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ALX-380-212 Revised 10-Dec-07
Elaiophylin
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SYNONYMS Antibiotic 255-E
Antibiotic 5001B
Antibiotic 56-62
Antibiotic 846 I
SNA 4606-3
Azalomycin B
Gopalamicin
Salbomycin
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Antifungal
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-380-212-M001   1 mg 130.00 USD Add To Cart
ALX-380-212-M005   5 mg 390.00 USD Add To Cart
Product Specification
FORMULA: C54H88O18
MW: 1025.3
CAS NUMBER: 37318-06-2
RTECS: CL8380000
SOURCE/HOST: Isolated from Streptomyces hygroscopicus MST-AS5386.
PURITY: ≥95% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in 100% ethanol, methanol, dimethyl formamide or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: HARMFUL.

Product Description
Macrolide antibiotic inhibiting testosterone 5-reductase and plasma-proton ATPase (P-ATPase). Shows antifungal, antiprotozoal, antitumor, antihelmintic and immunosuppressive activity.
Product Specific Literature References
Melanosporin and elaiophylin, new antibiotics from Streptomyces malanosporus (sive melanosporofaciens) n. sp.: F.M. Arcamone, et al.; G. Microbiol. 7, 207 (1959)
Metabolic products of microorganisms. 200 Isolation and characterization of niphithricins A, B, and elaiophylin, antibiotics produced by Streptomyces violaceoniger: H.P. Fiedler, et al.; J. Antibiot. (Tokyo) 34, 1107 (1981) Abstract
Elaiophylin as a rumen fermentation efficiency enhancer: C.M. Liu, et al.; J. Antibiot. (Tokyo) 46, 350 (1993) Abstract
SNA-4606-1, a new member of elaiophylins with enzyme inhibition activity against testosterone 5 alpha-reductase: M. Nakakoshi, et al.; J. Antibiot. (Tokyo) 52, 175 (1999) Abstract
Enhancement of the antifungal activity of rapamycin by the coproduced elaiophylin and nigericin: A. Fang, et al.; J. Antibiot. (Tokyo) 53, 158 (2000) Abstract
Cation selective ion channels formed by macrodiolide antibiotic elaiophylin in lipid bilayer membranes: P.A. Grigoriev, et al.; Bioelectrochemistry 54, 11 (2001) Abstract
 
 
ALX-380-007 Revised 16-Jun-08
Enniatin B
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Ionophores
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ALX-380-007-M001   1 mg 130.00 USD Add To Cart
Product Specification
FORMULA: C33H57N3O9
MW: 639.8
CAS NUMBER: 917-13-5
MERCK INDEX: 14: 3585
SOURCE/HOST: Isolated from Fusarium orthoceras var. enniatum.
PURITY: ≥90% (HPLC)
APPEARANCE: White to off-white crystalline solid.
SOLUBILITY: Soluble in DMSO or other organic solvents; almost insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Ionophore antibiotic. Inhibitor of the S. cerevisiae ABC transporter Pdr5p.
Inhibitor of acyl-CoA-cholesterol acyltransferase and of phosphodiesterase. Potential anticancer compound.
Product Specific Literature References
Ionophore antibiotics produced by the fungus Fusarium orthoceras var. enniatum and other Fusaria: E. Gaumann, et al.; Experientia 3, 202 (1947)
"Sandwich" complexation in cyclopeptides and its implications in membrane processes: V.T. Ivanov; Ann. N. Y. Acad. Sci. 264, 221 (1975) Abstract
Interaction of cyclic peptides and depsipeptides with calmodulin: K.A. Mereish, et al.; Pept. Res. 3, 233 (1990) Abstract
Enniatin has a new function as an inhibitor of Pdr5p, one of the ABC transporters in Saccharomyces cerevisiae: K. Hiraga, et al.; Biochem. Biophys. Res. Commun. 328, 1119 (2005) Abstract
Enniatin exerts p53-dependent cytostatic and p53-independent cytotoxic activities against human cancer cells: R. Dornetshuber, et al.; Chem. Res. Toxicol. 20, 465 (2007) Abstract
 
 
ALX-350-254 Revised 10-Mar-08
Epoxomicin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Proteasome / Ubiquitin Modulators
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ALX-350-254-C050   50 µg 132.00 USD Add To Cart
Product Specification
FORMULA: C28H50N4O7
MW: 554.7
CAS NUMBER: 134381-21-8
MERCK INDEX: 14: 3630
SOURCE/HOST: Synthetic.
PURITY: ≥95% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO (15mg/ml); insoluble in water.
ACTIVITY: kobs/[I] = 25’000M-1s-1 versus 20S proteasome.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Avoid freeze/thaw cycles. Protect from light.
IDENTITY: Identity determined by 1H-NMR.

Product Description
Cell permeable, potent and selective proteasome inhibitor originally isolated from Actinomycetes strain based on its potent in vivo antitumor activity. More potent inhibitor of the chymotrypsin-like activity of the proteasome than lactacystin. Effectively inhibits NF-κB activation in vitro and potently blocks inflammation in vivo in the mouse ear edema assay.
Product Specific Literature References
Epoxomicin, a new antitumor agent of microbial origin: M. Hanada, et al.; J. Antibiot. (Tokyo) 45, 1746 (1992) Abstract
Proteasome inhibition by the natural products epoxomicin and dihydroeponemycin: insights into specificity and potency: K.B. Kim, et al.; Bioorg. Med. Chem. Lett. 9, 3335 (1999) Abstract
Epoxomicin, a potent and selective proteasome inhibitor, exhibits in vivo antiinflammatory activity: L. Meng, et al.; PNAS 96, 10403 (1999) Abstract
Total synthesis of the potent proteasome inhibitor epoxomicin: a useful tool for understanding proteasome biology: N. Sin, et al.; Bioorg. Med. Chem. Lett. 9, 2283 (1999) Abstract
The selective proteasome inhibitors lactacystin and epoxomicin can be used to either up- or down-regulate antigen presentation at nontoxic doses: K. Schwarz, et al.; J. Immunol. 164, 6147 (2000) Abstract
Establishment and some characteristics of epoxomicin (a proteasome inhibitor) resistant variants of the human squamous cell carcinoma cell line, A431: K. Ohkawa, et al.; Int. J. Oncol. 24, 425 (2004) Abstract
 
 
ALX-380-065 Revised 24-Sep-08
Fostriecin
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SYNONYMS Phosphotrienin
CI-920
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Topoisomerase Inhibitors
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ALX-380-065-C010   10 µg 150.00 USD Add To Cart
Product Specification
FORMULA: C19H26O9PNa
MW: 452.4
CAS NUMBER: 87860-39-7
RTECS: UQ0600000
SOURCE/HOST: Isolated from Streptomyces pulveraceous subsp. fostreus.
PURITY: ≥98% (HPLC)
APPEARANCE: Colorless solid.
SOLUBILITY: Soluble in water (50mg/ml), methanol (10mg/ml) or 100% ethanol (10mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least 1 year when stored at -20°C. Use fresh solution.
HANDLING: Protect from light. Packaged under inert gas. Hygroscopic.

Product Description
Antitumor antibiotic. Catalytic inhibitor of topoisomerase II. Strong protein phosphatase 2A (PP2A) inhibitor (IC50=3.2nM). Weak inhibitor for PP1 (IC50=131µM). No apparent effect on PP2B. The binding site for fostriecin on PP2A is different from that of okadaic acid (see Prod. No. ALX-350-003).
Product Specific Literature References
Novel antitumor agents CI-920, PD 113,270 and PD 113,271. II. Isolation and characterization: S.S. Stampwala, et al.; J. Antibiot. (Tokyo) 36, 1601 (1983) Abstract
Novel antitumor agents CI-920, PD 113,270 and PD 113,271. I. Taxonomy, fermentation and biological properties: J.B. Tunac, et al.; J. Antibiot. (Tokyo) 36, 1595 (1983) Abstract
Studies on the biochemical mechanism of the novel antitumor agent, CI- 920: D.W. Fry, et al.; Cancer Chemother. Pharmacol. 13, 171 (1984) Abstract
Anticancer activity of the structurally novel antibiotic Cl-920 and its analogues: W.R. Leopold, et al.; Cancer Res. 44, 1928 (1984) Abstract
Inhibition of type II topoisomerase by fostriecin: T.J. Boritzki, et al.; Biochem. Pharmacol. 37, 4063 (1988) Abstract
Comparison of effects of fostriecin, novobiocin, and camptothecin, inhibitors of DNA topoisomerases, on DNA replication and repair in human cells: C.M. Gedik & A.R. Collins; Nucl. Acids Res. 18, 1007 (1990) Abstract
The cell cycle related differences in susceptibility of HL-60 cells to apoptosis induced by various antitumor agents: W. Gorczyca, et al.; Cancer Res. 53, 3186 (1993) Abstract
Induction of DNA strand breaks associated with apoptosis during treatment of leukemias: W. Gorczyca, et al.; Leukemia 7, 659 (1993) Abstract
Antitumor drug fostriecin inhibits the mitotic entry checkpoint and protein phosphatases 1 and 2A: M. Roberge, et al.; Cancer Res. 54, 6115 (1994) Abstract
Fostriecin: a review of the preclinical data: R.S. de Jong, et al.; Anticancer Drugs 8, 413 (1997) Abstract
Fostriecin, an antitumor antibiotic with inhibitory activity against serine/threonine protein phosphatases types 1 (PP1) and 2A (PP2A), is highly selective for PP2A: A.H. Walsh, et al.; FEBS Lett. 416, 230 (1997) Abstract
Fostriecin, an inhibitor of protein phosphatase 2A, limits myocardial infarct size even when administered after onset of ischemia: C. Weinbrenner, et al.; Circulation 98, 899 (1998) Abstract
Phase I and pharmacokinetic study of the topoisomerase II catalytic inhibitor fostriecin: R.S. de Jong, et al.; Br. J. Cancer 79, 882 (1999) Abstract
Fostriecin: chemistry and biology: D.S. Lewy, et al.; Curr. Med. Chem. 9, 2005 (2002) Abstract
 
 
ALX-350-119 Revised 20-Feb-08
Fumagillin
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SYNONYMS Fumidil B
Fumadil B
TNP-470
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics for Angiogenesis Research
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ALX-350-119-MC05   0.5 mg 65.00 USD Add To Cart
ALX-350-119-M001   1 mg 105.00 USD Add To Cart
Product Specification
FORMULA: C26H34O7
MW: 458.6
CAS NUMBER: 23110-15-8
MERCK INDEX: 14: 4286
SOURCE/HOST: Isolated from Aspergillus fumigatus.
PURITY: ≥95%
APPEARANCE: Light yellow solid
SOLUBILITY: Soluble in chloroform or diluted aqueous bases. Slightly soluble in methanol and other alcoholic solvents. Insoluble in water.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Unstable in aqueous solutions with pH >9.0 or pH <5.0.
HANDLING: Packaged under inert gas. Protect from light.
HAZARD: HARMFUL.

Product Description
Inhibitor of angiogenesis and endothelial cell proliferation. Specific inhibitor of methionine aminopeptidase type II (MetAP-II). Antineoplastic. Anti-infective.
Product Specific Literature References
Fumagillin (H-3), a new antibiotic with amebicidal properties: C.M. Mc, et al.; Science 113, 202 (1951) Abstract
Synthetic analogues of fumagillin that inhibit angiogenesis and suppress tumour growth: D. Ingber, et al.; Nature 348, 555 (1990) Abstract
The anti-angiogenic agent fumagillin covalently modifies a conserved active-site histidine in the Escherichia coli methionine aminopeptidase: W.T. Lowther, et al.; PNAS 95, 12153 (1998) Abstract; Full Text
Molecular recognition of angiogenesis inhibitors fumagillin and ovalicin by methionine aminopeptidase 2: E.C. Griffith, et al.; PNAS 95, 15183 (1998) Abstract
Fumagillin treatment of intestinal microsporidiosis: J.M. Molina, et al.; N. Engl. J. Med. 346, 1963 (2002) Abstract
Whirling disease of salmonid fish: life cycle, biology, and disease: M.A. Gilbert & W.O. Granath, Jr.; J. Parasitol. 89, 658 (2003) Abstract
Fumagillin treatment of hepatocellular carcinoma in rats: an in vivo study of antiangiogenesis: I.S. Sheen, et al.; World J. Gastroenterol. 11, 771 (2005) Abstract
Fumagillin: an anti-infective as a parent molecule for novel angiogenesis inhibitors: B. Lefkove, et al.; Expert Rev. Anti Infect. Ther. 5, 573 (2007), Review Abstract
FGFR1/PI3K/AKT signaling pathway is a novel target for antiangiogenic effects of the cancer drug fumagillin (TNP-470): G.J. Chen, et al.; J. Cell Biochem. 101, 1492 (2007) Abstract
 
 
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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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-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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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.