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Antitumor Reagents
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ALX-270-292 Revised 09-Feb-05
1L-6-Hydroxymethyl-chiro-inositol-2-[(R)-2-O-methyl-3-O-octadecylcarbonate]
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Phosphoinositide 3-kinase [PI(3)K] / Related Products
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ALX-270-292-M001   1 mg 85.00 USD Add To Cart
ALX-270-292-M005   5 mg 330.00 USD Add To Cart
Product Specification
FORMULA: C30H58O10
MW: 578.8
PURITY: >98%
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Keep cool and dry.

Product Description
Potent inhibitor of Akt (PKB) (IC50=2.0µM). Weak inhibitor of PI(3)K (phosphoinositide 3-kinase) (IC50=83µM). Has been shown to inhibit the growth of the following cancer cell lines: HeLa (IC50=2.5µM), HT-29 (IC50=10µM), MCF-7 (IC50=1.2µM) and PC-3 (IC50=2.0µM).
Product Specific Literature References
3-(Hydroxymethyl)-bearing phosphatidylinositol ether lipid analogues and carbonate surrogates block PI3-K, Akt, and cancer cell growth: Y. Hu, et al.; J. Med. Chem. 43, 3045 (2000) Abstract
Further Categories Containing This Product:
Akt [PKB] / Related Products • Protein Kinase Inhibitors Other Products • Antitumor Agents (Enzyme Inhibitors)
 
 
ALX-380-224 Revised 09-Jun-08
21-Hydroxyoligomycin A
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SYNONYMS Nemadectin ω
Antibiotic LL-F28249 ω
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antitumor Antibiotics
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ALX-380-224-M001   1 mg 360.00 USD Add To Cart
Product Specification
FORMULA: C45H74O12
MW: 807.1
CAS NUMBER: 102042-09-1
SOURCE/HOST: Isolated from Streptomyces sp. AS5351.
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

Product Description
Co-metabolite of nemadectin. Antitumor agent with weak antifungal and nematocidal activity.
Product Specific Literature References
Plasmid effects on secondary metabolite production by a streptomycete synthesizing an anthelmintic macrolide: D.I. Thomas, et al.; J. Gen. Microbiol. 137, 2331 (1991) Abstract
Structure and absolute stereochemistry of 21-hydroxyoligomycin A: M.M. Wagenaar, et al.; J. Nat. Prod. 70, 367 (2007) Abstract
 
 
ALX-350-097 Revised 16-Jun-08
Hyperforin . dicyclohexylammonium salt (high purity)
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products for Neurological Research
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ALX-350-097-C500   500 µg 130.00 USD Add To Cart
ALX-350-097-M001   1 mg 210.00 USD Add To Cart
Product Specification
FORMULA: C35H51O4 . C12H24N
MW: 535.8 . 182.3
CAS NUMBER: 11079-53-1 (non-salt form)
SOURCE/HOST: Isolated from St. John's wort (Hypericum perforatum).
PURITY: ≥97% (HPLC)
APPEARANCE: White to off-white powder.
PURITY DETAIL: Contains <3% adhyperforin.
SOLUBILITY: Soluble in DMSO, methanol or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Keep under inert gas. Protect from light.

Product Description
Major constituent of St. John’s wort, a herbal remedy widely used for the treatment of depression. Inhibits the reuptake of neurotransmitters in synapses. Activator of the pregnane X receptor (PXR), which serves as a key regulator of CYP3A4 transcription, a member of the cytochrome (CYP) P450 enzyme system. Specifically activates TRPC6 channels. Represents an interesting lead-structure for a new class of antidepressants. Displays several other biological properties of potential pharmacological interest, including antibacterial, anti-inflammational, antitumoral and anti-angiogenic effects. Induces apoptosis in various cancer cells.
Product Specific Literature References
Hyperforin as a possible antidepressant component of hypericum extracts: S.S. Chatterjee, et al.; Life Sci. 63, 499 (1998) Abstract
Hyperforin attenuates various ionic conductance mechanisms in the isolated hippocampal neurons of rat: S. Chatterjee, et al.; Life Sci. 65, 2395 (1999) Abstract
Antibacterial activity of hyperforin from St John's wort, against multiresistant Staphylococcus aureus and gram-positive bacteria: C.M. Schempp, et al.; Lancet 353, 2129 (1999) Abstract
Hyperforin, a major antidepressant constituent of St. John's Wort, inhibits serotonin uptake by elevating free intracellular Na+1: A. Singer, et al.; J. Pharmacol. Exp. Ther. 290, 1363 (1999) Abstract
St. John's wort induces hepatic drug metabolism through activation of the pregnane X receptor: L.B. Moore, et al.; PNAS 97, 7500 (2000) Abstract
Inhibition of human cytochrome P450 enzymes by constituents of St. John's Wort, an herbal preparation used in the treatment of depression: R.S. Obach; J. Pharmacol. Exp. Ther. 294, 88 (2000) Abstract
St John's wort, a herbal antidepressant, activates the steroid X receptor: J.M. Wentworth, et al.; J. Endocrinol. 166, R11 (2000) Abstract
St John's wort (Hypericum perforatum L.): a review of its chemistry, pharmacology and clinical properties: J. Barnes, et al.; J. Pharm. Pharmacol. 53, 583 (2001), (Review) Abstract
St John's wort: Prozac from the plant kingdom: G. Di Carlo, et al.; TIPS 22, 292 (2001), (Review) Abstract
Effect of St. John's wort on free radical production: E.J. Hunt, et al.; Life Sci. 69, 181 (2001) Abstract
Hypericum perforatum (St John's Wort): a non-selective reuptake inhibitor? A review of the recent advances in its pharmacology: P.J. Nathan; J. Psychopharmacol. 15, 47 (2001), (Review) Abstract
Aristoforin, a novel stable derivative of hyperforin, is a potent anticancer agent: M. Gartner, et al.; Chembiochem 6, 171 (2005) Abstract
Hyperforin, a new lead compound against the progression of cancer and leukemia?: C. Quiney, et al.; Leukemia 20, 1519 (2006), (Review) Abstract
Hyperforin a key constituent of St. John’s wort specifically activates TRPC6 channels: K. Leuner, et al.; FASEB J. 21, 4101 (2007) Abstract
Further Categories Containing This Product:
Other Natural Products - DNA Regulation / Transcription • Pregnane X Receptor [PXR] / Related Products • Natural Products - Anti-inflammatory Agents • Natural Products for Angiogenesis Research • Natural Products - Antitumor Reagents • Natural Products with Antibiotic Activity • Antitumor Agents (Apoptosis Inducers) • Neuroactive Agents Other Products • Natural Products - Apoptosis Inducers & Inhibitors
 
 
ALX-350-030 Revised 07-Apr-08
Hypericin (native)
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-030-M001   1 mg 50.00 USD Add To Cart
ALX-350-030-M005   5 mg 200.00 USD Add To Cart
ALX-350-030-M010   10 mg 370.00 USD Add To Cart
Product Specification
FORMULA: C30H16O8
MW: 504.4
CAS NUMBER: 548-04-9
MERCK INDEX: 14: 4863
SOURCE/HOST: Isolated from Hypericum perforatum.
PURITY: ≥98%
APPEARANCE: Black to black-red powder.
SOLUBILITY: Soluble in DMSO, 100% ethanol, methanol, acetone, ethylmethylketone, pyridine or other organic solvents and bases.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.
HAZARD: MAY BE TERATOGENIC. HARMFUL. MAY BE MUTAGENIC.

Product Description
Inhibitor of protein kinase C (PKC). Shows anti-viral and anti-retroviral activity. Displays antineoplastic and antitumor activities. Inhibits casein kinase II (CKII) and MAP kinase. Bright red fluorescence emission and photostability. Antidepressant.
Product Specific Literature References
Therapeutic agents with dramatic antiretroviral activity and little toxicity at effective doses: aromatic polycyclic diones hypericin and pseudohypericin: D. Meruelo, et al.; PNAS 85, 5230 (1988) Abstract
Hypericin and pseudohypericin specifically inhibit protein kinase C: possible relation to their antiretroviral activity: I. Takahashi, et al.; BBRC 165, 1207 (1989) Abstract
Evaluation of the antiviral activity of anthraquinones, anthrones and anthraquinone derivatives against human cytomegalovirus: D.L. Barnard, et al.; Antiviral Res. 17, 63 (1992) Abstract
Photosensitized inhibition of growth factor-regulated protein kinases by hypericin: P. Agostinis, et al.; Biochem. Pharmacol. 49, 1615 (1995) Abstract
Growth inhibition and apoptosis in human neuroblastoma SK-N-SH cells induced by hypericin, a potent inhibitor of protein kinase C: W. Zhang, et al.; Cancer Lett. 96, 31 (1995) Abstract
Hypericin-induced photosensitization of HeLa cells leads to apoptosis or necrosis. Involvement of cytochrome c and procaspase-3 activation in the mechanism of apoptosis: A. Vantieghem, et al.; FEBS Lett. 440, 19 (1998) Abstract
The activation of the c-Jun N-terminal kinase and p38 mitogen-activated protein kinase signaling pathways protects HeLa cells from apoptosis following photodynamic therapy with hypericin: Z. Assefa, et al.; J. Biol. Chem. 274, 8788 (1999) Abstract; Full Text
Over-expression of Bcl-2 does not protect cells from hypericin photo- induced mitochondrial membrane depolarization, but delays subsequent events in the apoptotic pathway: R. Chaloupka, et al.; FEBS Lett. 462, 295 (1999) Abstract
Hypericin induces both differentiation and apoptosis in human promyelocytic leukemia HL-60 cells: K.T. Lee, et al.; Biol. Pharm. Bull. 22, 1271 (1999) Abstract
Apoptotic and anti-apoptotic signaling pathways induced by photodynamic therapy with hypericin: P. Agostinis, et al.; Adv. Enzyme Regul. 40, 157 (2000) Abstract
Hypericin--a new antiviral and antitumor photosensitizer: mechanism of action and interaction with biological macromolecules: P. Miskovsky; Curr. Drug Targets 3, 55 (2002), (Review) Abstract
Hypericin--the facts about a controversial agent: A. Kubin, et al.; Curr. Pharm. Des. 11, 233 (2005), (Review) Abstract
Cellular mechanisms and prospective applications of hypericin in photodynamic therapy: T. Kiesslich, et al.; Curr. Med. Chem. 13, 2189 (2006), (Review) Abstract
Further Categories Containing This Product:
Casein Kinase Inhibitors • MAPK Pathway Inhibitors • PKC Inhibitors • Natural Products - Antitumor Reagents • Neuroactive Agents Other Products • Natural Products for Neurological Research • Natural Products - Antiviral / anti-HIV Agents
 
 
ALX-380-116 Revised 07-Apr-08
Hypothemycin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Antifungal
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ALX-380-116-C250   250 µg 140.00 USD Add To Cart
ALX-380-116-M001   1 mg 420.00 USD Add To Cart
Product Specification
FORMULA: C19H22O8
MW: 378.4
CAS NUMBER: 76958-67-3
SOURCE/HOST: Isolated from Phoma sp.
PURITY: ≥98% (HPLC)
APPEARANCE: Off-white solid.
SOLUBILITY: Soluble in DMSO or acetone; insoluble in methanol or water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Exhibits antifungal and cytotoxic activity against some tumor cell lines partly attributed to inhibition of Ras-inducible genes. Inhibits proliferation of mouse and human T cells and modulates production of cytokines during T cell activation. Facilitates the ubiquitinylation process of cyclin D1. Has been identified as a potent and selective inhibitor of threonine/tyrosine-specific kinase, MEK, and other protein kinases that contain a conserved cysteine residue in the ATP-binding site in both in vitro and in vivo studies.
Product Specific Literature References
Metabolites of pyrenomycetes XIII: Structure of (+) hypothemycin, an antibiotic macrolide from hypomyces trichothecoides: M.S.R. Nair & S.T. Carey; Tetrahedron Lett. 21, 2011 (1980)
Metabolites of pyrenomycetes. XIV: Structure and partial stereochemistry of the antibiotic macrolides hypothemycin and dihydrohypothemycin: M.S.R. Nair, et al.; Tetrahedron 37, 2445 (1981)
Revised structure and stereochemistry of hypothemycin: T. Agatsuma et al.; Chem. Pharm. Bull. 41, 373 (1993)
Antitumor efficacy of hypothemycin, a new Ras-signaling inhibitor: H. Tanaka, et al.; Jpn. J. Cancer Res. 90, 1139 (1999) Abstract
Hypothemycin inhibits the proliferative response and modulates the production of cytokines during T cell activation: R. Camacho, et al.; Immunopharmacology 44, 255 (1999) Abstract
Suppression of oncogenic transformation by hypothemycin associated with accelerated cyclin D1 degradation through ubiquitin-proteasome pathway: H. Sonoda, et al.; Life Sci. 65, 381 (1999) Abstract
Resorcylic acid lactones: naturally occurring potent and selective inhibitors of MEK: A. Zhao, et al.; J. Antibiot. 52, 1086 (1999) Abstract
Targeted covalent inactivation of protein kinases by resorcylic acid lactone polyketides: A. Schirmer, et al.; PNAS 103, 4234 (2006) Abstract; Full Text
Chemistry and biology of resorcylic acid lactones: N. Winssinger, et al.; Chem. Commun. (Camb). 1, 22 (2007), (Review) Abstract
Further Categories Containing This Product:
MAPK Pathway Inhibitors • Antitumor Antibiotics • Antibiotics - Protein Kinase Inhibitors • Tyrosine Kinase Inhibitors • Antitumor Agents (DNA Interaction & Gene Regulation) • Ras Signalling Pathway Other Products • Antibiotics - Proteasome / Ubiquitin Modulators • Ubiquitination Other Products • CDKs & Cyclins Other Products
 
 
ALX-550-249 Revised 27-May-03
Ibuprofen
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SYNONYMS α-Methyl-4-(2-methylpropyl)benzeneacetic acid
(±)-2-(4-Isobutylphenyl)propionic acid
PRODUCT LINE Inflammation
PRODUCT CATEGORY Non-Steroidal Anti-Inflammatory Drugs [NSAIDS]
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ALX-550-249-G001   1 g 17.00 USD Add To Cart
ALX-550-249-G005   5 g 48.00 USD Add To Cart
Product Specification
FORMULA: C13H18O2
MW: 206.3
CAS NUMBER: 15687-27-1
MERCK INDEX: 14: 4881
PURITY: ≥99%
APPEARANCE: White solid.
SOLUBILITY: Soluble in methanol or dilute aqueous base.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C

Product Description
Selective cyclooxygenase (COX) inhibitor.
Product Specific Literature References
Differential effects of anti-inflammatory drugs on lipoxygenase and cyclo-oxygenase activities of neutrophils from a reverse passive Arthus reaction: R.F. Myers & M.I. Siegel; BBRC 112, 586 (1983) Abstract
Suppression of inflammatory oedema by ibuprofen involving a mechanism independent of cyclo-oxygenase inhibition: M. Rampart & T.J. Williams; Biochem. Pharmacol. 35, 581 (1986) Abstract
Further Categories Containing This Product:
COX Inhibitors
 
 
ALX-380-260 Revised 07-Apr-08
Idarubicin . hydrochloride
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SYNONYMS Idamycin
DMDR
4-Demethoxydaunorubicin
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Apoptosis Inducers & Inhibitors
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ALX-380-260-M001   1 mg 45.00 USD Add To Cart
ALX-380-260-M005   5 mg 180.00 USD Add To Cart
Product Specification
FORMULA: C26H27NO9 . HCl
MW: 497.5 . 36.5
CAS NUMBER: 57852-57-0
MERCK INDEX: 14: 4886
RTECS: HB7877000
SOURCE/HOST: Synthetic.
PURITY: ≥98%
APPEARANCE: Orange crystalline solid.
SOLUBILITY: Soluble in water or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: VERY TOXIC. MAY BE TERATOGENIC. MAY BE CARCINOGENIC.

Product Description
More potent, lipophilic and antineoplastic analog of daunorubicin. DNA-damaging effect includes DNA oxidation and methylation, DNA intercalation, inhibition of DNA synthesis, induction of DNA strand breaks and delay of cell cycle progression. Inhibitor of topoisomerase IIα. Produces endonucleolytic cleavage and is a marker of apoptosis.
Product Specific Literature References
Idarubicin (4-demethoxydaunorubicin). A preliminary overview of preclinical and clinical studies: F. Ganzina, et al.; Invest. New Drugs 4, 85 (1986), Review Abstract
Antitumor activity of idarubicin, a derivative of daunorubicin, against drug sensitive and resistant P388 leukemia: T. Tsuruo, et al.; Anticancer Res. 13, 357 (1993) Abstract
Study of apoptosis-related responses of leukemic blast cells to in vitro anthracycline treatment: M.A. Belaud-Rotureau, et al.; Leukemia 14, 1266 (2000) Abstract
A comparison of the in vitro genotoxicity of anticancer drugs idarubicin and mitoxantrone: J. Blasiak, et al.; Acta Biochim. Pol. 49, 145 (2002) Abstract; Full Text
Repair of idarubicin-induced DNA damage: A cause of resistance?: D.C. Dartsch & F. Gieseler; DNA Repair (Amst) 6, 1618 (2007) Abstract
Further Categories Containing This Product:
Antitumor Agents (DNA Interaction & Gene Regulation) • Antitumor Agents (Apoptosis Inducers) • Antitumor Antibiotics • Antibiotics - Topoisomerase Inhibitors
 
 
ALX-350-240 Revised 05-Dec-07
Ilimaquinone
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SYNONYMS 3-[(Decahydro-1β,2β,4αβ-trimethyl-5-methylene-1-naphthyl)methyl]-2-hydroxy-5-methoxybenzoquinone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Other Signal Transduction Pathway Modulators
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ALX-350-240-C100   100 µg 140.00 USD Add To Cart
Product Specification
FORMULA: C22H30O4
MW: 358.5
CAS NUMBER: 71678-03-0
PURITY: ≥98%
APPEARANCE: Yellow powder.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Displays antimicrobial, anti-HIV and anti-inflammatory properties. Induces reversible breakdown of Golgi membranes. Inhibits the association of β-COP and ADP-ribosylation factor to Golgi membranes. Interacts with methylation enzymes. Shows anticancer activity.
Product Specific Literature References
R.T. Luibrand, et al.; Tetrahedron 35, 609 (1979)
Complete vesiculation of Golgi membranes and inhibition of protein transport by a novel sea sponge metabolite, ilimaquinone: P.A. Takizawa, et al.; Cell 73, 1079 (1993) Abstract
Interactions of (-)-ilimaquinone with methylation enzymes: implications for vesicular-mediated secretion: H.S. Radeke, et al.; Chem. Biol. 6, 639 (1999) Abstract
Ilimaquinone inhibits gap-junctional communication prior to Golgi fragmentation and block in protein transport: V. Cruciani, et al.; Exp. Cell Res. 287, 130 (2003) Abstract
Natural products with anti-HIV activity from marine organisms: L.A. Tziveleka, et al.; Curr. Top. Med. Chem. 3, 1512 (2003), Review Abstract
Interaction of the smooth endoplasmic reticulum and mitochondria: J.G. Goetz & I.R. Nabi; Biochem. Soc. Trans. 34, 370 (2006), Review Abstract
Ilimaquinone, a marine sponge metabolite, displays anticancer activity via GADD153-mediated pathway: P.H. Lu, et al.; Eur. J. Pharmacol. 556, 45 (2007) Abstract
Further Categories Containing This Product:
Natural Products - Anti-inflammatory Agents • ADP Ribosylation Factor [ARF] / Related Products • Golgi Apparatus • Natural Products - Chemopreventive Agents • PRMTs, Mono- & Dimethylarginine / Related Products • Natural Products - Antiviral / anti-HIV Agents
 
 
ALX-420-039 Revised 14-Aug-08
Imiquimod
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SYNONYMS 1-(2-Methylpropyl)-1H-imidazo[4,5-c]quinolin-4-amine
R-837
PRODUCT LINE Inflammation
PRODUCT CATEGORY TLR Agonists Other Products
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ALX-420-039-M100   100 mg 55.00 USD Add To Cart
ALX-420-039-M250   250 mg 120.00 USD Add To Cart
Product Specification
FORMULA: C14H16N4
MW: 240.3
CAS NUMBER: 99011-02-6
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO (3mg/ml) or dimethyl formamide; slightly soluble in water (warm to 37°C, vortex); insoluble in 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for up