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Antibiotics for Cancer Research
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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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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
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
Further Categories Containing This Product:
Antibiotics - Antiviral / Anti-HIV • Antitumor Agents (Apoptosis Inducers) • Hypoxia-inducible Factor [HIF] / Related Products • Antibiotics - Antifungal • Antitumor Antibiotics
 
 
ALX-380-115 Revised 03-Apr-08
Echinosporin
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SYNONYMS NSC357683
XK 213
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antitumor Antibiotics
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ALX-380-115-M001   1 mg 90.00 USD Add To Cart
ALX-380-115-M005   5 mg 360.00 USD Add To Cart
Product Specification
FORMULA: C10H9NO5
MW: 223.2
CAS NUMBER: 79127-35-8
RTECS: JW5313000
SOURCE/HOST: Isolated from Streptomyces sp.
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in dimethyl formamide, methanol or water.
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.
HAZARD: HARMFUL.

Product Description
Antitumor antibiotic. Inhibits cell cycle at the G(2)/M phase and induces apoptosis.
Product Specific Literature References
A new antibiotic echinosporin (XK-213) - producing organism, isolation and characterization: T. Sato, et al.; J. Antibiot. 35, 266 (1982) Abstract
Antitumor activity of echinosporin: M. Morimoto and R. Imai; J. Antibiot. 38, 490 (1985) Abstract
Approaches to the total synthesis of the antitumor antibiotic echinosporin: M. A. Kinsella; J. Org. Chem. 55, 105 (1990)
Applications of an asymmetric [2 + 2]-photocycloaddition. Total synthesis of (-)-echinosporin. Construction of an advanced 11-deoxyprostaglandin intermediate: A. B. Smith; JACS 114, 2567 (1992)
Biosynthesis of the antibiotic echinosporin by a novel branch of the shikimate pathway: A. Dubeler; Eur. J. Org. Chem. 2002, 983 (2002)
Echinosporins as new cell cycle inhibitors and apoptosis inducers from marine-derived Streptomyces albogriseolus: C.B. Cui, et al.; Fitoterapia 78, 238 (2007) Abstract
Further Categories Containing This Product:
Antibiotics - Apoptosis Inducers & Inhibitors • Antibiotics for Cell Cycle Research
 
 
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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ALX-380-212-M001   1 mg 170.00 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
Further Categories Containing This Product:
Antibiotics - Immunomodulators • Helminth Infections / Related Products • Antitumor Antibiotics • Antibiotics - ATPase Inhibitors
 
 
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
Further Categories Containing This Product:
Other Toxins • MDR Inhibitors • Antibiotics - Other Signal Transduction Pathway Modulators • Antitumor Antibiotics
 
 
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
Further Categories Containing This Product:
Antitumor Agents (Enzyme Inhibitors) • Proteasome / Related Products • Anti-inflammatory Agents Other Products • NF-kB Pathway Inhibitors • Antibiotics for Inflammation Research • Antibiotics - NF-kB Inhibitors • Antitumor Antibiotics
 
 
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
Further Categories Containing This Product:
Antitumor Agents (Enzyme Inhibitors) • Antibiotics - Other Signal Transduction Pathway Modulators • PP2A / Related Products • Antitumor Antibiotics
 
 
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
Further Categories Containing This Product:
Aminopeptidases / Related Products • Antitumor Agents (Anti-proliferative) • Fibroblast Growth Factors [FGFs] & Receptors / Related Products • Natural Products - Other Anti-infective Agents • Antitumor Antibiotics
 
 
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: