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Nuclear Receptors / Related Products
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ALX-270-309 Revised 23-Apr-08
T0901317
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SYNONYMS N-(2,2,2-Trifluoroethyl)-N-[4-[2,2,2-trifluoro-1-hydroxy-1(trifluoromethyl)ethyl]phenyl]-benzenesulfonamide
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY Liver X Receptor / Related Products
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-309-M010   10 mg 30.00 USD Add To Cart
ALX-270-309-M050   50 mg 120.00 USD Add To Cart
Product Specification
FORMULA: C17H12NF9O3S
MW: 481.3
CAS NUMBER: 293754-55-9
PURITY: ≥98% (TLC)
APPEARANCE: White to off-white crystalline solid.
SOLUBILITY: 50mg/ml soluble in 100% ethanol, DMSO, dimethyl formamide or any organic solvent; also soluble in a 1:1 solution of DMSO:PBS, pH 7.2 (500µg/ml).
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: We do not recommend storing the aqueous solutions for more than one day.
HAZARD: HARMFUL.
IDENTITY: Identity determined by NMR.

Product Description
Potent agonist (EC50=50nM) of the orphan nuclear hormone receptor (liver X receptor; LXR). Inhibitor of human sex hormone-dependent cancer cell lines.
Product Specific Literature References
Regulation of absorption and ABC1-mediated efflux of cholesterol by RXR heterodimers: J.J. Repa, et al.; Science 289, 1524 (2000) Abstract
Role of LXRs in control of lipogenesis: J.R. Schultz, et al.; Genes Dev. 14, 2831 (2000) Abstract; Full Text
Expression of sterol regulatory element-binding protein 1c (SREBP-1c) mRNA in rat hepatoma cells requires endogenous LXR ligands: R.A. DeBose-Boyd, et al.; PNAS 98, 1477 (2001) Abstract; Full Text
LXRs control lipid-inducible expression of the apolipoprotein E gene in macrophages and adipocytes: B.A. Laffitte, et al.; PNAS 98, 507 (2001) Abstract; Full Text
Antiproliferative effect of liver X receptor agonists on LNCaP human prostate cancer cells: J. Fukuchi, et al.; Cancer Res. 64, 7686 (2004) Abstract
The liver X receptor agonist T0901317 acts as androgen receptor antagonist in human prostate cancer cells: C.P. Chuu et al.; Biochem. Biophys. Res. Commun. 357, 341 (2007) Abstract
Further Categories Containing This Product:
Antitumor Agents (Hormone-related)
 
 
ALX-550-095 Revised 02-May-06
Tamoxifen . citrate
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SYNONYMS (Z)-2-[4-(1,2-Diphenyl-1-butenyl)phenoxy]-N,N-dimethyl-ethanamine . citrate
PRODUCT LINE Cancer
PRODUCT CATEGORY Antitumor Agents (Hormone-related)
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-550-095-G001   1 g 85.00 USD Add To Cart
Product Specification
FORMULA: C26H29NO . C6H8O7
MW: 371.5 . 192.1
CAS NUMBER: 54965-24-1
MERCK INDEX: 14: 9048
RTECS: KH2387000
PURITY: ≥99%
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in methanol; very slightly soluble in water or acetone.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HAZARD: TOXIC. MAY BE TERATOGENIC. MAY BE CARCINOGENIC.

Product Description
Antiestrogen. Selective protein kinase C (PKC) inhibitor. Induces apoptosis.
Product Specific Literature References
Inhibition of protein kinase C by tamoxifen: C.A. O'Brian, et al.; Cancer Res. 45, 2462 (1985) Abstract
Opposite effects of tamoxifen on in vitro protein kinase C activity and endogenous protein phosphorylation in intact MCF-7 cells: M. Issandou, et al.; Cancer Res. 50, 5845 (1990) Abstract
Signalling targets for anticancer drug development: G. Powis; TIPS 12, 188 (1991), (Review) Abstract
Protein kinase C inhibitors induce apoptosis in human malignant glioma cell lines: W.T. Couldwell, et al.; FEBS Lett. 345, 43 (1994) Abstract
Tamoxifen: teaching an old drug new tricks?: D.J. Grainge & J.C. Metcalfe; Nat. Med. 2, 381 (1996), (Review) Abstract
Genomic effects of tamoxifen: J.A. Kellen; Anticancer Res. 16, 3537 (1996) Abstract
Steroidal and nonsteroidal oestrogen antagonists in breast cancer: basic and clinical appraisal: R.E. Favoni & A. de Cupis; TIPS 19, 406 (1998), (Review) Abstract
Recent advances in understanding the molecular mechanisms of tamoxifen action: Z.Y. Friedman; Cancer Invest. 16, 391 (1998) Abstract
Activation of nitric oxide synthase is involved in tamoxifen-induced apoptosis of human erythroleukemia K562 cells: M. Maccarrone, et al.; FEBS Lett. 434, 421 (1998) Abstract
Tamoxifen in the treatment of metastatic malignant melanoma: still a controversy? (Review): S. Toma, et al.; Int. J. Oncol. 15, 321 (1999) Abstract
Effective tamoxifen therapy of breast cancer involves both antiproliferative and pro-apoptotic changes: D.A. Cameron, et al.; Eur. J. Cancer. 36, 845 (2000) Abstract
Activation of caspase-3 and c-Jun NH2-terminal kinase-1 signaling pathways in tamoxifen-induced apoptosis of human breast cancer cells: S. Mandlekar, et al.; Cancer Res. 60, 5995 (2000) Abstract; Full Text
Pharmacodynamics of tamoxifen and its 4-hydroxy and N-desmethyl metabolites: activation of caspases and induction of apoptosis in rat mammary tumors and in human breast cancer cell lines: S. Mandlekar, et al.; Cancer Res. 60, 6601 (2000) Abstract; Full Text
Update on clinical role of tamoxifen: J.R. Benson and V. Pitsinis; Curr. Opin. Obstet. Gynecol. 15, 13 (2003) Abstract
Tamoxifen for prevention of breast cancer: R.J. Cersosimo; Ann. Pharmacother. 37, 268 (2003) Abstract
Tamoxifen: a most unlikely pioneering medicine: V.C. Jordan; Nat. Rev. Drug Discov. 2, 205 (2003) Abstract
Is tamoxifen the Rosetta stone for breast cancer?: V.C. Jordan; J. Natl. Cancer Inst. 95, 338 (2003) Abstract
Further Categories Containing This Product:
Estrogen & Estrogen Receptors / Related Products • PKC Inhibitors • MDR Inhibitors • Apoptosis Inducers & Inhibitors Other Products • Autophagy Other Products
 
 
ALX-550-361 Revised 18-Dec-07
(Z)-4-Hydroxytamoxifen
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SYNONYMS (Z)-4-[1-(p-(Dimethylaminoethoxy)phenyl)-2-phenyl-1-butenyl]phenol
PRODUCT LINE Cancer
PRODUCT CATEGORY Antitumor Agents (Hormone-related)
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-550-361-M001   1 mg 40.00 USD Add To Cart
ALX-550-361-M005   5 mg 145.00 USD Add To Cart
Product Specification
FORMULA: C26H29NO2
MW: 387.5
CAS NUMBER: 68047-06-3, 65213-48-1
PURITY: ≥98% (Z-isomer)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in 100% ethanol (20mg/ml) or methanol (10mg/ml); insoluble water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.
HAZARD: MAY BE CARCINOGENIC. TOXIC.

Product Description
Metabolite of tamoxifen (Prod. No. ALX-550-095). Exhibits a more potent estrogen agonist/antagonist activity than the parent drug. Has antioxidant properties. Intramembranous inhibitor of lipid peroxidation.
Product Specific Literature References
The antioxidant action of tamoxifen and its metabolites. Inhibition of lipid peroxidation: H. Wiseman, et al.; FEBS Lett. 263, 192 (1990) Abstract
Mechanism of inhibition of lipid peroxidation by tamoxifen and 4-hydroxytamoxifen introduced into liposomes. Similarity to cholesterol and ergosterol: H. Wiseman, et al.; FEBS Lett. 274, 107 (1990) Abstract
Protective actions of tamoxifen and 4-hydroxytamoxifen against oxidative damage to human low-density lipoproteins: a mechanism accounting for the cardioprotective action of tamoxifen?: H. Wiseman, et al.; Biochem. J. 292, 635 (1993) Abstract
Tamoxifen and hydroxytamoxifen as intramembraneous inhibitors of lipid peroxidation. Evidence for peroxyl radical scavenging activity: J.B. Custódio, et al.; Biochem. Pharmacol. 47, 1989 (1994) Abstract
Peroxidase-catalyzed pro- versus antioxidant effects of 4-hydroxytamoxifen: enzyme specificity and biochemical sequelae: B.W. Day, et al.; Chem. Res. Toxicol. 12, 28 (1999) Abstract
Estrogen and tamoxifen metabolites protect smooth muscle cell membrane phospholipids against peroxidation and inhibit cell growth: R.K. Dubey, et al.; Circ. Res. 84, 229 (1999) Abstract
Further Categories Containing This Product:
Estrogen & Estrogen Receptors / Related Products • Antioxidants, Flavonoids & Free Radical Scavengers Other Products • Lipid Peroxidation
 
 
ALX-270-355 Revised 14-Sep-07
Troglitazone
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SYNONYMS 5-[[4-[(3,4-Dihydro-6-hydroxy-2,5,7,8-tetramethyl-2H-1-benzopyran-2-yl)methoxy]phenyl]methyl]-2,4-thiazolidinedione
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY PPAR Agonists
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ALX-270-355-M001   1 mg 20.00 USD Add To Cart
ALX-270-355-M005   5 mg 30.00 USD Add To Cart
Product Specification
FORMULA: C24H27NO5S
MW: 441.5
CAS NUMBER: 97322-87-7
MERCK INDEX: 14: 9769
RTECS: XJ5813130
SOURCE/HOST: Synthetic.
PURITY: ≥98% (HPLC)
APPEARANCE: White to beige solid.
SOLUBILITY: Soluble in DMSO or dimethyl formamide; slightly soluble in 100% ethanol.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C

Product Description
Potent and selective PPARγ ligand. Binds to the PPARγ ligand-binding domain and recruits ligand-specific transcriptional coactivators at 1µM [1]. In skeletal muscle and adipocyte cell cultures, the EC50 of troglitazone is about 10µM [2].
Product Specific Literature References
[1] Ligand type-specific interactions of peroxisome proliferator-activated receptor gamma with transcriptional coactivators: Y. Kodera, et al.; J. Biol. Chem. 275, 33201 (2000) Abstract; Full Text
[2] Enhancing effect of troglitazone on porcine adipocyte differentiation in primary culture: a comparison with dexamethasone: Y.D. Tchoukalova, et al.; Obes. Res. 8, 664 (2000) Abstract
[3] 15-Deoxy-{delta}12,14-prostaglandin j2 inhibits interleukin-1{beta}-induced nuclear factor-{kappa}b in human amnion and myometrial cells: mechanisms and implications: T.M. Lindström & P.R. Bennett; J. Clin. Endocrinol. Metab. 90, 3534 (2005) Abstract; Full Text
General Information
BACKGROUND/TECHNICAL INFORMATION Troglitazone is sparingly soluble in aqueous buffers. For maximum solubility in aqueous buffers, troglitazone should first be dissolved in DMSO and then diluted with the aqueous buffer of choice. Troglitazone has a solubility of 100µg/ml in a 1:6 solution of DMSO:PBS (pH 7.2) using this method. We do not recommend storing the aqueous solution for more than one day.
General Literature References
[[omega-(Heterocyclylamino)alkoxy]benzyl]-2,4-thiazolidinediones as potent antihyperglycemic agents: B.C. Cantello, et al.; J. Med. Chem. 37, 3977 (1994) Abstract
An antidiabetic thiazolidinedione is a high affinity ligand for peroxisome proliferator-activated receptor gamma (PPAR gamma): J.M. Lehmann, et al.; J. Biol. Chem. 270, 12953 (1995) Abstract; Full Text
The structure-activity relationship between peroxisome proliferator-activated receptor gamma agonism and the antihyperglycemic activity of thiazolidinediones: T.M. Willson, et al.; J. Med. Chem. 39, 665 (1996) Abstract
Further Categories Containing This Product:
Antidiabetic Agents / Related Products • Apoptosis Inducers & Inhibitors Other Products
 
 
ALX-460-025 Revised 25-Mar-08
Vitamin D2
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SYNONYMS Calciferol
Ergocalciferol
PRODUCT LINE Bone Metabolism
PRODUCT CATEGORY Vitamin D3 & Vitamin D3 Receptor / Related Products
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-460-025-G001   1 g 33.00 USD Add To Cart
ALX-460-025-G005   5 g 135.00 USD Add To Cart
Product Specification
FORMULA: C28H44O
MW: 396.7
CAS NUMBER: 50-14-6
MERCK INDEX: 14: 10018
SOURCE/HOST: Synthetic.
PURITY: ≥98% (HPLC)
APPEARANCE: Yellow powder.
SOLUBILITY: Soluble in 100% ethanol or acetone; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Oxidized and inactivated by moisture within a few days.
HANDLING: Protect from light and moisture. Keep under inert gas.

Further Categories Containing This Product:
Vitamins
 
 
ALX-460-026 Revised 25-Mar-08
Vitamin D3
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SYNONYMS Cholecalciferol
Colecalciferol
PRODUCT LINE Bone Metabolism
PRODUCT CATEGORY Vitamin D3 & Vitamin D3 Receptor / Related Products
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ALX-460-026-G001   1 g 23.00 USD Add To Cart
ALX-460-026-G005   5 g 75.00 USD Add To Cart
Product Specification
FORMULA: C27H44O
MW: 384.7
CAS NUMBER: 67-97-0
MERCK INDEX: 14: 10019
SOURCE/HOST: Synthetic.
PURITY: ≥98%
APPEARANCE: White crystalline powder.
SOLUBILITY: Soluble in 100% ethanol or acetone; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Oxidized and inactivated by moisture within a few days.
HANDLING: Keep under inert gas. Protect from light and moisture.

Further Categories Containing This Product:
Vitamins
 
 
ALX-270-198 Revised 20-Jul-07
WY-14,643
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SYNONYMS Pirinixic acid
(4-Chloro-6-[(2,3-dimethylphenyl)amino]-2-pyrimidinyl)thioacetic acid
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY PPAR Agonists
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ALX-270-198-M010   10 mg 20.00 USD Add To Cart
ALX-270-198-M050   50 mg 70.00 USD Add To Cart
Product Specification
FORMULA: C14H14ClN3O2S
MW: 323.8
CAS NUMBER: 50892-23-4
RTECS: AG2915000
PURITY: ≥98%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in 100% ethanol, DMSO or dimethyl formamide; also soluble in PBS, pH 7.2.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
USE/STABILITY: Stock solutions in organic solvents will be stable for at least 6 months at +20°C. We do not recommend storing the aqueous solution for more than one day.
HAZARD: MAY BE CARCINOGENIC. TOXIC.

Product Description
Widely used activator of peroxisome proliferator activator receptors (PPARs). PPARs belong to the family of nuclear hormone receptor transcription factors.
Product Specific Literature References
Control of the peroxisomal beta-oxidation pathway by a novel family of nuclear hormone receptors: C. Dreyer, et al.; Cell 68, 879 (1992) Abstract
 
 
ALX-350-280 Revised 07-Oct-08
Xanthohumol
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Other Natural Products - DNA Regulation / Transcription
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-280-M005   5 mg 135.00 USD Add To Cart
Product Specification
FORMULA: C21H22O5
MW: 354.4
CAS NUMBER: 569-83-5, 6754-58-1
SOURCE/HOST: Isolated from hops (Humulus lupulus).
PURITY: ≥98% (HPLC)
APPEARANCE: Yellow to orange powder.
SOLUBILITY: Soluble in DMSO (25mg/ml), methanol (10mg/ml) or 100% ethanol; soluble in aqueous buffers up to 20μM.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Stable as powder for at least 6 months when stored at +4°C in the dark. Stock solution made in DMSO should not be stored for longer than one month. Working solution is stable for 24 hours at 37°C and up to one week when stored at +4°C. Unstable in acidic (pH < 4.5) and alkaline (pH > 7.5) systems.
IDENTITY: Identity determined by NMR.

Product Description
Prenylated chalcone found in beer. Potent inhibitor of diacylglycerol acetyltransferase (DGAT). Inhibits DNA polymerase and induces cell differentiation. Has antiproliferative and cytotoxic effects in human cancer cell lines. Inhibits human P450 enzymes. Induces quinone reductase. Inhibits the expression of HIF-1α and VEGF under hypoxic conditions. Induces apoptosis in mature adipocytes.
Product Specific Literature References
Xanthohumols, diacylglycerol acyltransferase inhibitors, from Humulus lupulus: N. Tabata, et al.; Phytochemistry 46, 683 (1997) Abstract
Antiproliferative and cytotoxic effects of prenylated flavonoids from hops (Humulus lupulus) in human cancer cell lines: C.L. Miranda, et al.; Food Chem. Toxicol. 37, 271 (1999) Abstract
In vitro inhibition of human P450 enzymes by prenylated flavonoids from hops, Humulus lupulus: M.C. Henderson, et al.; Xenobiotica 30, 235 (2000) Abstract
Prenylated chalcones and flavanones as inducers of quinone reductase in mouse Hepa 1c1c7 cells: C.L. Miranda, et al.; Cancer Lett. 149, 21 (2000) Abstract
Cancer chemopreventive activity of Xanthohumol, a natural product derived from hop: C. Gerhauser, et al.; Mol. Cancer Ther. 1, 959 (2002) Abstract
Xanthohumol and related prenylflavonoids from hops and beer: to your good health!: J.F. Stevens & J.E. Page; Phytochemistry 65, 1317 (2004), (Review) Abstract
Effect of xanthohumol and isoxanthohumol on 3T3-L1 cell apoptosis and adipogenesis: J.Y. Yang, et al.; Apoptosis 12, 1953 (2007) Abstract
Further Categories Containing This Product:
Active Substances from Fruit and Vegetables • Antitumor Agents (Anti-proliferative) • Cell Differentiation • Estrogen & Estrogen Receptors / Related Products • Respiratory Chain Other Products • Chalcones • Hypoxia-inducible Factor [HIF] / Related Products • Obesity & Diabetes Other Products • Natural Products - Apoptosis Inducers & Inhibitors • Natural Products - Antitumor Reagents • Lipid Metabolism Other Products • VEGFs
 
 
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