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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
 
 
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
 
 
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
 
 
ALX-350-019 Revised 17-Apr-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%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in methylene chloride or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: TOXIC.

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
 
 
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-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
 
 
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. 67, 1722 (2004) Abstract
Growth and mycotoxin production by Chaetomium globosum: M.R. Fogle, et al.; Mycopathologia 164, 49 (2007) Abstract
Further Categories Containing This Product:
Antitumor Antibiotics
 
 
ALX-350-245 Revised 07-Apr-08
Lactacystin (native)
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Proteasome/Ubiquitin Modulators
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ALX-350-245-MC01   0.1 mg 60.00 USD Add To Cart
ALX-350-245-MC05   0.5 mg 250.00 USD Add To Cart
ALX-350-245-M001   1 mg 445.00 USD Add To Cart
Product Specification
FORMULA: C15H24N2O7S
MW: 376.4
CAS NUMBER: 133343-34-7
SOURCE/HOST: Isolated from Streptomyces sp.
PURITY: ≥97% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in acetonitrile (20mg/ml), 100% ethanol (1mg/ml), methanol, DMSO (20mg/ml), dimethyl formamide (20mg/ml) or water (5mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Organic stock solutions are stable for 3 months when stored at -20°C. Subject to hydrolysis in aqueous buffers. We do not recommend storing the aqueous solutions for more than one day.
HANDLING: Protect from light.

Product Description

Cell permeable and irreversible proteasome inhibitor. Specifically inhibits 26S proteasome (MCP; multicatalytic proteinase complex). Blocks proteasome activity by targeting the catalytic β-subunit. Has no effect on serine or cysteine proteases. Induces apoptosis in human monoblast U937 cells. Also inhibits NF-κB activation by inhibiting IκB degradation. Inhibits the ubiquitin proteasome pathway in cell culture (IC50=10µM). Inhibits cathepsin A. Upregulates HSP70 and HSP22, suggesting an initial neuroprotective pathway.

Product Specific Literature References
Lactacystin, a novel microbial metabolite, induces neuritogenesis of neuroblastoma cells: S. Omura, et al.; J. Antibiot. 44, 116 (1991) Abstract
A beta-lactone related to lactacystin induces neurite outgrowth in a neuroblastoma cell line and inhibits cell cycle progression in an osteosarcoma cell line: G. Fenteany, et al.; PNAS 91, 3358 (1994) Abstract
Lactacystin, a specific inhibitor of the proteasome, induces apoptosis in human monoblast U937 cells: S. Imajo-Ohmi, et al.; BBRC 217, 1070 (1995) Abstract
The neuritogenesis inducer lactacystin arrests cell cycle at both G0/G1 and G2 phases in neuro 2a cells: M. Katagiri, et al.; J. Antibiotics (Tokyo) 48, 344 (1995) Abstract
Degradation process of ligand-stimulated platelet-derived growth factor beta-receptor involves ubiquitin-proteasome proteolytic pathway: S. Mori, et al.; J. Biol. Chem. 270, 29447 (1995) Abstract; Full Text
Structure-activity relationships of lactacystin, the first non-protein neurotrophic factor: T. Nagamitsu, et al.; J. Antibiotics (Tokyo) 48, 747 (1995) Abstract
Neuronal differentiation of Neuro 2a cells by lactacystin and its partial inhibition by the protein phosphatase inhibitors calyculin A and okadaic acid: H. Tanaka, et al.; BBRC 216, 291 (1995) Abstract
Inhibition of proteasome activities and subunit-specific amino-terminal threonine modification by lactacystin: G. Fenteany, et al.; Science 268, 726 (1995) Abstract
Proteasome-dependent regulation of p21WAF1/CIP1 expression: M.V. Blagosklonny, et al.; BBRC 227, 564 (1996) Abstract
Enhancement of CPP32-like activity in the TNF-treated U937 cells by the proteasome inhibitors: E. Fujita, et al.; BBRC 224, 74 (1996) Abstract
Degradation of 3-hydroxy-3-methylglutaryl-CoA reductase in endoplasmic reticulum membranes is accelerated as a result of increased susceptibility to proteolysis: T.P. McGee, et al.; J.Biol. Chem. 271, 25630 (1996) Abstract; Full Text
Lactacystin increases LDL receptor level on HepG2 cells: H. Miura, et al.; BBRC 227, 684 (1996) Abstract
Proteasome pathway operates for the degradation of ornithine decarboxylase in intact cells: Y. Murakami, et al.; Biochem. J. 317, 77 (1996) Abstract; Full Text
Lactacystin, an inhibitor of the proteasome, blocks the degradation of a mutant precursor of glycosylphosphatidylinositol-linked protein in a pre-Golgi compartment: K. Oda, et al.; BBRC 219, 800 (1996) Abstract
Degradation of a mutant secretory protein, alpha1-antitrypsin Z, in the endoplasmic reticulum requires proteasome activity: D. Qu, et al.; J. Biol. Chem. 271, 22791 (1996) Abstract; Full Text
Accelerated degradation of PML-retinoic acid receptor alpha (PML-RARA) oncoprotein by all-trans-retinoic acid in acute promyelocytic leukemia: possible role of the proteasome pathway: H. Yoshida, et al.; Cancer Res. 56, 2945 (1996) Abstract
The proteasome inhibitor lactacystin induces apopto