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Antibiotics - Antifungal
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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 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
 
 
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-350-325 Revised 25-Jun-07
Altenusin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Antifungal
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ALX-350-325-M001   1 mg 110.00 USD Add To Cart
ALX-350-325-M005   5 mg 380.00 USD Add To Cart
Product Specification
FORMULA: C15H14O6
MW: 290.3
CAS NUMBER: 31186-12-6
SOURCE/HOST: Isolated from Alternaria sp.
PURITY: ≥97% (HPLC)
APPEARANCE: Yellow to brown solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
IDENTITY: Identity determined by 1H-NMR, 13C-NMR and MS.

Product Description
Antifungal penicillide. Non-competitive, specific neutral sphingomyelinase (N-SMase) and strong pp60c-Src inhibitor. Inhibits cFMS receptor tyrosine kinase (CSF-1/m-CSF receptor tyrosine kinase) which is implicated in cancer and bone diseases. Myosin light chain kinase inhibitor. Exhibits anti-HIV-1 integrase activity.
Product Specific Literature References
Studies in the biochemistry of micro-organisms. 103. Metabolites of Alternaria tenuis Auct.: Culture filtrate products: T. Rosett, et al.; Biochem. J. 67, 390 (1957) Full Text
Studies in the biosynthesis of fungal metabolites. 4. Alternariol monomethyl ether and its relation to other phenolic metabolites of Alternaria tenuis: R. Thomas; Biochem. J. 80, 234 (1961) Abstract; Full Text
Metabolites of some Alternaria species. The structures of altenusin and dehydroaltenusin: R. G. Coombe, et al.; Aus. J. Chem. 23, 2343 (1970)
Host-specific toxins and chemical structures from alternaria species: S. Nishimura, et al.; Ann. Rev. Phytopathol. 21, 87 (1983)
The metabolites of Talaromycesflavus: Part 1. Metabolites of the organic extracts : W. A. Ayer, et al.; Can. J. Chem. 68, 2085 (1990)
Isolation of myosin light chain kinase inhibitors from microorganisms: dehydroaltenusin, altenusin, atrovenetinone, and cyclooctasulfur: S. Nakanishi, et al.; Biosci. Biotechnol. Biochem. 59, 1333 (1995) Abstract
Alutenusin, a specific neutral sphingomyelinase inhibitor, produced by Penicillium sp. FO-7436: R. Uchida, et al.; J. Antibiot. 52, 572 (1999) Abstract
Isolation, structure, and HIV-1-integrase inhibitory activity of structurally diverse fungal metabolites: S.B. Singh, et al.; J. Ind. Microbiol. Biotechnol. 30, 721 (2003) Abstract
Fungal metabolites as potent protein kinase inhibitors: Identification of a novel metabolite and novel activities of known metabolites : M. Oyama, et al.; Lett. Drug Design Discov. 1, 24 (2004)
New penicillide derivatives isolated from Penicillium simplicissimum: S. I. Komai, et al.; J. Nat. Med. 60, 185 (2006)
HIV-1 integrase inhibitors: 2003-2004 update: R. Dayam, et al.; Med. Res. Rev. 26, 271 (2006) Abstract
 
 
ALX-380-004 Revised 21-Feb-08
Rapamycin
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SYNONYMS Sirolimus
AY-22,989
RAPA
Rapamune
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Immunomodulators
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ALX-380-004-C100   100 µg 35.00 USD Add To Cart
ALX-380-004-5100   5x100 µg 90.00 USD Add To Cart
ALX-380-004-M001   1 mg 120.00 USD Add To Cart
ALX-380-004-M005   5 mg 420.00 USD Add To Cart
ALX-380-004-M025   25 mg 950.00 USD Add To Cart
Product Specification
FORMULA: C51H79NO13
MW: 914.2
CAS NUMBER: 53123-88-9
MERCK INDEX: 14: 8114
RTECS: VE6250000
SOURCE/HOST: Isolated from Streptomyces hygroscopicus.
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in chloroform, DMSO or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: TOXIC.

Product Description
Macrocyclic-triene antibiotic possessing potent immunosuppressant activity. It forms a complex with FKBP12 that binds to an effector, thus inhibiting IL-2 and other growth promoting lymphokines. The effectors were recently identified as FRAP (FKBP12 rapamycin-associated protein) and RAFT1 (rapamycin and KFBP12 target). Rapamycin induces inhibition of p70s6k, p33cdk2 and p34cdc2. Enhances apoptosis.
Product Specific Literature References
Rapamycin (AY-22,989), a new antifungal antibiotic. I. Taxonomy of the producing streptomycete and isolation of the active principle: C. Vezina, et al.; J. Antibiot. (Tokyo) 28, 721 (1975) Abstract
Rapamycin (AY-22,989), a new antifungal antibiotic. II. Fermentation, isolation and characterization: S.N. Sehgal, et al.; J. Antibiot. (Tokyo) 28, 727 (1975) Abstract
Rapamycin-induced inhibition of the 70-kilodalton S6 protein kinase: D.J. Price, et al.; Science 257, 973 (1992) Abstract
Rapamycin: in vitro profile of a new immunosuppressive macrolide: S.N. Sehgal & C.C. Bansback; Ann. N. Y. Acad. Sci. 685, 58 (1993) Abstract
Rapamycin inhibition of interleukin-2-dependent p33cdk2 and p34cdc2 kinase activation in T lymphocytes: W.G. Morice, et al.; J. Biol. Chem. 268, 22737 (1993) Abstract; Full Text
A mammalian protein targeted by G1-arresting rapamycin-receptor complex: E.J. Brown, et al.; Nature 369, 756 (1994) Abstract
RAFT1: a mammalian protein that binds to FKBP12 in a rapamycin- dependent fashion and is homologous to yeast TORs: D.M. Sabatini, et al.; Cell 78, 35 (1994) Abstract
Rapamycin, a potent immunosuppressive drug, causes programmed cell death in B lymphoma cells: S. Muthukkumar, et al.; Transplantation 60, 264 (1995) Abstract
Rapamycin enhances apoptosis and increases sensitivity to cisplatin in vitro: Y. Shi, et al.; Cancer Res. 55, 1982 (1995) Abstract
Rapamycin potentiates dexamethasone-induced apoptosis and inhibits JNK activity in lymphoblastoid cells: T. Ishizuka, et al.; BBRC 230, 386 (1997) Abstract
Rapamycin and p53 act on different pathways to induce G1 arrest in mammalian cells: S.M. Metcalfe, et al.; Oncogene 15, 1635 (1997) Abstract
Rapamycin inhibition of the G1 to S transition is mediated by effects on cyclin D1 mRNA and protein stability: S. Hashemolhosseini, et al.; J. Biol. Chem. 273, 14424 (1998) Abstract; Full Text
Rapamycin causes poorly reversible inhibition of mTOR and induces p53- independent apoptosis in human rhabdomyosarcoma cells: H. Hosoi, et al.; Cancer Res. 59, 886 (1999) Abstract
Rapamycin: an anti-cancer immunosuppressant?: B.K. Law; Crit. Rev. Oncol. Hematol. 56, 47 (2005), Review Abstract
mTOR inhibitors (rapamycin and its derivatives) and nitrogen containing bisphosphonates: bi-functional compounds for the treatment of bone tumours: B. Ory, et al.; Curr. Med. Chem. 14, 1381 (2007), Review Abstract
 
 
ALX-380-036 Revised 10-Dec-07
Oligomycin A
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Apoptosis Inducers & Inhibitors
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ALX-380-036-M005   5 mg 140.00 USD Add To Cart
Product Specification
FORMULA: C45H74O11
MW: 791.1
CAS NUMBER: 579-13-5
MERCK INDEX: 14: 6833
RTECS: RK3328000
SOURCE/HOST: Isolated from Streptomyces sp. MST-AS5339.
PURITY: ≥95% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in 100% ethanol, methanol, dimethyl formamide or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: MAY BE MUTAGENIC. HARMFUL.

Product Description
Major component of the oligomycin complex. Macrolide antibiotic that inhibits membrane bound mitochondrial ATPase (F1F0), preventing phosphoryl group transfer. Induces apoptosis. Induces autophagy in the IPLB-LdFB insect cell line.
Product Specific Literature References
Production and isolation of the antibiotic, oligomycin: J. Visser, et al.; J. Biochem. Microbiol. Technol. Egr. 2, 31 (1960) Abstract
The BH3 domain is required for caspase-independent cell death induced by Bax and oligomycin: M.E. Fitch, et al.; Cell Death Differ. 7, 338 (2000) Abstract; Full Text
Oligomycin, inhibitor of the F0 part of H+-ATP-synthase, suppresses the TNF-induced apoptosis: L.A. Shchepina, et al.; Oncogene 21, 8149 (2000) Abstract; Full Text
Mitochondria-targeting drug oligomycin blocked P-glycoprotein activity and triggered apoptosis in doxorubicin-resistant HepG2 cells: Y.C. Li, et al.; Chemotherapy 50, 55 (2004) Abstract
Oligomycin A induces autophagy in the IPLB-LdFB insect cell line: G. Tettamanti, et al.; Cell Tissue Res. 326, 179 (2006) Abstract
 
 
ALX-380-037 Revised 20-Jun-08
Oligomycin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Apoptosis Inducers & Inhibitors
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ALX-380-037-M005   5 mg 50.00 USD Add To Cart
ALX-380-037-M010   10 mg 95.00 USD Add To Cart
Product Specification
MW: 789.3
CAS NUMBER: 1404-19-9
MERCK INDEX: 14: 6833
RTECS: RK3325000
SOURCE/HOST: Isolated from Streptomyces diastatochromogens.
PURITY: ≥90% (mixture of oligomycin A, B, and C (~65% oligomycin A))
APPEARANCE: White to faint yellow powder.
SOLUBILITY: Soluble in 100% ethanol, methanol (10mg/ml) or acetone (50mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: HARMFUL. MAY BE MUTAGENIC.

Product Description
Macrolide antibiotic that inhibits membrane bound mitochondrial ATPase (F1), preventing phosphoryl group transfer. Induces apoptosis.
Product Specific Literature References
Inhibition of the Na(+)-Ca++ exchanger enhances anoxia and glucopenia- induced [3H]aspartate release in hippocampal slices: S. Amoroso, et al.; J. Pharmacol. Exp. Ther. 264, 515 (1993) Abstract
Cyclosporin A suppression of uncoupling in liver mitochondria of ground squirrel during arousal from hibernation: N.N. Brustovetsky, et al.; FEBS Lett. 315, 233 (1993) Abstract
The lipophilic weak base (Z)-5-methyl-2-[2-(1-naphthyl)ethenyl]-4- piperidinopyridine (AU-1421) is a potent protonophore type cationic uncoupler of oxidative phosphorylation in mitochondria: H. Nagamune, et al.; Biochim. Biophys. Acta 1141, 231 (1993) Abstract
Mitochondrial respiratory chain inhibitors induce apoptosis: E.J. Wolvetang, et al.; FEBS Lett. 339, 40 (1994) Abstract
Dissociation of phagocyte recognition of cells undergoing apoptosis from other features of the apoptotic program: J. Zhuang, et al.; J. Biol. Chem. 273, 15628 (1998) Abstract; Full Text
Apoptosis in factor-dependent haematopoietic cells is linked to calcium- sensitive mitochondrial rearrangements and cytoskeletal modulation: J. Garland, et al.; Br. J. Haematol. 109, 221 (2000)