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ALX-270-371 Revised 18-Jun-07
Dimethyloxalyl glycine
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SYNONYMS DMOG
N-(Methoxyoxoacetyl)-glycine methyl ester
PRODUCT LINE Oxidative Stress
PRODUCT CATEGORY Hypoxia-inducible Factor [HIF]/Related Products
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-371-M010   10 mg 18.00 USD Add To Cart
ALX-270-371-M050   50 mg 72.00 USD Add To Cart
ALX-270-371-M100   100 mg 120.00 USD Add To Cart
Product Specification
FORMULA: C6H9NO5
MW: 175.1
CAS NUMBER: 89464-63-1
PURITY: ≥98%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in 100% ethanol, DMSO or dimethyl formamide; also soluble in PBS.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least 1 year when stored at -20°C. Stock solutions are stable for at least 6 months if stored at -20°C.

Product Description
Cell permeable, competitive inhibitor of PHDs (prolyl hydroxylase domain-containing proteins; HIF-PHs), which destructs HIF-1α when hydroxylated at a specific proline residue (P564). Stabilizes HIF-1α expression at normal oxygen tensions in cultured cells at concentrations between 0.1 and 1mM. Expected to act pro-angiogenic.
Product Specific Literature References
Targeting of HIF-alpha to the von Hippel-Lindau ubiquitylation complex by O2-regulated prolyl hydroxylation: P. Jaakkola, et al.; Science 292, 468 (2001) Abstract
A conserved family of prolyl-4-hydroxylases that modify HIF: R.K. Bruick & S.L. McKnight; Science 294, 1337 (2001) Abstract
HIFalpha targeted for VHL-mediated destruction by proline hydroxylation: implications for O2 sensing: M. Ivan, et al.; Science 292, 464 (2001) Abstract
General Information
BACKGROUND/TECHNICAL INFORMATION A stock solution may be made by dissolving the DMOG in an organic solvent purged with an inert gas. DMOG is soluble in organic solvents such as ethanol, DMSO and dimethyl formamide.The solubility of DMOG in these solvents is at least 30mg/ml. DMOG will be stable for at least six months in these solvents if stored at -20°C.
Further dilutions of the stock solution into aqueous buffers or isotonic saline should be made prior to performing biological experiments. Ensure that the residual amount of organic solvent is insignificant, since organic solvents may have physiological effects at low concentrations. Organic solvent-free aqueous solutions of DMOG can be prepared by directly dissolving the crystalline compound powder in aqueous buffers. The solubility of DMOG in PBS (pH 7.2) is at least 10mg/ml.
 
 
ALX-380-226 Revised 03-Apr-08
Dinactin
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SYNONYMS Antibiotic AKD 1C
Antibiotic S 3466A
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Ionophores
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ALX-380-226-M001   1 mg 370.00 USD Add To Cart
Product Specification
FORMULA: C42H68O12
MW: 765.0
CAS NUMBER: 20261-85-2
SOURCE/HOST: Isolated from Streptomyces sp. MST-AS5448.
PURITY: ≥95% (HPLC)
APPEARANCE: Colorless film.
SOLUBILITY: Soluble in ethyl acetate or DMSO; moderately soluble in 100% ethanol or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Antibioit. Cation ionophore with high selectivity for ammonium and potassium. Inhibits T cell proliferation induced by IL-2 and cytokine production at nanomolar levels. Dimeric dinactin shows potent antineoplastic and antibacterial activities.
Product Specific Literature References
The in Vitro Activity of Nonactin and Its Homologs: Monactin, Dinactin and Trinactin: E. Meyers, et al.; J. Antibiot. (Tokyo) 18, 128 (1965) Abstract
Antibiotics as tools for metabolic studies. V. Effect of nonactin, monactin, dinactin, and trinactin on oxidative phosphorylation and adenosine triphosphatase induction: S.N. Graven, et al.; Biochemistry 5, 1729 (1966) Abstract
Antibiotics as tools for metabolic studies. VI. Damped oscillatory swelling of mitochondria induced by nonactin, monactin, dinactin, and trinactin: S.N. Graven, et al.; Biochemistry 5, 1735 (1966) Abstract
Immunosuppressive effects of polynactins (tetranactin, trinactin and dinactin) on experimental autoimmune uveoretinitis in rats: Y. Tanouchi and H. Shichi; Jpn. J. Ophthalmol. 31, 218 (1987) Abstract
Effects of cyclosporin A and dinactin on T-cell proliferation, interleukin-5 production, and murine pulmonary inflammation: S.P. Umland, et al.; Am. J. Respir. Cell. Mol. Biol. 20, 481 (1999) Abstract; Full Text
Antibacterial and antitumor macrolides from Streptomyces sp. Is9131: P.J. Zhao, et al.; Arch. Pharm. Res. 28, 1228 (2005) Abstract
Related Products
Further Categories Containing This Product:
Antitumor Antibiotics • Antibiotics - Immunomodulators
 
 
ALX-385-031 Revised 06-Mar-08 New product
Diosmin
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SYNONYMS 3’,5,7-Trihydroxy-4’-methoxyflavone 7-rutinoside
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Flavonoids/Related Products
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-385-031-G005   5 g 30.00 USD Add To Cart
ALX-385-031-G025   25 g 90.00 USD Add To Cart
Product Specification
FORMULA: C28H32O15
MW: 608.5
CAS NUMBER: 520-27-4
MERCK INDEX: 14: 3297
SOURCE/HOST: Isolated from Citrus aurantium L. and Citrus reticulate Blanca.
PURITY: ≥90% (HPLC)
APPEARANCE: Light yellow to brown yellow powder.
SOLUBILITY: Soluble in DMSO (50mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
IDENTITY: Determined by IR.

Product Description

Flavonoid glycoside. Main component in citrus fruits. Phlebotropic drug used to control internal symptoms of hemorrhoids and in the treatment of venous diseases. Prolongs the vasoconstrictor effect of noradrenaline on the vein wall. Reduces venous hyperpressure. Reduces capillary hyperpermeability and the expression of endothelial adhesion molecules (ICAM1, VCAM1). Effectively inhibits the P-glycoprotein (Pgp)-mediated efflux in cells. Anti-inflammatory. Inhibits lipopolysaccharide (LPS)-induced endothelial cytotoxicity.
Product Specific Literature References
Clinical trial of oral diosmin (Daflon) in the treatment of hemorrhoids: W. Thanapongsathorn & T. Vajrabukka; Dis. Colon Rectum 35, 1085 (1992) Abstract
Amine uptake inhibition by diosmin and diosmetin in human neuronal and neuroendocrine cell lines: E. Sher, et al.; Pharmacol. Res. 26, 395 (1992) Abstract
Antioxidant activity of micronized diosmin on oxygen species from stimulated human neutrophils: B. Cypriani, et al.; Biochem. Pharmacol. 45, 1531 (1993) Abstract
Diosmin-induced increase in sensitivity to Ca2+ of the smooth muscle contractile apparatus in the rat isolated femoral vein: J.P. Savineau & R. Marthan; Br. J. Pharmacol. 111, 978 (1994) Abstract; Full Text
Venous elasticity after treatment with Daflon 500 mg: V. Ibegbuna, et al.; Angiology 48, 45 (1997) Abstract
Chemopreventive effects of diosmin and hesperidin on N-butyl-N-(4-hydroxybutyl)nitrosamine-induced urinary-bladder carcinogenesis in male ICR mice: M. Yang, et al.; Int. J. Cancer 73, 719 (1997) Abstract
Diosmin and diosmetin are agonists of the aryl hydrocarbon receptor that differentially affect cytochrome P450 1A1 activity: H.P. Ciolino, et al.; Cancer Res. 58, 2754 (1998) Abstract; Full Text
Modulation by phytochemicals of cytochrome P450-linked enzyme activity: R.W. Teel & H. Huynh; Cancer Lett. 133, 135 (1998) Abstract
Inhibition of lipopolysaccharide (LPS)-induced endothelial cytotoxicity by diosmin: M.F. Melzig & R. Loose; Pharmazie 54, 298 (1999) Abstract
Anti-inflammatory activity of diosmin and hesperidin in rat colitis induced by TNBS: M.E. Crespo, et al.; Planta Med. 65, 651 (1999) Abstract
Further investigation of the modifying effect of various chemopreventive agents on apoptosis and cell proliferation in human colon cancer cells: Q. Zheng, et al.; J. Cancer Res. Clin. Oncol. 128, 539 (2002) Abstract
The effect of diosmin hesperidin on intestinal ischaemia--reperfusion injury: M. Pehlivan, et al.; Acta Chir. Belg. 104, 715 (2004) Abstract
Treatment of metastatic melanoma B16F10 by the flavonoids tangeretin, rutin, and diosmin: C. Martinez Conesa, et al.; J. Agric. Food Chem. 53, 6791 (2005) Abstract
Further Categories Containing This Product:
CD11a, CD18 [LFA-1] & CD54 [ICAM-1], CD102 [ICAM-2], CD50 [ICAM-3]/Related Products • Natural Products - Anti-inflammatory Agents • Natural Products - Chemopreventive Agents • Active Substances from Fruit and Vegetables
 
 
ALX-380-110 Revised 03-Apr-08
17-DMAG
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SYNONYMS 17-[2-(Dimethylamino)ethyl]amino-17-desmethoxygeldanamycin
NSC 707545
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics for Angiogenesis Research
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-380-110-C100   100 µg 50.00 USD Add To Cart
ALX-380-110-M001   1 mg 150.00 USD Add To Cart
Product Specification
FORMULA: C32H48N4O8
MW: 616.8
CAS NUMBER: 150270-08-9
SOURCE/HOST: Semisynthetic from geldanamycin (Prod. No. ALX-380-054).
PURITY: ≥99%
APPEARANCE: Purple to black powder.
SOLUBILITY: Soluble in water, 100% ethanol (10mg/ml) or DMSO (>25mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description

Less toxic, more potent synthetic derivative of geldanamycin. Inhibitor of angiogenesis. Inhibitor of heat shock protein 90 (HSP90). Inducer of apoptosis with higher antitumor activity than 17-AAG (Prod. No. ALX-380-091).
Product Specific Literature References
Pharmacokinetics, tissue distribution, and metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin (NSC 707545) in CD2F1 mice and Fischer 344 rats: M.J. Egorin, et al.; Cancer Chemother. Pharmacol. 49, 7 (2002) Abstract
Biliary excretion of 17-(allylamino)-17-demethoxygeldanamycin (NSC 330507) and metabolites by Fischer 344 rats: S.M. Musser, et al.; Cancer Chemother. Pharmacol. 52, 139 (2003) Abstract
Crystal structure and molecular modeling of 17-DMAG in complex with human Hsp90: J.M. Jez, et al.; Chem. Biol. 10, 361 (2003) Abstract
Synthesis and biological activities of novel 17-aminogeldanamycin derivatives: Z.Q. Tian, et al.; Bioorg. Med. Chem. 12, 5317 (2004) Abstract
Antiangiogenic properties of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin: an orally bioavailable heat shock protein 90 modulator: G. Kaur, et al.; Clin. Cancer Res. 10, 4813 (2004) Abstract
Enhanced tumor cell radiosensitivity and abrogation of G2 and S phase arrest by the Hsp90 inhibitor 17-(Dimethylaminoethylamino)-17-demethoxygeldanamycin: E.E. Bull, et al.; Clin. Cancer Res. 10, 8077 (2004) Abstract
ErbB3 expression predicts tumor cell radiosensitization induced by Hsp90 inhibition: H. Dote, et al.; Cancer Res. 65, 6967 (2005) Abstract
In vivo antitumor efficacy of 17-DMAG (17-dimethylaminoethylamino-17-demethoxygeldanamycin hydrochloride), a water-soluble geldanamycin derivative: M. Hollingshead, et al.; Cancer Chemother. Pharmacol. 56, 115 (2005) Abstract
Comparison of 17-dimethylaminoethylamino-17-demethoxy-geldanamycin (17DMAG) and 17-allylamino-17-demethoxygeldanamycin (17AAG) in vitro: effects on Hsp90 and client proteins in melanoma models: V. Smith, et al.; Cancer Chemother. Pharmacol. 56, 126 (2005) Abstract
Preclinical toxicity of a geldanamycin analog, 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin (17-DMAG), in rats and dogs: potential clinical relevance: E.R. Glaze, et al.; Cancer Chemother. Pharmacol. 56, 637 (2005) Abstract
17-Allyamino-17-demethoxygeldanamycin and 17-NN-dimethyl ethylene diamine-geldanamycin have cytotoxic activity against multiple gynecologic cancer cell types: D.R. Gossett, et al.; Gynecol. Oncol. 96, 381 (2005) Abstract
Structure-based design of 7-carbamate analogs of geldanamycin: G. Rastelli, et al.; Biooorg. Med. Chem. Lett. 15, 5016 (2005) Abstract
Generation of a novel anti-geldanamycin antibody: E. Barzilay, et al.; BBRC 330, 561 (2005) Abstract
Determination of the heat shock protein 90 inhibitor 17-dimethylaminoethylamino-17-demethoxygeldanamycin in plasma by liquid chromatography-electrospray mass spectrometry: K. Hwang, et al.; J. Chromatogr. B Analyt. Technol. Biomed. Life Sci. 830, 35 (2006) Abstract
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Further Categories Containing This Product:
Antibiotics - Apoptosis Inducers & Inhibitors • Antitumor Agents (Enzyme Inhibitors) • Tyrosine Kinase Inhibitors • Antitumor Antibiotics • HSP90/HtpG/Related Products
 
 
ALX-260-120 Revised 12-Dec-07
Dnp-Pro-Leu-Gly-Met-Trp-Ser-Arg-OH
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PRODUCT LINE Cytoskeleton
PRODUCT CATEGORY MMP Substrates
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-260-120-M005   5 mg 250.00 USD Add To Cart
Product Specification
SEQUENCE: 2,4-Dinitrophenyl-Pro-Leu-Gly-Met-Trp-Ser-Arg-OH
FORMULA: C44H61N13O13S
MW: 1012.1
PURITY: ≥95% (HPLC)
APPEARANCE: Yellow solid
SOLUBILITY: Soluble in DMSO; dilute with distilled water or buffer.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
Product Description
Fluorogenic substrate for MMP-2 and MMP-9. Excitation: 280nm; emission 360nm.
Product Specific Literature References
Continuously recording fluorescent assays optimized for five human matrix metalloproteinases: S. Netzel-Arnett, et al.; Anal. Biochem. 195, 86 (1991) Abstract
 
 
ALX-380-042 Revised 05-May-08
Doxorubicin . hydrochloride
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SYNONYMS DXR . HCl
14-Hydroxydaunomycin . HCl
Adriamycin . HCl
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antitumor Antibiotics
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-380-042-M005   5 mg 60.00 USD Add To Cart
ALX-380-042-M010   10 mg 110.00 USD Add To Cart
ALX-380-042-M025   25 mg 250.00 USD Add To Cart
Product Specification
FORMULA: C27H29NO11 . HCl
MW: 543.5 . 36.5
CAS NUMBER: 25316-40-9
MERCK INDEX: 14: 3439
RTECS: QI9295900
SOURCE/HOST: Isolated from Streptomyces peucetius var. caesius.
PURITY: ≥98%
APPEARANCE: Red solid.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HAZARD: MAY BE CARCINOGENIC. MAY BE TERATOGENIC. TOXIC. MAY BE MUTAGENIC.

Product Description
Antitumor antibiotic. Induces DNA damage by intercalating into DNA and inhibiting topoisomerase II. Binds covalently to DNA. Inhbibits reverse transcriptase, RNA polymerase and the catalytic activity of Dnmt1. Immunosuppressive. Antineoplastic. Induces apoptosis.
Product Specific Literature References
Adriamycin and daunomycin induce programmed cell death (apoptosis) in tumour cells: A. Skladanowski & J. Konopa; Biochem. Pharmacol. 46, 375 (1993) Abstract
A critical evaluation of the mechanisms of action proposed for the antitumor effects of the anthracycline antibiotics adriamycin and daunorubicin: D.A. Gewirtz; Biochem. Pharmacol. 57, 727 (1999) Abstract
Doxorubicin treatment activates a Z-VAD-sensitive caspase, which causes deltapsim loss, caspase-9 activity, and apoptosis in Jurkat cells: S. Gamen, et al.; Exp. Cell Res. 258, 223 (2000) Abstract
Involvement of cyclin-dependent kinases in doxorubicin-induced apoptosis in human tumor cells: Y. Lu, et al.; Mol. Carcinog. 29, 1 (2000) Abstract
Characterization of Adriamycin-Induced G2 Arrest and Its Abrogation by Caffeine in FL-Amnion Cells with or without p53: Y. Minemoto, et al.; Exp. Cell Res. 262, 37 (2001) Abstract
Enhancement of Fas-mediated apoptosis in renal cell carcinoma cells by adriamycin: X.X. Wu, et al.; Cancer Res. 60, 2912 (2000) Abstract
Doxorubicin-induced apoptosis in endothelial cells and cardiomyocytes is ameliorated by nitrone spin traps and ebselen. Role of reactive oxygen and nitrogen species: S. Kotamraju, et al.; J. Biol. Chem. 275, 33585 (2000) Abstract; Full Text
The power and potential of doxorubicin-DNA adducts: S.M. Cutts, et al.; IUBMB Life 57, 73 (2005), Review Abstract
Adriamycin-induced interference with cardiac mitochondrial calcium homeostasis: K.B. Wallace; Cardiovasc. Toxicol. 7, 101 (2007), Review Abstract
Doxorubicin-induced cardiomyopathy from the cardiotoxic mechanisms to managemen: G. Takemura & H. Fujiwara; Prog. Cardiovasc. Dis. 49, 330 (2007), Review Abstract
Further Categories Containing This Product:
Other Toxins • Antitumor Agents (Enzyme Inhibitors) • Antitumor Agents (Apoptosis Inducers) • Antibiotics - Immunomodulators • Antibiotics - Topoisomerase Inhibitors • DNA Intercalators & Crosslinkers • Antibiotics - Apoptosis Inducers & Inhibitors • Antitumor Agents (DNA Interaction & Gene Regulation)
 
 
ALX-380-273 Revised 03-Apr-08
Doxycycline . hyclate
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SYNONYMS Doxycycline . hydrochloride . hemiethanolate . hemihydrate
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics for Angiogenesis Research
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-380-273-G001   1 g 20.00 USD Add To Cart
ALX-380-273-G005   5 g 60.00 USD Add To Cart
Product Specification
FORMULA: C22H24N2O8 . HCl . 0.5C2H6O . 0.5H2O
MW: 444.4 . 36.5 . 23.0 . 9.0
CAS NUMBER: 24390-14-5
MERCK INDEX: 14: 3440
RTECS: QI8925000
SOURCE/HOST: Semisynthetic from oxytetracycline.
PURITY: ≥98% (Assay on dry basis)
APPEARANCE: Yellow crystalline solid.
SOLUBILITY: Soluble in water (50mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Hygroscopic.
HAZARD: HARMFUL. MAY BE TERATOGENIC. MAY BE CARCINOGENIC.

Product Description
Broad spectrum antibiotic and bacteriostatic. Shows antiprotozoal properties. Potent inhibitor of MMPs (matrix metalloproteinases) in vivo. Inhibits collagen synthesis.
Product Specific Literature References
Alpha-6-deoxyoxytetracycline. I. Some biological properties: A.R. English; Proc. Soc. Exp. Biol. Med. 122, 1107 (1966) Abstract
A compilation of LD50 values in newborn and adult animals: E.I. Goldenthal; Toxicol. Appl. Pharmacol. 18, 185 (1971) Abstract
An efficacy trial of doxycycline chemoprophylaxis against leptospirosis: E.T. Takafuji, et al.; N. Engl. J. Med. 310, 497 (1984) Abstract
Specificity of the anticollagenase action of tetracyclines: relevance to their anti-inflammatory potential: K. Suomalainen, et al.; Antimicrob. Agents Chemother. 36, 227 (1992) Abstract
Matrix metalloproteinase-8 is expressed in rheumatoid synovial fibroblasts and endothelial cells. Regulation by tumor necrosis factor-alpha and doxycycline: R. Hanemaaijer, et al.; J. Biol. Chem. 272, 31504 (1997) Abstract; Full Text
Doxycycline and tissue repair in rats: S. Lamparter, et al.; J. Lab. Clin. Med. 139, 295 (2002) Abstract
Molecular interactions between matrilysin and the matrix metalloproteinase inhibitor doxycycline investigated by deuterium exchange mass spectrometry: R.A. Garcia, et al.; Mol. Pharmacol. 67, 1128 (2005) Abstract; Full Text
Doxycycline alters vascular smooth muscle cell adhesion, migration, and reorganization of fibrillar collagen matrices: C. Franco, et al.; Am. J. Pathol. 168, 1697 (2006) Abstract; Full Text
Doxycycline inhibits MMPs via modulation of plasminogen activators in focal cerebral ischemia: D. Burggraf, et al.; Neurobiol. Dis. 25, 506 (2007) Abstract
Further Categories Containing This Product:
Antitumor Agents (Anti-proliferative) • Antitumor Agents (Enzyme Inhibitors) • MMP Inhibitors • Antitumor Antibiotics
 
 
ALX-260-007 Revised 16-Feb-05
E-64
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SYNONYMS N-[N-(L-3-trans-Carboxyoxirane-2-carbonyl]-L-leucyl)-agmatine
L-trans-Epoxysuccinyl-leucylamide-(4-guanido)-butane
PRODUCT LINE Cancer
PRODUCT CATEGORY Cathepsin Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-260-007-M005   5 mg 55.00 USD Add To Cart
ALX-260-007-M025   25 mg 195.00 USD Add To Cart
Product Specification
FORMULA: C15H27N5O5
MW: 357.4
CAS NUMBER: 66701-25-5
SOURCE/HOST: Synthetic.
PURITY: ≥99%
SOLUBILITY: Soluble in DMSO or water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Irreversible inhibitor of cysteine proteinases like papain, cathepsin B and L. Acts by forming a thioether bond with the thiol of the active cysteine. Does not inhibit serine proteinases.
Product Specific Literature References