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Nuclear Receptors / Related Products
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ALX-460-036 Revised 17-Jan-05
Alfacalcidol
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SYNONYMS Hydroxyvitamin D3
1-Hydroxycholecalciferol
(1α,3β,5Z,7E)-9,10-Secocholesta-5,7,10(19)-triene-1,3-diol
PRODUCT LINE Bone Metabolism
PRODUCT CATEGORY Vitamin D3 & Vitamin D3 Receptor / Related Products
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ALX-460-036-M001   1 mg 75.00 USD Add To Cart
Product Specification
FORMULA: C27H44O2
MW: 400.6
CAS NUMBER: 41294-56-8
RTECS: VS2851000
PURITY: ≥97%
APPEARANCE: White to off white crystals.
SOLUBILITY: Soluble in ethanol.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
HANDLING: Protect from light. Keep under inert gas.

Product Description
Converts to active calcitriol (1α,25-dihydroxyvitamin D3; Prod. No. ALX-460-032) in vivo. Inhibits bone resorption.
Further Categories Containing This Product:
Vitamins
 
 
ALX-270-474 Revised 22-Oct-07
HSD Inhibitor 23
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SYNONYMS N-(5-Hydroxytricyclo[3.3.1.13,7]dec-2-yl)-α,α-dimethyl-4-[5-(trifluoromethyl)-2-pyridinyl]-1-piperazineacetamide
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY Glucocorticoids & Glucocorticoid Receptors / Related Products
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ALX-270-474-M001   1 mg 190.00 USD Add To Cart
Product Specification
FORMULA: C24H33F3N4O2
MW: 466.5
CAS NUMBER: 868604-75-5
PURITY: ≥95%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
IDENTITY: Determined by 1H-NMR, 13C-NMR and MS.

Product Description
Selective, potent and cell permeable small molecule inhibitor of 11-β-hydroxysteroid dehydrogenase.
Product Specific Literature References
Discovery and metabolic stabilization of potent and selective 2-amino-N-(adamant-2-yl) acetamide 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: J.J. Rohde, et al.; J. Med. Chem. 50, 149 (2007) Abstract; Full Text
 
 
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
Related Products
Further Categories Containing This Product:
GITR & GITRL Other Products • RANK & RANKL / OPG Other Products • Antitumor Agents (Hormone-related) • NOS Inhibitors (NOS Induction & Enzyme Activity) • Chemopreventive Agents Other Products • DNA & RNA Methyl & Alkyl Transferases / Related Products • Cell Cycle Other Products
 
 
ALX-370-007 Revised 09-Sep-08
Corticosterone
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SYNONYMS (11β)-11,21-Dihydroxypregn-4-ene-3,20-dione
Reichstein's Substance H
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY Glucocorticoids & Glucocorticoid Receptors / Related Products
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ALX-370-007-M050   50 mg 18.00 USD Add To Cart
Product Specification
FORMULA: C21H30O4
MW: 346.5
CAS NUMBER: 50-22-6
MERCK INDEX: 14: 2538
RTECS: GM7650000
PURITY: ≥98% (HPLC)
APPEARANCE: White to light yellow solid.
SOLUBILITY: Soluble in 100% ethanol (50mg/ml) or dioxane (20mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
HAZARD: MAY BE TERATOGENIC. IRRITANT.

Further Categories Containing This Product:
Apoptosis Inducers & Inhibitors Other Products • Nitric Oxide Pathway Other 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
Related Products
Further Categories Containing This Product:
GITR & GITRL Other Products • Glucocorticoids & Glucocorticoid Receptors / Related Products • RANK & RANKL / OPG Other Products • Natural Products - Nitric Oxide Pathway Modulators • DNA & RNA Methyl & Alkyl Transferases / Related Products • Antitumor Agents (Hormone-related) • NOS Inhibitors (NOS Induction & Enzyme Activity) • Natural Products - Chemopreventive Agents • Other Natural Products - DNA Regulation / Transcription • Natural Products for Cell Cycle Research
 
 
ALX-270-476 Revised 11-Mar-08
Bicalutamide
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SYNONYMS N-(4-Cyano-3-(trifluoromethyl)phenyl)-3-((4-fluorophenyl)sulfonyl)-2-hydroxy-2-methylpropanamide
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY Androgens & Androgen Receptors / Related Products
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ALX-270-476-M100   100 mg 40.00 USD Add To Cart
ALX-270-476-M500   500 mg 140.00 USD Add To Cart
ALX-270-476-G001   1 g 220.00 USD Add To Cart
Product Specification
FORMULA: C18H14F4N2O4S
MW: 430.4
CAS NUMBER: 90357-06-5
SOURCE/HOST: Synthetic.
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in acetone and tetrahydrofuran; slightly soluble in 100% ethanol or methanol; practically insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Nonsteroidal antiandrogen. Effective in the treatment of prostate cancer. Induces cell death by a pathway that is independent of changes in mitochondrial membrane potential and Bcl-2 action.
Product Specific Literature References
Antiproliferative activity of casodex (ICI 176.334) in hormone-dependent tumours: A. Maucher & E. von Angerer; J. Cancer Res. Clin. Oncol. 119, 669 (1993) Abstract
Antiandrogen-induced cell death in LNCaP human prostate cancer cells: E.C. Lee, et al.; Cell Death Differ. 10, 761 (2003) Abstract
Proanthocyanidins from grape seeds inhibit expression of matrix metalloproteinases in human prostate carcinoma cells, which is associated with the inhibition of activation of MAPK and NF kappa B: P.K. Vayalil, et al.; Carcinogenesis 25, 987 (2004) Abstract; Full Text
Wnt3a growth factor induces androgen receptor-mediated transcription and enhances cell growth in human prostate cancer cells: M. Verras, et al.; Cancer Res. 64, 8860 (2004) Abstract; Full Text
Glycogen synthase kinase-3beta activity is required for androgen-stimulated gene expression in prostate cancer: X. Liao, et al.; Endocrinology 145, 2941 (2004) Abstract; Full Text
A phase I pharmacokinetic and pharmacodynamic study of OGX-011, a 2’-methoxyethyl antisense oligonucleotide to clusterin, in patients with localized prostate cancer: K.N. Chi, et al.; J. Natl. Cancer Inst. 97, 1287 (2005) Abstract; Full Text
The mechanisms and managements of hormone-therapy resistance in breast and prostate cancers: K.M. Rau, et al.; Endocr. Relat. Cancer 12, 511 (2005), Review Abstract; Full Text
Signal transduction pathways in androgen-dependent and -independent prostate cancer cell proliferation: P.M. Ghosh, et al.; Endocr. Relat. Cancer 12, 119 (2005) Abstract; Full Text
Recent advances on multiple tumorigenic cascades involved in prostatic cancer progression and targeting therapies: M. Mimeault & S.K. Batra; Carcinogenesis 27, 1 (2006), Review Abstract; Full Text
Bcl-xL is overexpressed in hormone-resistant prostate cancer and promotes survival of LNCaP cells via interaction with proapoptotic Bak: C. Castilla, et al.; Endocrinology 147, 4960 (2006) Abstract; Full Text
Androgen receptor corepressors and prostate cancer: C.J. Burd, et al.; Endocr. Relat. Cancer 13, 979 (2006), Review Abstract; Full Text
Par-4-dependent apoptosis by the dietary compound withaferin A in prostate cancer cells: S. Srinivasan, et al.; Cancer Res. 67, 246 (2006) Abstract; Full Text
Androgen receptor structural and functional elements: role and regulation in prostate cancer: S.M. Dehm & D.J. Tindall; Mol. Endocrinol. 21, 2855 (2007), Review Abstract
Phosphoinositide 3-kinase-independent non-genomic signals transit from the androgen receptor to Akt1 in membrane raft microdomains: B. Cinar, et al.; JBC 282, 29584 (2007) Abstract; Full Text
A novel class of pyranocoumarin anti-androgen receptor signaling compounds: J. Guo, et al.; Mol. Cancer Ther. 6, 907 (2007) Abstract; Full Text
Increased resistance to trail-induced apoptosis in prostate cancer cells selected in the presence of bicalutamide: M. Mitterberger, et al.; Prostate 67, 1194 (2007) Abstract
Interplay of nuclear factor-kappaB and B-myb in the negative regulation of androgen receptor expression by tumor necrosis factor alpha: S. Ko, et al.; Mol. Endocrinol. 22, 273 (2008) Abstract
Further Categories Containing This Product:
Antitumor Agents (Hormone-related) • Antitumor Agents (Apoptosis Inducers)
 
 
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
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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-748-003 Revised 04-Mar-05
PPARγ (human) cDNA Probe
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SYNONYMS Peroxisome Proliferator Activator Receptor-γ (human) cDNA Probe
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY PPAR cDNA
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ALX-748-003-C002   2 µg 284.00 USD Add To Cart
Product Specification
SOURCE/HOST: Derived from the cDNA library of normal human bone marrow. Has a length of ~1.2kb.
QUANTITY: 2µg of an isolated double-stranded cDNA (coding region)
PURITY: ≥98%
FORMULATION: Solution in 100µl buffer (10mM Tris-HCl, 0.1Mm Na2EDTA, pH 7.5).
APPLICATION: This probe will hybridize with the full length PPARγ sequence (1.85kbp) of most hematopoietic cell lines. The probe may be labelled by radioactive or non-radioactive compounds using random primer labeling or nick translation. For best results avoid repeated freezing and thawing of the probe solution.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
Product Description
Ends: 5' overhang.
Further Categories Containing This Product:
DNA & RNA Probes / Related Products
 
 
ALX-803-004 Revised 15-Apr-08
Monoclonal Antibody to Estrogen Receptor α (33)
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SYNONYMS anti-ERα (33)
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY Estrogen & Estrogen Receptors / Related Products
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ALX-803-004-C050   50 µg 379.00 USD Add To Cart
Product Specification
SPECIES CROSSREACTIVITY:
Human
Mouse
Rat
Others
CLONE: 33
ISOTYPE: Mouse IgG1
CONCENTRATION: 0.5mg/ml
FORMULATION: Liquid. Ascites diluted in PBS containing 0.1% sodium azide.
IMMUNOGEN: Synthetic peptide corresponding to aa 247-261 (E247VGMMKGGIRKDRRG261) of the DNA binding domain of ERα (estrogen receptor α). This sequence is completely conserved in many species including mouse, rat, pig, bovine, sheep, chicken and frog.
SPECIFICITY: Recognizes both the steroid occupied and unoccupied forms of human, mouse, rat, bovine and monkey ERα. Detects a band of ~67kDa by Western blot. Does not cross-react with androgen receptor, PR (progesterone receptor), GR (glucocorticoid receptor) or ERβ. Does not inhibit binding of ER to nuclei and DNA.
APPLICATION: Flow Cytometry
Gel Supershift Assays.
Immunocytochemistry (10µg/ml)
Immunohistochemistry (frozen sections; paraffin sections): 5µg/ml. Staining of ERα in mouse Leydig cells results in both nuclear and cytoplasmic staining.
Immunoprecipitation
Western Blot: 1µg/ml
Optimal conditions must be determined individually for each application.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
HANDLING: Avoid freeze/thaw cycles.
BLOCKING PEPTIDE: For Blocking Peptide see Prod. No. ALX-155-028.
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