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Antibiotics - Signal Transduction Pathway Modulators
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ALX-380-091 Revised 21-Aug-08
17-AAG
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SYNONYMS 17-(Allylamino)-17-desmethoxygeldanamycin
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antitumor Antibiotics
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-380-091-C100   100 µg 65.00 USD Add To Cart
ALX-380-091-M001   1 mg 162.00 USD Add To Cart
Product Specification
FORMULA: C31H43N3O8
MW: 585.7
CAS NUMBER: 75747-14-7
SOURCE/HOST: Semisynthetic derivative from geldanamycin.
PURITY: ≥97%
APPEARANCE: Red to dark red powder.
SOLUBILITY: Soluble in DMSO (10mg/ml) or methanol (10mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Potent, less toxic derivative of geldanamycin (Prod. No. ALX-380-054). Inhibits the essential ATPase activity of HSP90. Inhibitor of telomerase activity. Inducer of apoptosis with antitumor activity.
Product Specific Literature References
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
The benzoquinone ansamycin 17-allylamino-17-demethoxygeldanamycin binds to HSP90 and shares important biologic activities with geldanamycin: T.W. Schulte & L.M. Neckers; Cancer Chemother. Pharmacol. 42, 273 (1998) Abstract
Gene expression profiling of human colon cancer cells following inhibition of signal transduction by 17-allylamino-17-demethoxygeldanamycin, an inhibitor of the hsp90 molecular chaperone: P.A. Clarke, et al.; Oncogene 19, 4125 (2000) Abstract
Geldanamycin and its analogue 17-allylamino-17-demethoxygeldanamycin lowers Bcr-Abl levels and induces apoptosis and differentiation of Bcr-Abl-positive human leukemic blasts: R. Nimmanapalli, et al.; Cancer Res. 61, 1799 (2001) Abstract; Full Text
Inhibition of heat shock protein 90 function by ansamycins causes the morphological and functional differentiation of breast cancer cells: P.N. Munster, et al.; Cancer Res. 61, 2945 (2001) Abstract; Full Text
Disruption of the EF-2 kinase/Hsp90 protein complex: a possible mechanism to inhibit glioblastoma by geldanamycin: J. Yang, et al.; Cancer Res. 61, 4010 (2001) Abstract; Full Text
Enhancement of paclitaxel-mediated cytotoxicity in lung cancer cells by 17-allylamino geldanamycin: in vitro and in vivo analysis: D.M. Nguyen, et al.; Ann. Thorac. Surg. 72, 371 (2001) Abstract
ErbB2 degradation mediated by the co-chaperone protein CHIP: P. Zhou, et al.; J. Biol. Chem. 278, 13829 (2003) 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
Geldanamycin and its 17-allylamino-17-demethoxy analogue antagonize the action of Cisplatin in human colon adenocarcinoma cells: differential caspase activation as a basis for interaction: I.A. Vasilevskaya, et al.; Cancer Res. 63, 3241 (2003) Abstract
A high-affinity conformation of Hsp90 confers tumour selectivity on Hsp90 inhibitors: A. Kamal, et al.; Nature 425, 407 (2003) Abstract
Chaperoning oncogenes: HSP90 as a target of geldanamycin: L. Neckers; Handb. Exp. Pharmacol. 259 (2006) Abstract
Drugging the cancer chaperone HSP90: Combinatorial therapeutic exploitation of oncogene addiction and tumor stress: P. Workman, et al.; Ann. N.Y. Acad. Sci. 1113, 202 (2007) Abstract
Synergism between etoposide and 17-AAG in leukemia cells: critical roles for Hsp90, FLT3, topoisomerase II, Chk1, and Rad51: Q. Yao, et al.; Clin. Cancer Res. 13, 1591 (2007) Abstract; Full Text
Phase I and pharmacodynamic study of 17-(allylamino)-17-demethoxygeldanamycin in adult patients with refractory advanced cancers: R.K. Ramanathan, et al.; Clin. Cancer Res. 13, 1769 (2007) Abstract
HSP90 inhibitor 17AAG causes apoptosis in ATRA-resistant acute promyelocytic leukemia cells: P.N. Meyer, et al.; Leuk. Res. 32, 143 (2008) Abstract
Intratumor injection of the Hsp90 inhibitor 17AAG decreases tumor growth and induces apoptosis in a prostate cancer xenograft model: C.R. Williams, et al.; J. Urol. 178, 1528 (2007) Abstract
Rituximab and 17-allylamino-17-demethoxygeldanamycin induce synergistic apoptosis in B-cell chronic lymphocytic leukaemia: A.J. Johnson, et al.; Br. J. Haematol. 139, 837 (2007) Abstract
An in vitro and in vivo study of the combination of the heat shock protein inhibitor 17-allylamino-17-demethoxygeldanamycin and carboplatin in human ovarian cancer models: U. Banerji, et al.; Cancer Chemother. Pharmacol. 62, 769 (2008) Abstract
Further Categories Containing This Product:
Antibiotics - Apoptosis Inducers & Inhibitors • Antitumor Agents (Enzyme Inhibitors) • Tyrosine Kinase Inhibitors • Antibiotics - Other Signal Transduction Pathway Modulators • HSP90 / HtpG / Related Products
 
 
ALX-450-001 Revised 23-Jul-08
A23187 (free acid)
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SYNONYMS Calcium Ionophore A23187
Calcimycin
Antibiotic A23187
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Ionophores
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-450-001-M001   1 mg 28.00 USD Add To Cart
ALX-450-001-M005   5 mg 65.00 USD Add To Cart
ALX-450-001-5001   5x1 mg 80.00 USD Add To Cart
ALX-450-001-M010   10 mg 92.00 USD Add To Cart
ALX-450-001-M025   25 mg 195.00 USD Add To Cart
ALX-450-001-M050   50 mg 350.00 USD Add To Cart
Product Specification
FORMULA: C29H37N3O6
MW: 523.6
CAS NUMBER: 52665-69-7
MERCK INDEX: 14: 1639
RTECS: DM4676000
SOURCE/HOST: Isolated from Streptomyces chartreusis.
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO, 100% ethanol or methylene chloride; slightly soluble in water. Solubilize in DMSO or ethanol prior to preparing aqueous solutions of very low concentrations.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: In aqueous systems product may aggregate over time.
HANDLING: Protect from light. In aqueous systems, the product aggregates over time.
HAZARD: IRRITANT.

Product Description
Antibiotic possessing weak in vitro antimicrobial activity against gram positive bacteria and fungi. Divalent cation ionophore commonly used to increase intracellular Ca2+ levels in intact cells.
Product Specific Literature References
A23187: a divalent cation ionophore: P. W. Reed & H. A. Lardy; J. Biol. Chem. 247, 6970 (1972) Abstract
Effects of antibiotic ionophore, A23187, on oxidative phosphorylation and calcium transport of liver mitochondria: D.T. Wong, et al.; Arch. Biochem. Biophys. 156, 578 (1973) Abstract
Biological applications of ionophores: B.C. Pressman; Annu. Rev. Biochem. 45, 501 (1976), (Review) Abstract
Molecular mechanisms of endothelium-mediated vasodilation: R.R. Fiscus; Semin. Thromb. Hemost. 14 Suppl, 12 (1988), (Review) Abstract
Calcium ionophore A23187 action on cardiac myocytes is accompanied by enhanced production of reactive oxygen species: 1740, 481 (2005): T. Przygodzki, et al.; Biochim. Biophys. Acta 1740, 481 (2005) Abstract
Further Categories Containing This Product:
Nitric Oxide Pathway Other Products • Respiratory Chain Other Products • Antibiotics - ATPase Inhibitors
 
 
ALX-350-315 Revised 03-Apr-08
Agelasine D
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products with Antibiotic Activity
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ALX-350-315-M001   1 mg 185.00 USD Add To Cart
Product Specification
FORMULA: C26H40N5
MW: 422.6
CAS NUMBER: 92664-80-7
SOURCE/HOST: Isolated from the sponge Agelas nakamurai.
PURITY: ≥97% (HPLC)
APPEARANCE: White to off-white 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
Displays broad spectrum of antibacterial activities. Antineoplastic compound. Associated with contractive responses of smooth muscles and inhibition of Na+/K+-ATPase.
Product Specific Literature References
(+)-agelasine D: improved synthesis and evaluation of antibacterial and cytotoxic activities: A. Vik, et al.; J. Nat. Prod. 69, 381 (2006) Abstract
Antimicrobial and cytotoxic activity of agelasine and agelasimine analogs: A. Vik, et al.; Bioorg. Med. Chem. 15, 4016 (2007) Abstract
Further Categories Containing This Product:
Na+ / K+-ATPase / Related Products • Antitumor Agents (Anti-proliferative) • Natural Products - Antitumor Reagents • Antibiotics - ATPase Inhibitors
 
 
ALX-350-106 Revised 29-Nov-07
Ampullosporin A
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Other Signal Transduction Pathway Modulators
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ALX-350-106-M001   1 mg 50.00 USD Add To Cart
Product Specification
SEQUENCE: Ac-Trp-Ala-Aib-Aib-Leu-Aib-Gln-Aib-Aib-Aib-Gln-Leu-Aib-Gln-Leucinol
FORMULA: C77H127N19O19
MW: 1623.0
SOURCE/HOST: Antibiotic isolated from Sepedonium ampullosporum.
PURITY: ≥98% (HPLC)
SOLUBILITY: Soluble in alcohols, chloroform or dichloromethane. Insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HAZARD: TOXIC.
Product Description
Peptaibol-type polypeptide. Induces pigment formation by the fungus Phoma destructiva, causes hypothermia in mice, displays neuroleptic activity in rats and forms instable pores in artificial bilayer membranes.
Product Specific Literature References
Ampullosporin, a new peptaibol-type antibiotic from Sepedonium ampullosporum HKI-0053 with neuroleptic activity in mice: M. Ritzau, et al.; J. Antibiot. 50, 722 (1997) Abstract
Differences in ion permeability of an artificial bilayer membrane caused by ampullosporin and bergofungin, new 15-membered peptaibol-type antibiotics: P. Grigoriev, et al.; Bioelectrochemistry 44, 155 (1997)
Differences in ion-channel formation by ampullosporins B, C, D and semisynthetic desacetyltryptophanyl ampullosporin A: P. Grigoriev, et al.; Bioelectrochemistry 57, 119 (2002) Abstract
Synthesis and biological evaluation of analogues of the peptaibol ampullosporin A: H.H. Nguyen, et al.; J. Med. Chem. 45, 2781 (2002) Abstract
Crystal structure and conformational analysis of ampullosporin A: M. Kronen, et al.; J. Pept. Sci. 9, 729 (2003) Abstract
Membrane association and activity of 15/16-membered peptide antibiotics: zervamicin IIB, ampullosporin A and antiamoebin I: T.N. Kropacheva, et al.; Biochim. Biophys. Acta 1715, 6 (2005) Abstract
Transcriptional response to the neuroleptic-like compound Ampullosporin A in the rat ketamine model: H. Krugel, et al.; J. Neurochem. 97, Suppl. 1, 74 (2006) Abstract
Further Categories Containing This Product:
Alzheimer Research Other Products • Ion Channels & Transporters Other Products • Peptides
 
 
ALX-380-051 Revised 20-Jun-08
Anisomycin
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SYNONYMS 2-(p-Methoxybenzyl)-3,4-pyrrolidinediol-3-acetate
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Other Signal Transduction Pathway Modulators
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-380-051-M010   10 mg 35.00 USD Add To Cart
ALX-380-051-M050   50 mg 140.00 USD Add To Cart
ALX-380-051-M100   100 mg 250.00 USD Add To Cart
Product Specification
FORMULA: C14H19NO4
MW: 265.3
CAS NUMBER: 22862-76-6
MERCK INDEX: 14: 670
RTECS: BZ9800000
SOURCE/HOST: Isolated from Streptomyces griseolus.
PURITY: ≥98% (HPLC)
APPEARANCE: White crystalline solid.
SOLUBILITY: Soluble in DMSO (25mg/ml), 100% ethanol, methanol or ethyl acetate (10mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: TOXIC.

Product Description
Antibiotic. Activator of p38 and MAP kinases. Synergistic with growth factors and phorbol esters to superinduce cFos and cJun, by acting as a potent signalling agonist. Induces apoptosis in the human monoblastoid cell line. Used in the eradication of bean mildew. Inhibits other pathogenic fungi in plants.
Product Specific Literature References
Anisomycin, a new anti-protozoan antibiotic: B. A. Sobin & F. W. Tanner; J. Am. Chem. Soc. 76, 4053 (1954)
DNA fragmentation and cytolysis in U937 cells treated with diphtheria toxin or other inhibitors of protein synthesis: S.K. Kochi & R.J. Collier; Exp. Cell. Res. 208, 296 (1993) Abstract
The stress-activated protein kinase subfamily of c-Jun kinases: J.M. Kyriakis, et al.; Nature 369, 156 (1994) Abstract
Role of SAPK/ERK kinase-1 in the stress-activated pathway regulating transcription factor c-Jun: I. Sanchez, et al.; Nature 372, 794 (1994) Abstract
Anisomycin and rapamycin define an area upstream of p70/85S6k containing a bifurcation to histone H3-HMG-like protein phosphorylation and c-fos-c-jun induction: E. Kardalinou, et al.; Mol. Cell. Biol. 14, 1066 (1994) Abstract
Protein synthesis inhibitor phase shifts vasopressin rhythms in long- term suprachiasmatic cultures: K. Shinohara & T. Oka; NeuroReport 5, 2201 (1994) Abstract
Anisomycin selectively desensitizes signalling components involved in stress kinase activation and fos and jun induction: C.A. Hazzalin, et al.; Mol Cell Biol 18, 1844 (1998) Abstract
Anisomycin treatment paradigm affects duration of long-term potentiation in slices of the amygdala: P. Okulski, et al.; Neuroscience 114, 1 (2002) Abstract
Downregulation of Ski and SnoN co-repressors by anisomycin: A. Vazquez-Macias, et al.; FEBS Lett. 579, 3701 (2005) Abstract
Anisomycin and the reconsolidation hypothesis: J.W. Rudy, et al.; Learn. Mem. 13, 1 (2006), Review Abstract
A chemical screen identifies anisomycin as an anoikis sensitizer that functions by decreasing FLIP protein synthesis: I.A. Mawji, et al.; Cancer Res. 67, 8307 (2007) Abstract
Anisomycin abrogates repression of protooncogene c-fos transcription in E1A + cHa-ras-transformed cells through activation of MEK/ERK kinase cascade: A. N. Kukushkin, et al.; J. Cell. Biochem. 103, 1005 (2008) Abstract
Further Categories Containing This Product:
MAPK Pathway Activators • Antibiotics - Apoptosis Inducers & Inhibitors • JNK [SAPK1] / Related Products
 
 
ALX-380-005 Revised 03-Apr-08
Ascomycin
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SYNONYMS Immunomycin
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Immunomodulators
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-380-005-M001   1 mg 125.00 USD Add To Cart
ALX-380-005-M005   5 mg 540.00 USD Add To Cart
Product Specification
FORMULA: C43H69NO12
MW: 792.0
CAS NUMBER: 11011-38-4
RTECS: CI75700000
SOURCE/HOST: Isolated from Streptomyces sp.
PURITY: ≥95%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: HARMFUL.

Product Description
Antibiotic. Ethyl analog of FK506 (Prod. No. ALX-380-008) with similar immunosuppressant properties. Inhibits calcineurin phosphatase.
Product Specific Literature References
Ascomycin, an antifungal antibiotic: T. Arai, et al.; J. Antibiot. (Tokyo) 15, 23 (1962) Abstract
NMR studies of an FK-506 analog, [U-13C]ascomycin, bound to FK-506-binding protein: A.M. Petros, et al.; J. Med. Chem. 35, 2467 (1992) Abstract
Structure-activity profiles of macrolactam immunosuppressant FK-506 analogues: M. Kawai, et al.; FEBS Lett. 316, 107 (1993) Abstract
Enzymatic synthesis and immunosuppressive activity of novel desmethylated immunomycins (ascomycins): A. Shafiee, et al.; J. Antibiot. (Tokyo) 46, 1397 (1993) Abstract
Further Categories Containing This Product:
Antibiotics - Other Signal Transduction Pathway Modulators • PP2B [Calcineurin] / Related Products
 
 
ALX-380-030 Revised 17-Oct-07
Bafilomycin A1
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - ATPase Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-380-030-C100   100 µg 70.00 USD Add To Cart
ALX-380-030-M001   1 mg 210.00 USD Add To Cart
Product Specification
FORMULA: C35H58O9
MW: 622.8
CAS NUMBER: 88899-55-2
SOURCE/HOST: Isolated from Streptomyces griseus.
PURITY: ≥95%
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in 100% ethanol, methanol or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: TOXIC.

Product Description
Macrolide antibiotic that acts as a specific inhibitor of vacuolar-type H+-ATPase. Valuable tool for distinguishing among different types of ATPases. Inhibitor of endosomal acidification.
Product Specific Literature References
Metabolic products of microorganisms. 224. Bafilomycins, a new group of macrolide antibiotics. Production, isolation, chemical structure and biological activity: G. Werner, et al.; J. Antibiot. 37, 110 (1984) Abstract
Bafilomycins: a class of inhibitors of membrane ATPases from microorganisms, animal cells, and plant cells: E.J. Bowman, et al.; PNAS 85, 7972 (1988) Abstract
The evolution of H+-ATPases [see comments]: N. Nelson & L. Taiz; TIPS 14, 113 (1989), (Review) Abstract
Kinetic studies of chromaffin granule H+-ATPase and effects of bafilomycin A1: H. Hanada, et al.; BBRC 170, 873 (1990) Abstract
Inhibition of osteoclast proton transport by bafilomycin A1 abolishes bone resorption: K. Sundqui, et al.; BBRC 168, 309 (1990) Abstract
The cytotoxic action of diphtheria toxin and its degradation in intact Vero cells are inhibited by bafilomycin A1, a specific inhibitor of vacuolar-type H(+)-ATPase: T. Umata, et al.; J. Biol. Chem. 265, 21940 (1990) Abstract; Full Text
Bafilomycin A1 inhibits the targeting of lysosomal acid hydrolases in cultured hepatocytes: K. Oda, et al.; BBRC 178, 369 (1991) Abstract
Bafilomycin A1, a specific inhibitor of vacuolar-type H(+)-ATPase, inhibits acidification and protein degradation in lysosomes of cultured cells: T. Yoshimori, et al.; J. Biol. Chem. 266, 17707 (1991) Abstract; Full Text
Inhibitory effect of modified bafilomycins and concanamycins on P- and V-type adenosinetriphosphatases: S. Drose, et al.; Biochemistry 32, 3902 (1993) Abstract
Bafilomycin A1, a specific inhibitor of vacuolar-type H(+)-ATPase, blocks lysosomal cholesterol trafficking in macrophages: T. Furuchi, et al.; J. Biol. Chem. 268, 27345 (1993) Abstract; Full Text
Bafilomycin inhibits proton flow through the H+ channel of vacuolar proton pumps: B.P. Crider, et al.; J. Biol. Chem. 269, 17379 (1994) Abstract; Full Text
Active vacuolar H+ATPase is required for both endocytic and exocytic processes during viral infection of BHK-21 cells: H. Palokangas, et al.; J. Biol. Chem. 269, 17577 (1994) Abstract; Full Text
Inositol trisphosphate-dependent and -independent Ca2+ mobilization pathways at the vacuolar membrane of Candida albicans: C.M. Calvert & D. Sanders; J. Biol. Chem. 270, 7272 (1995) Abstract; Full Text
The vacuolar H(+)-ATPase inhibitor bafilomycin A1 differentially affects proteolytic processing of mutant and wild-type beta-amyloid precursor protein: C. Haass, et al.; J. Biol. Chem. 270, 6186 (1995) Abstract; Full Text
Cell-type and amyloid precursor protein-type specific inhibition of A beta release by bafilomycin A1, a selective inhibitor of vacuolar ATPases: J. Knops, et al.; J. Biol. Chem. 270, 2419 (1995) Abstract; Full Text
Specific inhibitors of vacuolar type H(+)-ATPases induce apoptotic cell death: T. Nishihara, et al.; BBRC 212, 255 (1995) Abstract
Inhibition of mitogen-induced DNA synthesis by bafilomycin A1 in Swiss 3T3 fibroblasts: A.J. Saurin, et al.; Biochem. J. 313, 65 (1996) Abstract
Autophagy, bafilomycin and cell death: the "a-B-cs" of plecomacrolide-induced neuroprotection: J.J. Shacka, et al.; Autophagy 2, 228 (2006), Review Abstract
Bafilomycin A1-sensitive pathway is required for the maturation of cystic fibrosis transmembrane conductance regulator: T. Okiyoneda, et al.; Biochim. Biophys. Acta 1763, 1017 (2006) Abstract
Further Categories Containing This Product:
H+-ATPase / Related Products • Vesicles & Membrane Trafficking Other Products • Autophagy Other Products • Antibiotics - Apoptosis Inducers & Inhibitors
 
 
ALX-380-063 Revised 03-Apr-08
Bafilomycin B1
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - ATPase Inhibitors
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ALX-380-063-M001   1 mg 70.00 USD Add To Cart
Product Specification
FORMULA: C44H65NO13
MW: 816.0
CAS NUMBER: 88899-56-3; 80112-34-1
SOURCE/HOST: Isolated from Streptomyces griseus.
PURITY: ≥95%
APPEARANCE: Off-white to yellow powder.
SOLUBILITY: Soluble in methanol.
SHIPPING: AMBIENT