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Antibiotics for Cancer Research
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ALX-260-128 Revised 03-Apr-08
Actinonin
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SYNONYMS 3[[1-[[2-(Hydroxymethyl)-1-pyrrolidinyl]-carbonyl]-2-methylpropyl]-carbamoyl]-octanohydroxamic acid
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antitumor Antibiotics
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ALX-260-128-M005   5 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C19H35N3O5
MW: 385.5
CAS NUMBER: 13434-13-4
SOURCE/HOST: Synthetic.
PURITY: ≥98%
APPEARANCE: White powder.
SOLUBILITY: Soluble in 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Inhibitor of aminopeptidase M, leucine aminopeptidase and deformylase. Shows antitumor activity. Apoptosis inducer.
Product Specific Literature References
Production of actinonin, an inhibitor of aminopeptidase M, by actinomycetes: H. Umezawa, et al.; J. Antibiot. (Tokyo) 38, 1629 (1985) Abstract
Analgesic effect of actinonin, a new potent inhibitor of multiple enkephalin degrading enzymes: M. Hachisu, et al.; Life Sci. 41, 235 (1987) Abstract
Effects of an antibiotic protease inhibitor, actinonin on the growth within collagen gels of non-metastatic and metastatic mouse mammary tumors of the same origin: K. Sayama, et al.; Cancer Lett 94, 171 (1995) Abstract
Inhibition of alanyl aminopeptidase induces MAP-kinase p42/ERK2 in the human T cell line KARPAS-299: U. Lendeckel, et al.; BBRC 252, 5 (1998) Abstract
Antitumor activity of actinonin in vitro and in vivo: Y. Xu, et al.; Clin. Cancer Res. 4, 171 (1998) Abstract
Actinonin, a naturally occurring antibacterial agent, is a potent deformylase inhibitor: D.Z. Chen, et al.; Biochemistry 39, 1256 (2000) Abstract
Human mitochondrial peptide deformylase, a new anticancer target of actinonin-based antibiotics: M.D. Lee, et al.; J. Clin. Invest. 114, 1107 (2004) Abstract
Actinonin induces apoptosis in U937 leukemia cells: M. Grujic, et al.; Cancer Lett. 223, 211 (2005) Abstract
Further Categories Containing This Product:
Aminopeptidases / Related Products • Natural Products - Apoptosis Inducers & Inhibitors • Antitumor Agents (Enzyme Inhibitors)
 
 
ALX-270-346 Revised 28-May-08
Ratjadone A (synthetic)
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics for Cell Cycle Research
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ALX-270-346-C002   2 µg 150.00 USD Add To Cart
Product Specification
FORMULA: C28H40O5
MW: 456.6
CAS NUMBER: 163564-92-9
SOURCE/HOST: Synthetic.
PURITY: ≥95%
FORMULATION: Liquid. Solution in methanol.
SOLUBILITY: Soluble in methanol (20mg/ml) or aqueous buffers (<100µM).
SHIPPING: SHIPPED ON DRY ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Sensitive to acids and bases. Unstable in acidic buffer systems (pH<6). Stable in substance as oil and in solution in methanol at -20°C.
HANDLING: Protect from light.
HAZARD: TOXIC.

Product Description
Represents a new class of natural compounds, which inhibit proliferation in eukaryotes by blocking nuclear export. As potent as leptomycin B (Prod. No. ALX-380-100) and specific for G1/S checkpoint. Cytotoxic secondary metabolite (IC50=50pg/ml in mouse cell line L929) that arrests tumor cells in the G1 phase at remarkably low concentrations (50pg/ml in HeLa cell line KB3.1). Inhibits the binding between the nuclear export signal (NES) of proteins and the chromosome maintenance region protein (CRM1). Anticancer compound. Belongs to the family of orphan ligands which include polyketides like leptomycin B, callystatin A and other related compounds.
Product Specific Literature References
Antibiotics from gliding bacteria, LXIII. Ratjadone: a new antifungal metabolite from Sorangium cellulosum: D. Schummer, et al.; Liebigs Ann. 685 (1995)
Ratjadon: a new antifungal compound from Sorangium cellulosum (myxobacteria) production, physio-chemical and biological properties: J. Gerth, et al.; J. Antibiot. 48, 973 (1995) Abstract
The chemistry and biology of ratjadone: M. Kalesse, et al.; ChemBioChem. 9, 709 (2001) Abstract
The chemistry and biology of the leptomycin family: M. Kalesse & M. Christmann; Synthesis 8, 981 (2002) Abstract
Ratjadone and leptomycin B block CRM1-dependent nuclear export by identical mechanisms: T. Meissner, et al.; FEBS Lett. 576, 27 (2004)
Nuclear targeting of adenovirus type 2 requires CRM1-mediated nuclear export: S. Strunze, et al.; Mol. Biol. Cell 16, 2999 (2005) Abstract
Further Categories Containing This Product:
Antitumor Antibiotics • Antibiotics - Antifungal • Cell Cycle Blockers & Inhibitors / Related Products • Nuclear Envelope & Nuclear Transport • Antitumor Agents (Anti-proliferative)
 
 
ALX-270-369 Revised 28-May-08
Ratjadone C (native)
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics for Cell Cycle Research
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ALX-270-369-C005   5 µg 180.00 USD Add To Cart
Product Specification
FORMULA: C28H40O5
MW: 456.6
SOURCE/HOST: Isolated from Sorangium cellulosum.
PURITY: ≥95%
FORMULATION: Liquid. Solution in methanol (5µg in 1ml).
SOLUBILITY: Soluble in methanol (>50mg/ml). Sparingly soluble in aqueous buffers (up to 10µg/ml in PBS).
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Acid and base sensitive. Unstable in acidic and alkaline buffer systems (pH <6 or >7). Stable in methanolic solution at -20°C.
HANDLING: Protect from light.
HAZARD: TOXIC.

Product Description
Cytotoxic secondary metabolite that inhibits cell growth of mammalian cell lines in the picomolar range (IC50=0.2ng/ml with L929 mouse cells) including multidrug resistant (MDR) HeLa cells (IC50=0.1ng/ml with KB-V1). Like leptomycin B (Prod. No. ALX-380-100), ratjadone C binds covalently to the nuclear export protein CRM1. It inhibits cargo protein binding to the leucine-rich nuclear export sequence and thereby blocks nuclear export.
Product Specific Literature References
Antibiotics from gliding bacteria, LXIII. Ratjadone: a new antifungal metabolite from Sorangium cellulosum: D. Schummer, et al.; Liebigs Ann. 685 (1995)
Ratjadon: a new antifungal compound from Sorangium cellulosum (myxobacteria) production, physico-chemical and biological properties: K. Gerth, et al.; J. Antibiot. (Tokyo) 48, 973 (1995) Abstract
The chemistry and biology of the leptomycin family: M. Kalesse & M. Christmann; Synthesis 8, 981 (2002) Abstract
Ratjadones inhibit nuclear export by blocking CRM1/exportin 1: M. Koster, et al.; Exp. Cell. Res. 286, 321 (2003) Abstract
Further Categories Containing This Product:
Antitumor Antibiotics • Antibiotics - Antifungal • Cell Cycle Blockers & Inhibitors / Related Products • Nuclear Envelope & Nuclear Transport • Antitumor Agents (Anti-proliferative)
 
 
ALX-350-019 Revised 16-Oct-08
(+)-Brefeldin A
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SYNONYMS BFA
Ascotoxin
Decumbin
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Apoptosis Inducers & Inhibitors
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ALX-350-019-M005   5 mg 80.00 USD Add To Cart
ALX-350-019-M010   10 mg 130.00 USD Add To Cart
ALX-350-019-M025   25 mg 270.00 USD Add To Cart
ALX-350-019-M050   50 mg 420.00 USD Add To Cart
Product Specification
FORMULA: C16H24O4
MW: 280.4
CAS NUMBER: 20350-15-6
MERCK INDEX: 14: 1369
SOURCE/HOST: Isolated from Eupenicillium brefeldianum.
PURITY: ≥97% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO, methanol, acetone or ethyl acetate.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: HARMFUL.

Product Description
Inhibitor of intracellular protein transport and protein secretion, interfering with trafficking in the trans-Golgi network, leading to the accumulation of cycling proteins in ERGIC clusters. Blocks ADP-ribosylation factor (Arf) in an inactive GDP-bound conformation and thereby prevents binding of COPI coats to ERGIC and Golgi membranes. Upon brefeldin A treatment the Golgi rapidly tubulates and fuses with the ER by an energy-, temperature-, and microtubule-dependent process. In contrast, the drug has little effect on the ERGIC, which keeps its identity, although the ERGIC clusters become larger and more uniformly distributed in the cytoplasm of the cells. Inhibits intracellular collagen degradation. Also inhibits apical Na+ channels in epithelia. Induces apoptosis.
Product Specific Literature References
Decumbin, a new compound from a species of Penicillium: V.L. Singleton, et al.; Nature 181, 1072 (1958)
Über die Isolierung neuer Stoffwechselprodukte aus Penicillium brefeldianum Dodge.: E. Harri, et al.; Helv. Chim. Acta 46, 1235 (1963)
Novel blockade by brefeldin A of intracellular transport of secretory proteins in cultured rat hepatocytes: Y. Misumi, et al.; J. Biol. Chem. 261, 11398 (1986) Abstract; Full Text
Brefeldin A causes disassembly of the Golgi complex and accumulation of secretory proteins in the endoplasmic reticulum: T. Fujiwara, et al.; J. Biol. Chem. 263, 18545 (1988) Abstract; Full Text
Brefeldin A, thapsigargin, and AIF4- stimulate the accumulation of GRP78 mRNA in a cycloheximide dependent manner, whilst induction by hypoxia is independent of protein synthesis: B.D. Price, et al.; J. Cell. Physiol. 152, 545 (1992) Abstract
Brefeldin A and the endocytic pathway. Possible implications for membrane traffic and sorting: W. Hunziker, et al.; FEBS Lett. 307, 93 (1992), (Review) Abstract
Brefeldin A inhibits degradation as well as production and secretion of collagen in human lung fibroblasts: C.R. Ripley, et al.; J. Biol. Chem. 268, 3677 (1993) Abstract
Brefeldin A is a potent inducer of apoptosis in human cancer cells independently of p53: R.G. Shao, et al.; Exp. Cell Res. 227, 190 (1996) Abstract
Brefeldin A inhibition of apical Na+ channels in epithelia: R.S. Fisher, et al.; Am. J. Physiol. 270, C138 (1996) Abstract
Brefeldin A: deciphering an enigmatic inhibitor of secretion: A. Nebenfuhr, et al.; Plant Physiol. 130, 1102 (2002), Review Abstract
NKT cells provide help for dendritic cell-dependent priming of MHC class I-restricted CD8+ T cells in vivo: D. Stober, et al.; J. Immunol. 170, 2540 (2003) Abstract; Full Text
Interaction of BIG2, a brefeldin A-inhibited guanine nucleotide-exchange protein, with exocyst protein Exo70: K.F. Xu, et al.; PNAS 102, 2784 (2005) Abstract
Further Categories Containing This Product:
ADP Ribosylation Factor [ARF] / Related Products • Golgi Apparatus • Collagen / Related Products • Na+ Channels • Antitumor Antibiotics • Antibiotics - Antiviral / Anti-HIV • Antibiotics - Antifungal • Autophagy Other Products • Antitumor Agents (Apoptosis Inducers)
 
 
ALX-350-029 Revised 07-Oct-08
Herbimycin A
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Protein Kinase Inhibitors
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ALX-350-029-C100   100 µg 110.00 USD Add To Cart
ALX-350-029-M001   1 mg 560.00 USD Add To Cart
Product Specification
FORMULA: C30H42N2O9
MW: 574.7
CAS NUMBER: 70563-58-5
RTECS: LX8930000
SOURCE/HOST: Isolated from Streptomyces sp.
PURITY: ≥97%
APPEARANCE: Yellow powder.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.

Product Description
Antibiotic. Cell permeable tyrosine kinase inhibitor. Inhibitor of HSP90, NF-κB activation and angiogenesis. Increases the sensitivity of certain cancer cells to chemotherapeutic agents. Blocks mitotic activity. Neurotoxic.
Product Specific Literature References
Herbimycin, a new antibiotic produced by a strain of Streptomyces: S. Omura, et al.; J. Antibiot. (Tokyo) 32, 255 (1979) Abstract
A new activity of herbimycin A: inhibition of angiogenesis: T. Yamashita, et al.; J. Antibiot. (Tokyo) 42, 1015 (1989) Abstract
Stimulation by Bt2cAMP of epidermal mucous metaplasia in retinol- pretreated chick embryonic cultured skin, and its inhibition by herbimycin A, an inhibitor for protein-tyrosine kinase: A. Obinata, et al.; Exp. Cell. Res. 193, 36 (1991) Abstract
IgE-induced tyrosine phosphorylation of phospholipase C-gamma 1 in rat basophilic leukemia cells: D.J. Park, et al.; J. Biol. Chem. 266, 24237 (1991) Abstract; Full Text
Bacterial lipopolysaccharide stimulates protein tyrosine phosphorylation in macrophages: S.L. Weinstein, et al.; PNAS 88, 4148 (1991) Abstract
Inhibition of interleukin 3 and granulocyte-macrophage colony- stimulating factor stimulated increase of active ras.GTP by herbimycin A, a specific inhibitor of tyrosine kinases: T. Satoh, et al.; J. Biol. Chem. 267, 2537 (1992) Abstract; Full Text
New insight into oncoprotein-targeted antitumor effect: herbimycin A as an antagonist of protein tyrosine kinase against Ph1-positive leukemia cells: M. Okabe and M. Uehara; Leuk. Lymphoma 12, 41 (1993) Abstract
Prevention of anti-CD3 monoclonal antibody-induced thymic apoptosis by protein tyrosine kinase inhibitors: K. Migita, et al.; J. Immunol. 153, 3457 (1994) 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; Full Text
Inhibition of PDGF-induced phospholipase D but not phospholipase C activation by herbimycin A: B.Y. Kim; BBRC 212, 1061 (1995) Abstract
Controlling the vasculature: angiogenesis, anti-angiogenesis and vascular targeting of gene therapy: T.-P.D. Fan, et al.; TIPS 16, 57 (1995), (Review) Abstract
Herbimycin A enhances apoptotic effect of chemotherapeutic drugs on K562 cells: H. Ren, et al.; Chin. Med. J. (Engl.) 111, 678 (1998) Abstract
Hsp-90-associated oncoproteins: multiple targets of geldanamycin and its analogs: M.V. Blagosklonny; Leukemia 16, 455 (2002) Abstract; Full Text
Geldanamycin and herbimycin A induce apoptotic killing of B chronic lymphocytic leukemia cells and augment the cells’ sensitivity to cytotoxic drugs: D.T. Jones, et al.; Blood 103, 1855 (2004) Abstract; Full Text
Herbimycin A abrogates nuclear factor-kappaB activation by interacting preferentially with the IkappaB kinase beta subunit: S. Ogino, et al.; Mol. Pharmacol. 65, 1344 (2004) Abstract; Full Text
Herbimycin A suppresses mitotic activity and egg production of female Schistosoma mansoni: J. Knobloch, et al.; Int. J. Parasitol. 36, 1261 (2006) Abstract
Further Categories Containing This Product:
Tyrosine Kinase Inhibitors • Neurotoxins • Phospholipase D / Related Products • Antibiotics for Angiogenesis Research • HSP90 / HtpG / Related Products
 
 
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 • Fibroblast Growth Factors [FGFs] & Receptors / Related Products • Natural Products - Other Anti-infective Agents • Antitumor Antibiotics • Antitumor Agents (Anti-proliferative)
 
 
ALX-350-128 Revised 03-Apr-08
Chetomin
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SYNONYMS Chaetomin
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Immunomodulators
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ALX-350-128-M001   1 mg 185.00 USD Add To Cart
ALX-350-128-M005   5 mg 495.00 USD Add To Cart
Product Specification
FORMULA: C31H30N6O6S4
MW: 710.9
CAS NUMBER: 1403-36-7
SOURCE/HOST: Isolated from Chaetomium species.
PURITY: ≥98% (HPLC)
APPEARANCE: Off-white to fawn solid.
SOLUBILITY: Soluble in DMSO, ethyl acetate or pyridine; fairly soluble in methanol, 100% ethanol; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HAZARD: TOXIC.
IDENTITY: Determined by 1H-NMR.

Product Description
Dithiodiketopiperazine inhibitor of HIF-1 formation by disrupting the binding of p300 to both HIF-1α and HIF-2α. Inhibitor of tumor growth. Potent immunosuppressor. Antibacterial.
Product Specific Literature References
The structure of chetomin: A.G. McInnes, et al.; JACS 98, 6741 (1976) Abstract
Effects of chetomin on growth and acidic fermentation products of rumen bacteria: W.C. Jen and G.A. Jones; Can. J. Microbiol. 29, 1399 (1983) Abstract
Small molecule blockade of transcriptional coactivation of the hypoxia-inducible factor pathway: A.L. Kung, et al.; Cancer Cell 6, 33 (2004) Abstract
Immunomodulatory constituents from an Ascomycete, Chaetomium seminudum: H. Fujimoto, et al.; J. Nat. Prod. 67, 98 (2004) Abstract
Effects of HIF-1 inhibition by chetomin on hypoxia-related transcription and radiosensitivity in HT 1080 human fibrosarcoma cells: A. Staab, et al.; BMC Cancer 7, 213 (2007) Abstract; Full Text
Further Categories Containing This Product:
Hypoxia-inducible Factor [HIF] / Related Products • Antitumor Antibiotics • Immunomodulators Other Products • Antitumor Agents (Anti-proliferative)
 
 
ALX-350-131 Revised 03-Apr-08
Chaetoglobosin A
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Antifungal
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ALX-350-131-M001   1 mg 40.00 USD Add To Cart
ALX-350-131-M005   5 mg 160.00 USD Add To Cart
Product Specification
FORMULA: C32H36N2O5
MW: 528.7
SOURCE/HOST: Isolated from Chaetomium sp.
PURITY: ≥98% (HPLC)
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in methanol; almost unsoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: TOXIC.
IDENTITY: Determined by 1H-NMR.

Product Description
Cytochalasin analog with anti-fungal activity. Phytotoxic and anti-bacterial activity. Exhibits cytotoxic effects against human cancer cell lines. Enhances fibrinolytic activity of bovine aortic endothelial cells.
Product Specific Literature References
Acute toxic effects of chaetoglobosin A, a new cytochalasan compound produced by Chaetomium globosum, on mice and rats: K. Ohtsubo, et al.; Jpn. J. Exp. Med. 48, 105 (1978) Abstract
Chaetoglobosins, cytotoxic 10-(indol-3-yl)-[13]cytochalasans from Chaetomium spp. I. Production, isolation and some cytological effects of chaetoglobosins A-J: S. Sekita, et al.; Chem. Pharm. Bull. 30, 1609 (1982) Abstract
Enhancement of fibrinolytic activity of vascular endothelial cells by chaetoglobosin A, crinipellin B, geodin and triticone B: C. Shinohara, et al.; J. Antibiot. 53, 262 (2000) Abstract
Phytotoxic chaetoglobosins are produced by the plant pathogen Calonectria morganii (anamorph Cylindrocladium scoparium): C. Von Wallbrunn, et al.; J. Gen. Appl. Microbiol. 47, 33 (2001) Abstract; Full Text
Chaetoglobosins Q, R, and T, three further new metabolites from Chaetomium globosum: W. Jiao, et al.; J. Nat. Prod.