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Antitumor Reagents
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ALX-380-117 Revised 10-Apr-07
UK-1
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Antifungal
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ALX-380-117-C250   250 µg 140.00 USD Add To Cart
ALX-380-117-M001   1 mg 420.00 USD Add To Cart
Product Specification
FORMULA: C22H14N2O5
MW: 386.4
CAS NUMBER: 151271-53-3
SOURCE/HOST: Isolated from Streptomyces sp.
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO, dimethyl formamide or acetone.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Antibiotic. Antifungal. Inhibitor of topoisomerase II (Topo II). Mg2+- and Zn2+-dependent DNA binding agent. Displays a wide spectrum of potent anticancer activities.
Product Specific Literature References
UK-1, a novel cytotoxic metabolite from Streptomyces sp. 517-02. I. Taxonomy, fermentation, isolation, physico-chemical and biological properties: M. Ueki, et al.; J. Antibiot. 46, 1089 (1993) Abstract
UK-1, a novel cytotoxic metabolite from Streptomyces sp. 517-02. II. Structural elucidation: K. Shibata, et al.; J. Antibiot. 46, 1095 (1993) Abstract
UK-1, a novel cytotoxic metabolite from Streptomyces sp. 517-02. III. Antibacterial action of demethyl UK-1: M. Ueki and M. Taniguchi; J. Antibiot. 50, 788 (1997) Abstract
UK-1, a novel cytotoxic metabolite from Streptomyces sp. 517-02. IV. Antifungal action of methyl UK-1: M. Ueki, et al.; J. Antibiot. 51, 883 (1998) Abstract
The novel bis(benzoxazole) cytotoxic natural product UK-1 is a magnesium ion-dependent DNA binding agent and inhibitor of human topoisomerase II: M.B. Reynolds, et al.; Bioorg. Chem. 27, 326 (1999)
Evaluation of complexation of metal-mediated DNA-binding drugs to oligonucleotides via electrospray ionization mass spectrometry: M.L. Reyzer, et al.; Nucl. Acids Res. 29, E103 (2001) Abstract; Full Text
Synthesis and evaluation of anticancer benzoxazoles and benzimidazoles related to UK-1: D. Kumar, et al.; Bioorg. Med. Chem. 10, 3997 (2002) Abstract
Critical structural motif for the catalytic inhibition of human topoisomerase II by UK-1 and analogs: B.B. Wang, et al.; Bioorg. Med. Chem. Lett. 14, 3221 (2004) Abstract
Synthesis and antimicrobial activity of some 5-[2-(morpholin-4-yl)acetamido] and/or 5-[2-(4-substituted piperazin-1-yl)acetamido]-2-(p-substituted phenyl)benzoxazoles: O. Temiz-Arpaci, et al.; Arch. Pharm. 338, 105 (2005) Abstract
Synthesis and anticancer evaluation of bis(benzimidazoles), bis(benzoxazoles), and benzothiazoles: S.T. Huang, et al.; Bioorg. Med. Chem. 14, 6106 (2006) Abstract
Further Categories Containing This Product:
Antibiotics - Topoisomerase Inhibitors • Antitumor Antibiotics • Antitumor Agents (DNA Interaction & Gene Regulation)
 
 
ALX-270-194 Revised 19-Sep-05
Valeryl salicylate
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SYNONYMS 2-Valeryloxybenzoic acid
PRODUCT LINE Inflammation
PRODUCT CATEGORY Non-Steroidal Anti-Inflammatory Drugs [NSAIDS]
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ALX-270-194-M100   100 mg 51.00 USD Add To Cart
Product Specification
FORMULA: C12H14O4
MW: 222.2
CAS NUMBER: 64206-54-8
PURITY: ≥99%
APPEARANCE: White crystalline solid.
SOLUBILITY: Soluble in 100% ethanol (95mg/ml), methanol, DMSO (43mg/ml) or dimethyl formamide (70mg/ml); also soluble in PBS, pH 7.2 (6mg/ml)). Insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C

Product Description
Selective inhibitor of cyclooxygenase-1 (COX-1).
Product Specific Literature References
Selective inhibition of prostaglandin endoperoxide synthase-1 (cyclooxygenase-1) by valerylsalicylic acid: D.K. Bhattacharyya, et al.; Arch. Biochem. Biophys. 317, 19 (1995) Abstract
Purification and characterization of prostaglandin H synthase-2 from sheep placental cotyledons: J.L. Johnson, et al.; Arch. Biochem. Biophys. 324, 26 (1995) Abstract
Further Categories Containing This Product:
COX Inhibitors
 
 
ALX-550-306 Revised 09-Nov-07
(±)-Verapamil . hydrochloride
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SYNONYMS 5-[(3,4-Dimethoxyphenylethyl)methylamino]-2-(3,4-dimethoxyphenyl)-2-isopropyl-valeronitrile . HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Ca2+ Channels (L-type)
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ALX-550-306-G001   1 g 24.00 USD Add To Cart
ALX-550-306-G005   5 g 80.00 USD Add To Cart
Product Specification
FORMULA: C27H38N2O4 . HCl
MW: 454.6 . 36.5
CAS NUMBER: 152-11-4
MERCK INDEX: 14: 9950
RTECS: YV8320000
PURITY: ≥99%
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in 100% ethanol, methanol or water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
HAZARD: TOXIC.

Product Description
Blocks L-type Ca2+ channels. Adrenergic antagonist. Inhibits platelet-activating factor and PMA-stimulated prostaglandin production in Kupffer cells. Induces apoptosis. In vitro resistance modifier in drug resistant human tumor cell lines.
Product Specific Literature References
Specific pharmacology of calcium in myocardium, cardiac pacemakers, and vascular smooth muscle: A. Fleckenstein; Ann. Rev. Pharmacol. 17, 149 (1977) Abstract
alpha-adrenergic antagonists as possible calcium channel inhibitors: D. Atlas & M. Adler; PNAS 78, 1237 (1981) Abstract
Effect of trifluoperazine, compound 48/80, TMB-8 and verapamil on the rate of calmodulin binding to erythrocyte Ca2+-ATPase: O. Scharff & B. Foder; Biochim. Biophys. Acta 772, 29 (1984) Abstract
Participation of intracellular sites in the action of Ca2+ channel blockers: E.J. White & H.F. Bradford; Eur. J. Pharmacol. 130, 243 (1986) Abstract
R. Janis, et al.; Adv. Drug Res. 16, 309 (1987)
Goodman and Gilman's The Pharmacological Basis of Therapeutics, vol. 8; p. 774 (1990)
Functional imaging of multidrug-resistant P-glycoprotein with an organotechnetium complex: D. Piwnica-Worms, et al.; Cancer Res. 53, 977 (1993) Abstract
Effect of high-dose verapamil administration on the Ca2+ channel density in rat cardiac tissue: B.B. Lonsberry, et al.; Pharmacology 49, 23 (1994) Abstract
Apoptosis of human primary and metastatic colon adenocarcinoma cell lines in vitro induced by 5-fluorouracil, verapamil, and hyperthermia: I.B. Shchepotin, et al.; Anticancer Res. 14, 1027 (1994) Abstract
Apoptosis induced by hyperthermia and verapamil in vitro in a human colon cancer cell line: I.B. Shchepotin, et al.; Int. J. Hyperthermia 13, 547 (1997) Abstract
Hyperthermia and verapamil inhibit the growth of human colon cancer xenografts in vivo through apoptosis: I.B. Shchepotin, et al.; Anticancer Res. 17, 2213 (1997) Abstract
Neuron degeneration induced by verapamil and attenuated by EGb761: L. Zhu, et al.; J. Basic Clin. Physiol. Pharmacol. 8, 301 (1997) Abstract
Further Categories Containing This Product:
Adrenergics & Adrenergic Receptors / Related Products • Chemopreventive Agents Other Products
 
 
ALX-350-257 Revised 08-Oct-08
Vinblastine . sulfate
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SYNONYMS Vincaleukoblastine . sulfate
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products for Cell Cycle Research
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ALX-350-257-M005   5 mg 45.00 USD Add To Cart
ALX-350-257-M025   25 mg 190.00 USD Add To Cart
Product Specification
FORMULA: C46H58N4O9 . H2SO4
MW: 811.0 . 98.1
CAS NUMBER: 143-67-9
MERCK INDEX: 14: 9982
SOURCE/HOST: Semisynthetic from catharanthine or vindoline.
PURITY: ≥98%
APPEARANCE: White powder.
SOLUBILITY: Soluble in DMSO, methanol or water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: TOXIC. MAY BE CARCINOGENIC.

Product Description
Plant alkaloid that arrests the cell cycle in G2/M phase by blocking mitotic spindle formation. Depolymerizes microtubules and blocks binding of tubulin to microtubule proteins. Induces apoptosis. Triggers Raf-1 activation, phosphorylation of Bcl-2 family proteins and induction of p53 expression.
Product Specific Literature References
Microtubule antagonists activate programmed cell death (apoptosis) in cultured rat hepatocytes: K. Tsukidate, et al.; Am. J. Pathol. 143, 918 (1993) Abstract
Resistance of Ehrlich tumor cells to apoptosis can be due to accumulation of heat shock proteins: V.L. Gabai, et al.; FEBS Lett. 375, 21 (1995) Abstract
The interaction of taxol and vinblastine with radiation induction of p53 and p21 WAF1/CIP1: R.B. Tishler & D.M. Lamppu; Br. J. Cancer. Suppl. 27, S82 (1996) Abstract
Raf-1/bcl-2 phosphorylation: a step from microtubule damage to cell death: M.V. Blagosklonny, et al.; Cancer Res. 57, 130 (1997) Abstract
Tubulin as a target for anticancer drugs: agents which interact with the mitotic spindle: A. Jordan, et al.; Med. Res. Rev. 18, 259 (1998) Abstract
The C terminus of beta-tubulin regulates vinblastine-induced tubulin polymerization: S.S. Rai & J. Wolff; PNAS 95, 4253 (1998) Abstract; Full Text
Caspase-3 activation is not responsible for vinblastine-induced Bcl-2 phosphorylation and G2/M arrest in human small cell lung carcinoma Ms-1 cells: E. Tashiro, et al.; Jpn. J. Cancer Res. 89, 940 (1998) Abstract
Use of drugs to study role of microtubule assembly dynamics in living cells: A. Jordan & L. Wilson; Meth. Enzymol. 298, 252 (1998) Abstract
Vinblastine-induced phosphorylation of Bcl-2 and Bcl-XL is mediated by JNK and occurs in parallel with inactivation of the Raf-1/MEK/ERK cascade: M. Fan, et al.; J. Biol. Chem. 275, 29980 (2000) Abstract; Full Text
Vinblastine, a chemotherapeutic drug, inhibits palmitoylation of tubulin in human leukemic lymphocytes: J.M. Caron & M. Herwood; Chemotherapy 53, 51 (2007) Abstract
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Further Categories Containing This Product:
Microtubule Modulators • Alkaloids • Cell Cycle Blockers & Inhibitors / Related Products • Antitumor Agents (Apoptosis Inducers) • Natural Products for Cytoskeletal Research • Natural Products - Apoptosis Inducers & Inhibitors • Natural Products - Antitumor Reagents • Autophagy Blockers & Inhibitors / Related Products
 
 
ALX-350-069 Revised 02-Oct-08
Vincristine . sulfate
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SYNONYMS VCR . sulfate
Leukocristine . sulfate
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products for Cell Cycle Research
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ALX-350-069-M001   1 mg 35.00 USD Add To Cart
ALX-350-069-M005   5 mg 95.00 USD Add To Cart
Product Specification
FORMULA: C46H56N4O10 . H2SO4
MW: 825.0 . 98.1
CAS NUMBER: 2068-78-2
MERCK INDEX: 14: 9986
RTECS: OH6340000
SOURCE/HOST: Semisynthetic from catharanthine or vindoline.
PURITY: ≥95%
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in water (25mg/ml) or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least 1 year after receipt when stored at -20°C. Stock solutions are stable for up to 3 months at -20°C.
HANDLING: Protect from light and moisture.
HAZARD: MAY BE TERATOGENIC.

Product Description
Plant alkaloid that arrests the cell cycle in G2/M phase by blocking mitotic spindle formation. Depolymerizes microtubules and blocks binding of tubulin to microtubule proteins. Induces apoptosis. Triggers Raf-1 activation, phosphorylation of Bcl-2 family proteins and induction of p53 expression.
Product Specific Literature References
Cell death induced by vincristine in the intestinal crypts of mice and in a human Burkitt's lymphoma cell line: B.V. Harmon, et al.; Cell Prolif. 25, 523 (1992) Abstract
Binding selectivity of rhizoxin, phomopsin A, vinblastine, and ansamitocin P-3 to fungal tubulins: differential interactions of these antimitotic agents with brain and fungal tubulins [published erratum appears in BBRC 190, 1180 (1993)]: Y. Li, et al.; BBRC 187, 722 (1992) Abstract
Interaction of vinca alkaloids with tubulin: a comparison of vinblastine, vincristine, and vinorelbine: S. Lobert, et al.; Biochemistry 35, 6806 (1996) Abstract
Raf-1/bcl-2 phosphorylation: a step from microtubule damage to cell death: M.V. Blagosklonny, et al.; Cancer Res. 57, 130 (1997) Abstract
Tubulin as a target for anticancer drugs: agents which interact with the mitotic spindle: A. Jordan, et al.; Med. Res. Rev. 18, 259 (1998) Abstract
Bcl-xL is phosphorylated in malignant cells following microtubule disruption: M.S. Poruchynsky, et al.; Cancer Res. 58, 3331 (1998) Abstract
The effect of antimicrotubule agents on signal transduction pathways of apoptosis: a review: L.G. Wang, et al.; Cancer Chemother. Pharmacol. 44, 355 (1999), (Review) Abstract
Vincristine-induced apoptosis in vivo in peripheral blood mononuclear cells of children with acute lymphoblastic leukaemia (ALL): E. Groninger, et al.; Br. J. Haematol. 111, 875 (2000) Abstract
Selective toxicity of vincristine against chronic lymphocytic leukemia cells in vitro: J.A. Vilpo, et al.; Eur. J. Haematol. 65, 370 (2000) Abstract
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Further Categories Containing This Product:
Antitumor Agents (Anti-proliferative) • Microtubule Modulators • Cell Cycle Blockers & Inhibitors / Related Products • Natural Products for Cytoskeletal Research • Antitumor Agents (Apoptosis Inducers) • Alkaloids • Natural Products - Apoptosis Inducers & Inhibitors • Natural Products - Antitumor Reagents • Antitumor Agents (DNA Interaction & Gene Regulation)
 
 
ALX-350-102 Revised 25-Mar-08
Vindoline
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SYNONYMS (2β,3β,4β,5α,12β,19α)-4-(Acetyloxy)-6,7-didehydro-3-hydroxy-16-methoxy-1-methyl-aspidospermidine-3-carbox
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products for Cytoskeletal Research
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ALX-350-102-M100   100 mg 160.00 USD Add To Cart
ALX-350-102-G001   1 g 430.00 USD Add To Cart
Product Specification
FORMULA: C25H32N2O6
MW: 456.5
CAS NUMBER: 2182-14-1
MERCK INDEX: 14: 9988
SOURCE/HOST: Isolated from Catharanthus roseus.
PURITY: ≥90%
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Very hygroscopic.

Product Description
Lacks physiological activity itself, but is contained as the pentacyclic moiety in the antineoplastic agents vinblastine and vincristine.
Product Specific Literature References
Photochemical one-pot synthesis of vinblastine and vincristine: S. Pennanen & A. Huhtikangas; Photochem. Photobiol. 51, 515 (1990) Abstract
Mechanism of interaction of vinca alkaloids with tubulin: catharanthine and vindoline: V. Prakash & S.N. Timasheff; Biochemistry 30, 873 (1991) Abstract
Antimitotic agents: chemistry and recognition of tubulin molecule: S. Iwasaki; Med. Res. Rev. 13, 183 (1993) Abstract
Catharanthus roseus L. plants and explants infected with phytoplasmas: alkaloid production and structural observations: M.A. Favali, et al.; Protoplasma 223, 45 (2004) Abstract
Related Products
Further Categories Containing This Product:
Microtubule Modulators • Natural Products - Antitumor Reagents • Antitumor Agents (Apoptosis Inducers) • Alkaloids • Natural Products - Apoptosis Inducers & Inhibitors
 
 
ALX-350-153 Revised 28-Jul-08
Withaferin A
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SYNONYMS 5,6-Epoxy-4,27-dihydroxy-1-oxowitha-2,24-dienolide
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antitumor Reagents
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ALX-350-153-M001   1 mg 60.00 USD Add To Cart
ALX-350-153-M005   5 mg 240.00 USD Add To Cart
Product Specification
FORMULA: C28H38O6
MW: 470.6
CAS NUMBER: 5119-48-2
MERCK INDEX: 14: 10048
RTECS: KE7288500
SOURCE/HOST: Isolated from Withania somnifera.
PURITY: ≥94% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO (20 mg/ml), methanol (10 mg/ml) or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: MAY BE MUTAGENIC. MAY BE CARCINOGENIC. HARMFUL.

Product Description
Cell permeable and potent angiogenesis inhibitor from the family of withanolides. Inhibits endothelial cells (HUVEC) sprouting in vitro (IC50=12nM) and in vivo. Exhibits antitumor, anti-inflammatory, radiosensitizing, and immunosuppressive properties. Potently inhibits NF-κB activation by preventing the TNF-induced activation of IκB kinase β (IKKβ). Affects AP1 transcription and induces cell death. Alters cytoskeletal architecture by covalently binding annexin II and stimulating its basal F-actin cross-linking activity which inhibits the migratory and invasive capability of endothelial cells. Displays neuronal regenerative properties. Targets the intermediate filament protein vimentin.
Product Specific Literature References
Tumor inhibitors. XXXIX. Active principles of Acnistus arborescens. Isolation and structural and spectral studies of withaferin A and withacnistin: S.M. Kupchan, et al.; J. Org. Chem. 34, 3858 (1969) Abstract
In vivo growth inhibitory and radiosensitizing effects of withaferin A on mouse Ehrlich ascites carcinoma: P.U. Devi, et al.; Cancer Lett. 95, 189 (1995) Abstract
Growth inhibition of human tumor cell lines by withanolides from Withania somnifera leaves: B. Jayaprakasam, et al.; Life Sci. 74, 125 (2003) Abstract
Withaferin A is a potent inhibitor of angiogenesis: R. Mohan, et al.; Angiogenesis 7, 115 (2004) Abstract
Neuritic regeneration and synaptic reconstruction induced by withanolide: A: T. Kuboyama, et al.; Br. J. Pharmacol. 144, 961 (2005) Abstract; Full Text
Actin microfilament aggregation induced by withaferin A is mediated by annexin II: R.R. Falsey, et al.; Nat. Chem. Biol. 2, 33 (2006) Abstract
Withaferin a strongly elicits IkappaB kinase beta hyperphosphorylation concomitant with potent inhibition of its kinase activity: M. Kaileh, et al.; J. Biol. Chem. 282, 4253 (2007) Abstract; Full Text
The tumor inhibitor and antiangiogenic agent withaferin A targets the intermediate filament protein vimentin: P. Bargagna-Mohan, et al.; Chem. Biol. 14, 623 (2007) Abstract
Further Categories Containing This Product:
Natural Products - Immunomodulators • Natural Products for Angiogenesis Research • Vimentin / Related Products • Natural Products - NF-kB Pathway Inhibitors • Antitumor Agents (Apoptosis Inducers) • Natural Products for Cytoskeletal Research • NF-kB Pathway Inhibitors • Natural Products - Anti-inflammatory Agents
 
 
ALX-385-033 Revised 28-May-08
Wogonin
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SYNONYMS 5,7-Dihydroxy-8-methoxyflavone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Flavones
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ALX-385-033-M005   5 mg 60.00 USD Add To Cart
ALX-385-033-M025   25 mg 210.00 USD Add To Cart
Product Specification
FORMULA: C16H12O5
MW: 284.3
CAS NUMBER: 632-85-9
RTECS: LK8331000
PURITY: ≥98% (HPLC)
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO (10mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.

Product Description

Cell permeable and orally available flavonoid. Induces apoptosis in tumor cells but not in healthy cells by increasing peroxide production. Displays anti-inflammatory properties. Suppresses the release of nitric oxide (NO) by inducible nitric oxide synthase (iNOS; NOS II), PGE2 by cyclooxygenase-2 (COX-2), proinflammatory cytokines, MCP-1 gene expression and NF-κB activation. Antioxidant.
Product Specific Literature References
The anti-inflammatory activity of Scutellaria rivularis extracts and its active components, baicalin, baicalein and wogonin: C.C. Lin & D.E. Shieh; Am. J. Chin. Med. 24, 31 (1996) Abstract
Inhibitory effects of baicalein and wogonin on lipopolysaccharide-induced nitric oxide production in macrophages: I. Wakabayashi; Pharmacol. Toxicol. 84, 288 (1999) Abstract
Antitumor effects of Scutellariae radix and its components baicalein, baicalin, and wogonin on bladder cancer cell lines: S. Ikemoto, et al.; Urology 55, 951 (2000)