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Chemopreventive Agents & Inhibitors of Carcinogenesis
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ALX-270-171 Revised 30-Jun-08
Chlorpromazine . hydrochloride
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SYNONYMS 2-Chloro-10-(3-dimethylaminopropyl)phenothiazine . HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Calmodulin Inhibitors
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ALX-270-171-G001   1 g 22.00 USD Add To Cart
ALX-270-171-G005   5 g 66.00 USD Add To Cart
Product Specification
FORMULA: C17H19ClN2S . HCl
MW: 318.9 . 36.5
CAS NUMBER: 69-09-0
MERCK INDEX: 14: 2185
RTECS: SO1750000
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in 100% ethanol, methanol or water (50mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Not stable in aqueous solution. We strongly recommend always to use freshly prepared solutions.
HANDLING: Protect from light.
HAZARD: VERY TOXIC.

Product Description
Inhibits calmodulin stimulation of cyclic nucleotide phosphodiesterase. Dopamine antagonist. D2 antagonist. H1 antagonist. Inhibits TNF-α production. Potent PLA2 inhibitor. Inhibits nitric oxide synthase (NOS) in mouse brain and prevents lipopolysaccharide induction of NOS in mouse lung. Antipsychotic.
Product Specific Literature References
Chlorpromazine as a substitute for ortho-dianisidine and ortho-tolidine in the determination of chlorine, hemoglobin, and peroxidase activity: H.B. Collier; Clin. Biochem. 7, 331 (1974) Abstract
Drug-protein interactions: binding of chlorpromazine to calmodulin, calmodulin fragments, and related calcium binding proteins: D.R. Marshak, et al.; Biochemistry 24, 144 (1985) Abstract
Selective inhibition of group II phospholipase A2 by quercetin: M. Lindahl & C. Tagesson; Inflammation 17, 573 (1993) Abstract
Chlorpromazine inhibits both the constitutive nitric oxide synthase and the induction of nitric oxide synthase after LPS challenge: M. Palacios, et al.; BBRC 196, 280 (1993) Abstract
Protective effect of calmodulin inhibitors against acute cyanide- induced lethality and convulsions in mice: H. Yamamoto; Toxicol. Lett. 66, 73 (1993) Abstract
Pharmacologic inhibitors of tumor necrosis factor production exert differential effects in lethal endotoxemia and in infection with live microorganisms in mice: M.G. Netea, et al.; J. Infect. Dis. 171, 393 (1995) Abstract
Pharmacological regulation of mitochondrial nitric oxide synthase: A. Boveris, et al.; Methods Enzymol. 359, 328 (2002) Abstract
Brain mitochondrial nitric oxide synthase: in vitro and in vivo inhibition by chlorpromazine: S. Lores-Arnaiz, et al.; Arch. Biochem. Biophys. 430, 170 (2004) Abstract
Further Categories Containing This Product:
Phosphodiesterases/Related Products • TNF-alpha & TNF Receptors Other Products • NOS Inhibitors (NOS Induction & Enzyme Activity) • PLA2 Inhibitors • Chemopreventive Agents Other Products • Dopaminergics & Dopamine Receptors/Related Products
 
 
ALX-550-516 Revised 21-May-08
Compound A
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SYNONYMS CpdA
2-((4-Acetophenyl)-2-chloro-N-methyl)ethylammonium chloride
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Anti-inflammatory Agents
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ALX-550-516-M005   5 mg 40.00 USD Add To Cart
ALX-550-516-M025   25 mg 120.00 USD Add To Cart
Product Specification
FORMULA: C11H14ClNO2 . HCl
MW: 227.7 . 36.5
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO, 100% ethanol or water.
SHIPPING: SHIPPED ON DRY ICE
LONG TERM STORAGE: -80°C
USE/STABILITY: Stock solutions in ethanol are stable for up to 1 month when stored at -80°C.
HANDLING: Protect from moisture. After reconstitution, prepare aliquots and store at -80°C.

Product Description
Cell permeable, nonsteroidal glucocorticoid receptor modulator with high binding affinity. Exerts anti-inflammatory potential by down-modulating TNF-induced pro-inflammatory gene expression, such as IL-6 and E-selectin. Unlike dexamethasone (Prod. No. ALX-370-002) it does not enhance glucocorticoid response element (GRE)-driven gene expression or induce glucocorticoid receptor (GR) binding to GRE-dependent genes in vivo.
Product Specific Literature References
A fully dissociated compound of plant origin for inflammatory gene repression: K. De Bosscher, et al.; PNAS 102, 15827 (2005) Abstract
A plant-derived ligand favoring monomeric glucocorticoid receptor conformation with impaired transactivation potential attenuates collagen-induced arthritis: P. Dewint, et al.; J. Immunol. 180, 2608 (2008) Abstract
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Further Categories Containing This Product:
GITR & GITRL Other Products • Glucocorticoids & Glucocorticoid Receptors/Related Products • RANK & RANKL/OPG Other Products • NOS Inhibitors (NOS Induction & Enzyme Activity) • DNA & RNA Methyl & Alkyl Transferases/Related Products • Antitumor Agents (Hormone-related) • Natural Products for Cell Cycle Research • Natural Products - Nitric Oxide Pathway Modulators • Natural Products - Chemopreventive Agents • Other Natural Products - DNA Regulation/Transcription
 
 
ALX-350-248 Revised 23-Jun-05
Daidzin
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SYNONYMS Daidzein-7-O-glucoside
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Chemopreventive Agents
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ALX-350-248-M002   2 mg 75.00 USD Add To Cart
ALX-350-248-M010   10 mg 290.00 USD Add To Cart
Product Specification
FORMULA: C21H20O9
MW: 416.4
CAS NUMBER: 552-66-9
MERCK INDEX: 14: 2801
PURITY: ≥98%
APPEARANCE: White to beige powder.
SOLUBILITY: Soluble in DMSO or dilute aqueous base; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Glucoside of the isoflavone daidzein (Prod. No. ALX-350-009) found in soy beans.
Product Specific Literature References
Metabolism of puerarin and daidzin by human intestinal bacteria and their relation to in vitro cytotoxicity: D.H. Kim, et al.; Biol. Pharm. Bull. 21, 628 (1998) Abstract
Daidzin and its antidipsotropic analogs inhibit serotonin and dopamine metabolism in isolated mitochondria: W.M. Keung & B.L. Vallee; PNAS 95, 2198 (1998) Abstract
Daidzein and genistein but not their glucosides are absorbed from the rat stomach: M.K. Piskula, et al.; FEBS Lett. 447, 287 (1999) Abstract
Further Categories Containing This Product:
Active Substances from Fruit and Vegetables • Flavonoids/Related Products
 
 
ALX-307-002 Revised 24-Feb-05
1-D-3-Deoxy-phosphatidylinositol
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SYNONYMS DPI
3-Deoxy-D-myo-inositol 1-[(R)-2,3-bis(hexa-
decanoyloxy)propyl hydrogenphosphate]
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Inositols & Inositolphosphates/Related Products
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ALX-307-002-C100   100 µg 30.00 USD Add To Cart
ALX-307-002-M001   1 mg 150.00 USD Add To Cart
Product Specification
FORMULA: C41H79O12P
MW: 795.0
PURITY: ≥98%
APPEARANCE: Off-white amorphous solid.
SOLUBILITY: Solube in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Antimetabolite of phosphatidylinositol-3-phosphate. Inhibitor of cancer cell colony formation.
Product Specific Literature References
Synthesis and biology of 1D-3-deoxyphosphatidylinositol: a putative antimetabolite of phosphatidylinositol-3-phosphate and an inhibitor of cancer cell colony formation: A.P. Kozikowski, et al.; J. Med. Chem. 38, 1053 (1995) Abstract
Further Categories Containing This Product:
Chemopreventive Agents Other Products
 
 
ALX-370-002 Revised 19-Sep-06
Dexamethasone
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SYNONYMS 9α-Fluoro-16α-methylprednisolone
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY Glucocorticoids & Glucocorticoid Receptors/Related Products
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ALX-370-002-M250   250 mg 22.00 USD Add To Cart
ALX-370-002-G001   1 g 45.00 USD Add To Cart
Product Specification
FORMULA: C22H29FO5
MW: 392.5
CAS NUMBER: 50-02-2
MERCK INDEX: 14: 2943
RTECS: TU3980000
PURITY: ≥98%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO, 100% ethanol or methanol. Slightly soluble in acetone or chloroform. Insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.
HAZARD: HARMFUL. MAY BE TERATOGENIC.

Product Description
Inhibits constitutive OPG mRNA steady-state levels in a dose- and time-dependent fashion, promoting osteoclast formation. Glucocorticoid with anti-inflammatory activity. Inhibits the induction of nitric oxide synthases (NOS).
Product Specific Literature References
Inhibition of the induction of nitric oxide synthase by glucocorticoids: yet another explanation for their anti-inflammatory effects?: S. Moncada & R.M.J. Palmer; TIPS 12, 130 (1991), (Review) Abstract
Glucocorticoids inhibit the induction of nitric oxide synthase and the related cell damage in adenocarcinoma cells: K.J. O'Connor & S. Moncada; Biochim. Biophys. Acta 1097, 227 (1991) Abstract
Nitric oxide mediates tumor necrosis factor-alpha cytotoxicity in endothelial cells: C. Estrada, et al.; BBRC 186, 475 (1992) Abstract
Dexamethasone inhibits the expression of an inducible nitric oxide synthase in infarcted rabbit myocardium: R.R. Dudek, et al.; BBRC 202, 1120 (1994) Abstract
Induction of the alkyltransferase (MGMT) gene by DNA damaging agents and the glucocorticoid dexamethasone and comparison with the response of base excision repair genes: T. Grombacher, et al.; Carcinogenesis 17, 2329 (1996) Abstract
Activation of human O6-methylguanine-DNA methyltransferase gene by glucocorticoid hormone: T. Biswas, et al.; Oncogene 18, 525 (1999) Abstract
Dexamethasone-induced thymocyte apoptosis: apoptotic signal involves the sequential activation of phosphoinositide-specific phospholipase C, acidic sphingomyelinase, and caspases: M.G. Cifone, et al.; Blood 93, 2282 (1999) Abstract; Full Text
Dexamethasone induces apoptosis in human T cell clones expressing low levels of Bcl-2: M.S. Montani, et al.; Cell Death Differ 6, 79 (1999) Abstract
Dexamethasone inhibits the phosphorylation of retinoblastoma protein in the suppression of human vascular smooth muscle cell proliferation: T.D. Reil, et al.; J. Surg. Res. 92, 108 (2000) Abstract
Dexamethasone suppresses iNOS gene expression by inhibiting NF-kappaB in vascular smooth muscle cells: M. Matsumura, et al.; Life Sci. 69, 1067 (2001) Abstract
Dexamethasone inhibits inducible nitric-oxide synthase expression and nitric oxide production by destabilizing mRNA in lipopolysaccharide-treated macrophages: R. Korhonen, et al.; Mol. Pharmacol. 62, 698 (2002) Abstract; Full Text
Molecular mechanisms underlying dexamethasone inhibition of iNOS expression and activity in C6 glioma cells: J. Shinoda, et al.; Glia 42, 68 (2003) Abstract
Dexamethasone prevents granulocyte-macrophage colony-stimulating factor-induced nuclear factor-kappaB activation, inducible nitric oxide synthase expression and nitric oxide production in a skin dendritic cell line: A.L. Vital, et al.; Mediators Inflamm. 12, 71 (2003) Abstract
Dexamethasone suppresses eNOS and CAT-1 and induces oxidative stress in mouse resistance arterioles: S.C. Schafer, et al.; Am. J. Physiol. Heart Circ. Physiol. 288, H436 (2005) Abstract; Full Text
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Further Categories Containing This Product:
NOS Inhibitors (NOS Induction & Enzyme Activity) • GITR & GITRL Other Products • RANK & RANKL/OPG Other Products • Antitumor Agents (Hormone-related) • Chemopreventive Agents Other Products • DNA & RNA Methyl & Alkyl Transferases/Related Products • Cell Cycle Other Products
 
 
ALX-270-283 Revised 06-May-08
DL-α-Difluoromethylornithine . hydrochloride . monohydrate
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SYNONYMS DFMO . HCl . H2O
Eflornithine . HCl . H2O
RMI-71782
PRODUCT LINE Cancer
PRODUCT CATEGORY Antitumor Agents (Apoptosis Inducers)
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ALX-270-283-M010   10 mg 25.00 USD Add To Cart
ALX-270-283-M050   50 mg 95.00 USD Add To Cart
Product Specification
FORMULA: C6H12F2N2O2 . HCl . H2O
MW: 182.2 . 36.5 . 18.0
CAS NUMBER: 96020-91-6
MERCK INDEX: 14: 3522
PURITY: ≥98% (TLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in water or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Hygroscopic.
HAZARD: HARMFUL.

Product Description
Specific, irreversible inhibitor of ornithine decarboxylase (ODC), the rate-limiting enzyme in polyamine biosynthesis. Potent chemopreventive agent. Induces apoptosis. Arginase activity inhibitor.
Product Specific Literature References
Effect of alpha-difluoromethylornithine, an enzyme-activated irreversible inhibitor of ornithine decarboxylase, on L1210 leukemia in mice: N.J. Prakash, et al.; Cancer Res. 38, 3059 (1978) Abstract
Inhibition of cell proliferation by DL-alpha-difluoromethylornithine, a catalytic irreversible inhibitor of ornithine decarboxylase: S. Oredsson, et al.; Acta Chem. Scand. B 34, 457 (1980) Abstract
Kinetics of alpha-difluoromethylornithine: an irreversible inhibitor of ornithine decarboxylase: K.D. Haegele, et al.; Clin. Pharmacol. Ther. 30, 210 (1981) Abstract
The competitive inhibition of tissue transglutaminase by alpha-difluoromethylornithine: J.G. Delcros, et al.; FEBS Lett. 171, 221 (1984) Abstract
The effect of alpha-difluoromethylornithine, an inhibitor of polyamine biosynthesis, on mitogen-induced interleukin 2 production: T.L. Bowlin, et al.; Immunopharmacology 13, 143 (1987) Abstract
The enzyme-activated irreversible inhibitor of ornithine decarboxylase, DL-alpha-difluoromethylornithine: a chemopreventive agent: A.K. Verma; Prev. Med. 18, 646 (1989) Abstract
Inhibition of tumor promotion by DL-alpha-difluoromethylornithine, a specific irreversible inhibitor of ornithine decarboxylase: A.K. Verma; Basic Life Sci. 52, 195 (1990), (Review) Abstract
The polyamine synthesis inhibitor alpha-difluoromethylornithine blocks NMDA-induced neurotoxicity: M.A. Markwell, et al.; Eur. J. Pharmacol. 182, 607 (1990) Abstract
Difluoromethylornithine (DFMO), an inhibitor of nitrite production by macrophages?: D.M. Morgan; Biochem. Soc. Trans. 22, 389S (1994) Abstract
Alpha-difluoromethylornithine (DFMO) as a potent arginase activity inhibitor in human colon carcinoma cells: M. Selamnia, et al.; Biochem. Pharmacol. 55, 1241 (1998) Abstract
Development of difluoromethylornithine (DFMO) as a chemoprevention agent: F.L. Meyskens, Jr. & E.W. Gerner; Clin. Cancer Res. 5, 945 (1999), (Review) Abstract; Full Text
alpha-difluoromethylornithine induces apoptosis as well as anti-angiogenesis in the inhibition of tumor growth and metastasis in a human gastric cancer model: Y. Takahashi, et al.; Int. J. Cancer 85, 243 (2000) Abstract
Further Categories Containing This Product:
Arginine & Arginases/Related Products • Angiogenesis Modulators Other Products • Chemopreventive Agents Other Products • Antitumor Agents (Enzyme Inhibitors)
 
 
ALX-350-370 Revised 22-Apr-08
3,3’-Diindolylmethane
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SYNONYMS DIM
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antitumor Reagents
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ALX-350-370-M100   100 mg 20.00 USD Add To Cart
ALX-350-370-M500   500 mg 50.00 USD Add To Cart
Product Specification
FORMULA: C17H14N2
MW: 246.3
CAS NUMBER: 1968-05-4
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO (200mg/ml); insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Dimer of indole-3-carbinol (Prod. No. ALX-350-347). Anticancer and antineoplastic agent. Induces apoptosis in human cancer cells. Activator of cytochrome P450. Partial agonist of aryl hydrocarbon receptor (AhR).
Product Specific Literature References
Oligomerization of indole-3-carbinol in aqueous acid: K.R. Grose & L.F. Bjeldanes; Chem. Res. Toxicol. 5, 188 (1992) Abstract
The anticarcinogen 3,3'-diindolylmethane is an inhibitor of cytochrome P-450: D.M. Stresser, et al.; J. Biochem. Toxicol. 10, 191 (1995) Abstract
3,3’-Diindolylmethane induces apoptosis in human cancer cells: X. Ge, et al.; BBRC 228, 153 (1996) Abstract
Indole-3-carbinol and diindolylmethane as aryl hydrocarbon (Ah) receptor agonists and antagonists in T47D human breast cancer cells: I. Chen, et al.; Biochem. Pharmacol. 51, 1069 (1996) Abstract
3,3’-Diindolylmethane induces CYP1A2 in cultured precision-cut human liver slices: B.G. Lake, et al.; Xenobiotica 28, 803 (1998) Abstract
Agonist and chemopreventative ligands induce differential transcriptional cofactor recruitment by aryl hydrocarbon receptor: E.V. Hestermann & M. Brown; Mol. Cell. Biol. 23, 7920 (2003) Abstract; Full Text
Interplay of genes regulated by estrogen and diindolylmethane in breast cancer cell lines: L. Mulvey, et al.; Mol. Med. 13, 69 (2007) Abstract; Full Text
3,3’-Diindolylmethane stimulates murine immune function in vitro and in vivo: L. Xue, et al.; J. Nutr. Biochem. 19, 336 (2008) Abstract
3,3’-diindolylmethane reduces levels of HIF-1alpha and HIF-1 activity in hypoxic cultured human cancer cells: J.E. Riby, et al.; Biochem. Pharmacol. 75, 1858 (2008) Abstract
Indole-3-carbinol as a chemopreventive and anti-cancer agent: J.R. Weng, et al.; Cancer Lett. 262, 153 (2008) Abstract
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Further Categories Containing This Product:
Antitumor Agents (Apoptosis Inducers) • Chemopreventive Agents Other Products • Cytochrome P450 [CYP450]/Related Products
 
 
ALX-385-031 Revised 06-Mar-08 New product
Diosmin
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SYNONYMS 3’,5,7-Trihydroxy-4’-methoxyflavone 7-rutinoside
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Flavonoids/Related Products
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ALX-385-031-G005   5 g 30.00 USD Add To Cart
ALX-385-031-G025   25 g 90.00 USD Add To Cart
Product Specification
FORMULA: C28H32O15
MW: 608.5
CAS NUMBER: 520-27-4
MERCK INDEX: 14: 3297
SOURCE/HOST: Isolated from Citrus aurantium L. and Citrus reticulate Blanca.
PURITY: ≥90% (HPLC)
APPEARANCE: Light yellow to brown yellow powder.
SOLUBILITY: Soluble in DMSO (50mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
IDENTITY: Determined by IR.

Product Description

Flavonoid glycoside. Main component in citrus fruits. Phlebotropic drug used to control internal symptoms of hemorrhoids and in the treatment of venous diseases. Prolongs the vasoconstrictor effect of noradrenaline on the vein wall. Reduces venous hyperpressure. Reduces capillary hyperpermeability and the expression of endothelial adhesion molecules (ICAM1, VCAM1). Effectively inhibits the P-glycoprotein (Pgp)-mediated efflux in cells. Anti-inflammatory. Inhibits lipopolysaccharide (LPS)-induced endothelial cytotoxicity.
Product Specific Literature References
Clinical trial of oral diosmin (Daflon) in the treatment of hemorrhoids: W. Thanapongsathorn & T. Vajrabukka; Dis. Colon Rectum 35, 1085 (1992) Abstract
Amine uptake inhibition by diosmin and diosmetin in human neuronal and neuroendocrine cell lines: E. Sher, et al.; Pharmacol. Res. 26, 395 (1992) Abstract
Antioxidant activity of micronized diosmin on oxygen species from stimulated human neutrophils: B. Cypriani, et al.; Biochem. Pharmacol. 45, 1531 (1993) Abstract
Diosmin-induced increase in sensitivity to Ca2+ of the smooth muscle contractile apparatus in the rat isolated femoral vein: J.P. Savineau & R. Marthan; Br. J. Pharmacol. 111, 978 (1994) Abstract; Full Text
Venous elasticity after treatment with Daflon 500 mg: V. Ibegbuna, et al.; Angiology 48, 45 (1997) Abstract
Chemopreventive effects of diosmin and hesperidin on N-butyl-N-(4-hydroxybutyl)nitrosamine-induced urinary-bladder carcinogenesis in male ICR mice: M. Yang, et al.; Int. J. Cancer 73, 719 (1997) Abstract
Diosmin and diosmetin are agonists of the aryl hydrocarbon receptor that differentially affect cytochrome P450 1A1 activity: H.P. Ciolino, et al.; Cancer Res. 58, 2754 (1998) Abstract; Full Text
Modulation by phytochemicals of cytochrome P450-linked enzyme activity: R.W. Teel & H. Huynh; Cancer Lett. 133, 135 (1998) Abstract
Inhibition of lipopolysaccharide (LPS)-induced endothelial cytotoxicity by diosmin: M.F. Melzig & R. Loose; Pharmazie 54, 298 (1999) Abstract
Anti-inflammatory activity of diosmin and hesperidin in rat colitis induced by TNBS: M.E. Crespo, et al.; Planta Med. 65, 651 (1999) Abstract
Further investigation of the modifying effect of various chemopreventive agents on apoptosis and cell proliferation in human colon cancer cells: Q. Zheng, et al.; J. Cancer Res. Clin. Oncol. 128, 539 (2002) Abst