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ALX-380-054 Revised 18-Jun-08
Geldanamycin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Protein Kinase Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-380-054-C100   100 µg 28.00 USD Add To Cart
ALX-380-054-C500   500 µg 50.00 USD Add To Cart
ALX-380-054-M001   1 mg 75.00 USD Add To Cart
ALX-380-054-M005   5 mg 300.00 USD Add To Cart
Product Specification
FORMULA: C29H40N2O9
MW: 560.6
CAS NUMBER: 30562-34-6
RTECS: LX8920000
SOURCE/HOST: Isolated from Streptomyces hygroscopicus.
PURITY: ≥96%
APPEARANCE: Yellow solid.
SOLUBILITY: Slightly soluble in methanol, chloroform or DMSO; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Potent antitumor antibiotic. Inhibitor of pp60src tyrosine kinase and of c-myc gene expression in murine lymphoblastoma cells. Inhibits the transforming activity of abl, erbB, fps, src, and yes. Binds specifically to heat shock protein 90 (HSP90) and to its endoplasmic reticulum homolog GP96 (GRP94). Capable of destabilizing several oncogene and proto-oncogene products. Potent inhibitor of the nuclear hormone receptor family. Protects against α-synuclein toxicity to dopaminergic neurons in Drosophila. Destabilizes mutant p53 protein from a number of breast, leukemic, and prostate cell lines. Inhibits basal and hypoxia-induced expression of c-Jun (IC50=75nM) and abolishes hypoxia-induced increase in c-Jun N-terminal kinase (JNK) activity. Inhibits telomerase activity through inhibition of HSP90, a chaperone required for the assembly and activation of telomerase in human cells. ~10-fold more potent than herbimycin A (Prod. No. ALX-350-029)
Product Specific Literature References
Geldanamycin, a new antibiotic: C. DeBoer, et al.; J. Antibiot. 23, 442 (1970) Abstract
Phenotypic change from transformed to normal induced by benzoquinonoid ansamycins accompanies inactivation of p60src in rat kidney cells infected with Rous sarcoma virus: Y. Uehara, et al.; Mol. Cell. Biol. 6, 2198 (1986) Abstract
Inhibition of c-myc gene expression in murine lymphoblastoma cells by geldanamycin and herbimycin, antibiotics of benzoquinoid ansamycin group: H. Yamaki, et al.; J.Antibiot. 42, 604 (1989) Abstract
Inhibition of heat shock protein HSP90-pp60v-src heteroprotein complex formation by benzoquinone ansamycins: essential role for stress proteins in oncogenic transformation: L. Whitesell, et al.; PNAS 91, 8324 (1994) Abstract
Geldanamycin selectively destabilizes and conformationally alters mutated p53: M.V. Blagosklonny, et al.; Oncogene 11, 933 (1995) Abstract
Inhibition of the oncogene product p185erbB-2 in vitro and in vivo by geldanamycin and dihydrogeldanamycin derivatives: R.C. Schnur, et al.; J. Med. Chem. 38, 3806 (1995) Abstract
p185erbB2 binds to GRP94 in vivo. Dissociation of the p185erbB2/GRP94 heterocomplex by benzoquinone ansamycins precedes depletion of p185erbB2: C. Chavany, et al.; J. Biol. Chem. 271, 4974 (1996) Abstract; Full Text
Stable and specific binding of heat shock protein 90 by geldanamycin disrupts glucocorticoid receptor function in intact cells: L. Whitesell & P. Cook; Mol. Endocrinol. 10, 705 (1996) Abstract
Geldanamycin as a potential anti-cancer agent: its molecular target and biochemical activity: L. Neckers, et al.; Invest. New Drugs 17, 361 (1999), (Review) Abstract
Hsp-90-associated oncoproteins: multiple targets of geldanamycin and its analogs: M.V. Blagosklonny; Leukemia 16, 455 (2002), (Review) Abstract
Pharmacological prevention of Parkinson disease in Drosophila: P.K. Auluck & N.M. Bonini; Nat. Med. 8, 1185 (2002) Abstract
Effects of geldanamycin on signaling through activator-protein 1 in hypoxic HT29 human colon adenocarcinoma cells: I.A. Vasilevskaya and P.J. O'Dwyer; Cancer Res. 59, 3935 (1999) Abstract
Inhibition of telomerase activity by geldanamycin and 17-allylamino, 17-demethoxygeldanamycin in human melanoma cells: R. Villa, et al.; Carcinogenesis 24, 851 (2003) Abstract
Chaperoning oncogenes: HSP90 as a target of geldanamycin: L. Neckers; Handb. Exp. Pharmacol. 259 (2006), (Review) Abstract
Geldanamycin interferes with the 90-kDa heat shock protein, affecting lipopolysaccharide-mediated interleukin-1 expression and apoptosis within macrophages: H.Y. Hsu, et al.; Mol. Pharmacol. 71, 344 (2007) Abstract; Full Text
Relationship among ligand conformations in solution, in the solid state, and at the Hsp90 binding site: geldanamycin and radicicol: P. Thepchatri, et al.; JACS 129, 3127 (2007) Abstract
Inhibition of heat shock protein 90 impairs epidermal growth factor-mediated signaling in gastric cancer cells and reduces tumor growth and vascularization in vivo: S.A. Lang, et al.; Mol. Cancer Ther. 6, 1123 (2007) Abstract; Full Text
Geldanamycin, a heat-shock protein 90-binding agent, induces thymocyte apoptosis through destabilization of Lck in presence of 12-O-tetradecanoylphorbol 13-acetate: K. Ohta, et al.; Biomed. Res. 28, 33 (2007) Abstract; Full Text
Low dose geldanamycin inhibits hepatocyte growth factor and hypoxia-stimulated invasion of cancer cells: F. Koga, et al.; Cell Cycle 6, 1393 (2007) Abstract
The heat-shock protein 90 inhibitor, geldanamycin, induces apoptotic cell death in Epstein-Barr virus-positive NK/T-cell lymphoma by Akt down-regulation: Y.K. Jeon, et al.; J. Pathol. 213, 170 (2007) Abstract
Geldanamycin, a HSP90 inhibitor, attenuates the hypoxia-induced vascular endothelial growth factor expression in retinal pigment epithelium cells in vitro: W.C. Wu, et al.; Exp. Eye Res. 85, 721 (2007) Abstract
HSP90 antagonist, geldanamycin, inhibits proliferation, induces apoptosis and blocks migration of rhabdomyosarcoma cells in vitro and seeding into bone marrow in vivo: E. Lesko, et al.; Anticancer Drugs 18, 1173 (2007) Abstract
Geldanamycin enhances hepatocyte growth factor stimulation of eNOS phosphorylation in endothelial cells: K. Makondo, et al.; Eur. J. Pharmacol. 582, 110 (2007) Abstract
Hsp90-inhibitor geldanamycin abrogates G(2) arrest in p53-negative leukemia cell lines through the depletion of Chk1: K. Sugimoto, et al.; Oncogene 27, 3091 (2008) Abstract
 
 
ALX-350-150 Revised 16-Jun-08
Gelonin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antitumor Reagents
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ALX-350-150-M001   1 mg 190.00 USD Add To Cart
Product Specification
MW: ~30kDa
CAS NUMBER: 75037-46-6
SOURCE/HOST: Isolated from Gelonium multiflorum.
CONCENTRATION: 2.1mg/ml
PURITY: ≥95%
FORMULATION: Liquid. In 5mM phosphate buffer, pH 6.5, containing 5mM EDTA and 120mM sodium chloride.
SHIPPING: SHIPPED ON DRY ICE
LONG TERM STORAGE: -80°C
HAZARD: HARMFUL.
Product Description
Type I ribosome inactivating protein (RIP). Depurinates RNA in ribosomes, thus inhibiting protein synthesis in eukaryotic cells, which results in cell death. Widely used to construct immunotoxins composed of cell-targeted antibodies. As a type I RIP it lacks the lectin subunit and is practically non-toxic to intact cells. Inhibits cell-free protein synthesis in reticulocyte assay with globin messenger (IC50=2.7ng/ml).
Product Specific Literature References
Gelonin, a new inhibitor of protein synthesis, nontoxic to intact cells. Isolation, characterization, and preparation of cytotoxic complexes with concanavalin: A: F. Stirpe, et al.; J. Biol. Chem. 255, 6947 (1980) Abstract; Full Text
The antileukemic efficacy of an immunotoxin composed of a monoclonal anti-Thy-1 antibody disulfide linked to the ribosome-inactivating protein gelonin: C.F. Scott, Jr., et al.; Cancer Immunol. Immunother. 25, 31 (1987) Abstract
Requirements for the inactivation of ribosomes by gelonin: S. Sperti, et al.; Biochem. J. 277, 281 (1991) Abstract; Full Text
Monoclonal antibodies to gelonin: production and characterization: J. Zimmermann & W.E. Trommer; Hybridoma 10, 65 (1991) Abstract
Toxin-targeted design for anticancer therapy. II: Preparation and biological comparison of different chemically linked gelonin-antibody conjugates: L. Delprino, et al.; J. Pharm. Sci. 82, 699 (1993) Abstract
Cloning and expression of a gene encoding gelonin, a ribosome-inactivating protein from Gelonium multiflorum: P.A. Nolan, et al.; Gene 134, 223 (1993) Abstract
Structural characterization of gelonin: evidence for separate antigenic and cytotoxic domains: M.R. Sairam, et al.; Biochem. Mol. Biol. Int. 31, 575 (1993) Abstract
Antigen-specific therapy of experimental myasthenia gravis with acetylcholine receptor-gelonin conjugates in vivo: I.L. Urbatsch, et al.; Eur. J. Immunol. 23, 776 (1993) Abstract
Gelonin analogs with engineered cysteine residues form antibody immunoconjugates with unique properties: M. Better, et al.; J. Biol. Chem. 269, 9644 (1994) Abstract
Amino acid sequence analysis, gene construction, cloning, and expression of gelonin, a toxin derived from Gelonium multiflorum: M.G. Rosenblum, et al.; J. Interferon Cytokine Res. 15, 547 (1995) Abstract
Direct evidence for the deoxyribonuclease activity of the plant ribosome inactivating protein gelonin: E. Nicolas, et al.; FEBS Lett. 406, 162 (1997) Abstract
A new class of DNA glycosylase/apurinic/apyrimidinic lyases that act on specific adenines in single-stranded DNA: E. Nicolas, et al.; J. Biol. Chem. 273, 17216 (1998) Abstract; Full Text
Identity elements in bovine tRNA(Trp) required for the specific stimulation of gelonin, a plant ribosome-inactivating protein: M. Brigotti, et al.; RNA 5, 1357 (1999) Abstract; Full Text
Comparative cytotoxicity and pharmacokinetics of antimelanoma immunotoxins containing either natural or recombinant gelonin: M.G. Rosenblum, et al.; Cancer Chemother. Pharmacol. 44, 343 (1999) Abstract
Purification and characterisation of gelonin from seeds of Gelonium multiflorum: V. Singh, et al.; Indian J. Biochem. Biophys. 36, 258 (1999) Abstract
Gelonin is an unusual DNA glycosylase that removes adenine from single-stranded DNA, normal base pairs and mismatches: E. Nicolas, et al.; J. Biol. Chem. 275, 31399 (2000) Abstract; Full Text
Intein-mediated fusion expression, high efficient refolding, and one-step purification of gelonin toxin: C. Guo, et al.; Protein Expr. Purif. 37, 361 (2004) Abstract
On the contentious sequence and glycosylation motif of the ribosome inactivating plant protein gelonin: T. Daubenfeld, et al.; BBRC 333, 984 (2005) Abstract
Novel immunotoxin: a fusion protein consisting of gelonin and an acetylcholine receptor fragment as a potential immunotherapeutic agent for the treatment of Myasthenia gravis: M. Hossann, et al.; Protein Expr. Purif. 46, 73 (2006) Abstract
Multimodality molecular imaging of glioblastoma growth inhibition with vasculature-targeting fusion toxin VEGF121/rGel: A.R. Hsu, et al.; J. Nucl. Med. 48, 445 (2007) Abstract
Further Categories Containing This Product:
Antitumor Agents (Anti-proliferative)Natural Proteins
 
 
ALX-350-006 Revised 05-Apr-08
Genistein (synthetic)
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SYNONYMS 4',5,7-Trihydroxyisoflavone
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-350-006-M010   10 mg 25.00 USD Add To Cart
ALX-350-006-M025   25 mg 50.00 USD Add To Cart
ALX-350-006-M050   50 mg 90.00 USD Add To Cart
ALX-350-006-M100   100 mg 150.00 USD Add To Cart
ALX-350-006-G001   1 g 480.00 USD Add To Cart
Product Specification
FORMULA: C15H10O5
MW: 270.2
CAS NUMBER: 446-72-0
MERCK INDEX: 14: 4391
RTECS: NR2392000
SOURCE/HOST: Synthetic.
PURITY: ≥99% (HPLC)
APPEARANCE: White to yellow crystalline powder.
SOLUBILITY: Soluble in DMSO, 100% ethanol or dilute aqueous base; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.
HAZARD: MAY BE CARCINOGENIC. HARMFUL.

Product Description
Tyrosine protein kinase inhibitor. Inhibits phosphorylation of EGFR kinase. Inhibits tumor cell proliferation and induces tumor cell differentiation. Inhibits topoisomerase II activity in vivo. Produces cell cycle arrest and apoptosis. Direct inhibitor of insulin-induced glucose uptake in adipocytes (IC50=20µM).
Product Specific Literature References
Genistein, a specific inhibitor of tyrosine-specific protein kinases: T. Akiyama, et al.; J. Biol. Chem. 262, 5592 (1987) Abstract; Full Text
Erbstatin blocks platelet activating factor-induced protein-tyrosine phosphorylation, polyphosphoinositide hydrolysis, protein kinase C activation, serotonin secretion and aggregation of rabbit platelets: H. Salari, et al.; FEBS Lett. 263, 104 (1990) Abstract
Mechanisms of cancer chemoprevention by soy isoflavone genistein: F.H. Sarkar & Y. Li; Cancer Metastasis Rev. 21, 265 (2002) Abstract
Soy isoflavone phyto-pharmaceuticals in interleukin-6 affections. Multi-purpose nutraceuticals at the crossroad of hormone replacement, anti-cancer and anti-inflammatory therapy: N. Dijsselbloem, et al.; Biochem. Pharmacol. 68, 1171 (2004), Review Abstract
Genistein affects testosterone secretion by Leydig cells in roosters (Gallus gallus domesticus): M. Opalka, et al.; Reprod. Biol. 4, 185 (2004) Abstract
Genistein directly inhibits GLUT4-mediated glucose uptake in 3T3-L1 adipocytes: M. Bazuine, et al.; BBRC 325, 511 (2005) Abstract
Decreased circulating levels of tumor necrosis factor-alpha in postmenopausal women during consumption of soy-containing isoflavones: Y. Huang, et al.; J. Clin. Endocrinol. Metab. 90, 3956 (2005) Abstract
Phytoestrogens and lipoproteins in women: C.N. Bairey Merz, et al.; J. Clin. Endocrinol. Metab. 91, 2209 (2006) Abstract
Clinical review: a critical evaluation of the role of soy protein and isoflavone supplementation in the control of plasma cholesterol concentrations: A. Dewell, et al.; J. Clin. Endocrinol. Metab. 91, 772 (2006), Review Abstract
The role of genistein and synthetic derivatives of isoflavone in cancer prevention and therapy: F.H. Sarkar, et al.; Mini Rev. Med. Chem. 6, 401 (2006), Review Abstract
 
 
ALX-350-247 Revised 21-May-08
Genistin
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SYNONYMS Genistein-7-O-glucoside
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-247-M010   10 mg 180.00 USD Add To Cart
Product Specification
FORMULA: C21H20O10
MW: 432.4
CAS NUMBER: 529-59-9
MERCK INDEX: 14: 4391
PURITY: ≥98%
APPEARANCE: Off-white to light yellow powder.
SOLUBILITY: Soluble in DMSO or dilute aqueous base; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Glucoside of genistein (Prod. No. ALX-350-006) found in soy beans. Useful as a negative control for genistein and other tyrosine kinase inhibitors. Selective inhibitor of terminal deoxyribonucleotidyltransferase (TdT). Displays antioxidant and anticarcinogenic properties.
Product Specific Literature References
Soybean isoflavones, genistein and genistin, inhibit rat myoblast proliferation, fusion and myotube protein synthesis: S. Ji, et al.; J. Nutr. 129, 1291 (1999) Abstract
Daidzein and genistein but not their glucosides are absorbed from the rat stomach: M.K. Piskula, et al.; FEBS Lett. 447, 287 (1999) Abstract
Inhibition of CYP1A1 enzyme activity in mouse hepatoma cell culture by soybean isoflavones: H.G. Shertzer, et al.; Chem. Biol. Interact. 123, 31 (1999) Abstract
Selective inhibitors of terminal deoxyribonucleotidyltransferase (TdT): baicalin and genistin: Y. Uchiyama, et al.; Biochim. Biophys. Acta 1725, 298 (2005) Abstract
Genistin inhibits UV light-induced plasmid DNA damage and cell growth in human melanoma cells: A. Russo, et al.; J. Nutr. Biochem. 17, 103 (2006) Abstract
Pro-apoptotic effect and cytotoxicity of genistein and genistin in human ovarian cancer SK-OV-3 cells: E.J. Choi, et al.; Life Sci. 80, 1403 (2007) Abstract
 
 
ALX-380-228 Revised 09-Jun-08
Gilvocarcin M
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SYNONYMS Anandimycin B
Toromycin B
Antibiotic 1072A
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Other Antibiotics - DNA Regulation/Transcription
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ALX-380-228-MC05   0.5 mg 360.00 USD Add To Cart
Product Specification
FORMULA: C26H26O9
MW: 482.5
CAS NUMBER: 77879-89-1
RTECS: DI2250000
SOURCE/HOST: Isolated from Streptomyces sp. MST-AS5353.
PURITY: ≥95% (HPLC)
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in dimethyl formamide or DMSO; slightly soluble in methanol or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: HARMFUL.

Product Description
Antibiotic. Has antibacterial, antifungal, antiviral and antitumor activities. Interacts with DNA. Less active than gilvocarcin V (Prod. No. ALX-380-113).
Product Specific Literature References
Gilvocarcins, new antitumor antibiotics. 1. Taxonomy, fermentation, isolation and biological activities: H. Nakano, et al.; J. Antibiot. (Tokyo) 34, 266 (1981) Abstract
Activation of antitumor agent gilvocarcins by visible light: R.K. Elespuru and S.K. Gonda; Science 223, 69 (1984) Abstract
Photophysical properties of gilvocarcins V and M and their binding constant to calf thymus DNA: R. Oyola, et al.; Photochem. Photobiol. 65, 802 (1997) Abstract
 
 
ALX-380-113 Revised 16-Jun-08
Gilvocarcin V
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SYNONYMS Anandimycin A
Toromycin
B 21085
Antibiotic 1072B
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Other Antibiotics - DNA Regulation/Transcription
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-380-113-C250   250 µg 180.00 USD Add To Cart
ALX-380-113-M001   1 mg 540.00 USD Add To Cart
Product Specification
FORMULA: C27H26O9
MW: 494.5
CAS NUMBER: 77879-90-4; 84236-01-1
RTECS: DI2240000
SOURCE/HOST: Isolated from Streptomyces sp.
PURITY: ≥98% (HPLC)
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Stock solutions are stable for at least 3 months when stored at -20°C.
HANDLING: Protect from light also when in solution.
HAZARD: HARMFUL.

Product Description

Antibiotic. Cytotoxic against Gram-positive bacteria. Mediates a unique cross-linking reaction between DNA and histidine H3. Weakly active against Gram-negative bacteria, fungi and tumors. Antineoplastic and photosensitizing compound.

Product Specific Literature References
Gilvocarcins, new antitumor antibiotics. 1. Taxonomy, fermentation, isolation and biological activities: H. Nakano, et al.; J. Antibiot. (Tokyo) 34, 266 (1981) Abstract
Activation of antitumor agent gilvocarcins by visible light: R.K. Elespuru and S.K. Gonda; Science 223, 69 (1984) Abstract
Photosensitized DNA breaks and DNA-to-protein crosslinks induced in human cells by antitumor agent gilvocarcin V: M.J. Peak, et al.; Chem. Biol. Interact. 67, 267 (1988) Abstract
Biochemical characterisation of elsamicin and other coumarin-related antitumour agents as potent inhibitors of human topoisomerase II: A. Lorico & B. H. Long; Eur. J. Cancer 29A, 1985 (1993) Abstract
Photophysical properties of gilvocarcins V and M and their binding constant to calf thymus DNA: R. Oyola, et al.; Photochem. Photobiol. 65, 802 (1997) Abstract
Histone H3 and heat shock protein GRP78 are selectively cross-linked to DNA by photoactivated gilvocarcin V in human fibroblasts: A. Matsumoto and P.C. Hanawalt; Cancer Res. 60, 3921 (2000) Abstract; Full Text
 
 
ALX-850-278 Revised 24-Feb-05
Glutathione S-transferase Assay Kit
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SYNONYMS GST Assay Kit
PRODUCT LINE Cancer
PRODUCT CATEGORY Glutathione S-Transferase
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ALX-850-278-KI01   1 Kit 349.00 USD Add To Cart
Product Specification
QUANTITY: 96 wells (~80 tests).
APPLICATION: For the measurement of glutathione S-transferase (GST) activity in plasma, erythrocyte lysates, tissue homogenates and cell lysates.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
Further Categories Containing This Product:
Glutathione/Related ProductsActivity Assays
 
 
ALX-350-113 Revised 28-May-08
Gossypol
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SYNONYMS 2,2’-bis[8-Formyl-1,6,7-trihydroxy-5-isopropyl-3-
methylnaphthalene]
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antitumor Reagents
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ALX-350-113-M100   100 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C30H30O8
MW: 518.6
CAS NUMBER: 303-45-7
MERCK INDEX: 14: 4528