostagl. Leukotr. Med. 13, 53 (1984) Abstract
Effects of indomethacin on fetal renal function, renal and umbilicoplacental blood flow and lung liquid production: K.M. Stevenson & E.R. Lumbers; J. Dev. Physiol. 17, 257 (1992) Abstract
NS-398, a new anti-inflammatory agent, selectively inhibits prostaglandin G/H synthase/cyclooxygenase (COX-2) activity in vitro: N. Futaki, et al.; Prostaglandins 47, 55 (1994) Abstract
Further Categories Containing This Product:
Analgesic / Anti-nociceptive Agents / Related ProductsCOX Inhibitors
 
 
ALX-270-097 Revised 07-Sep-06
Ebselen
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SYNONYMS 2-Phenyl-1,2-benzisoselenazol-3-(2H)-one
PRODUCT LINE Oxidative Stress
PRODUCT CATEGORY Peroxynitrite / Scavengers / Detection
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ALX-270-097-M001   1 mg 12.00 USD Add To Cart
ALX-270-097-M005   5 mg 20.00 USD Add To Cart
ALX-270-097-M025   25 mg 60.00 USD Add To Cart
Product Specification
FORMULA: C13H9NOSe
MW: 274.2
CAS NUMBER: 60940-34-3
PURITY: ≥98% (NMR)
APPEARANCE: White to off-white crystalline solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT