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DNA Regulation / Transcription
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ALX-270-303 Revised 13-Apr-06
Sodium 4-phenylbutyrate
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SYNONYMS SPB
4-Phenylbutyric acid
4PBA
PBNa
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY HDAC Inhibitors
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ALX-270-303-M100   100 mg 35.00 USD Add To Cart
Product Specification
FORMULA: C10H11O2Na
MW: 186.2
CAS NUMBER: 1716-12-7
PURITY: ≥98%
APPEARANCE: White to yellowish solid.
SOLUBILITY: Soluble in DMSO or water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Hygroscopic.
Product Description
Inhibitor of histone deacetylase (HDAC). Anti-neoplastic agent and transcriptional regulator. Also acts as an inducer of tumor cytostasis and differentiation. Shows chemical chaperone activity.
Product Specific Literature References
Discordant effects of butyrate analogues on erythroleukemia cell proliferation, differentiation and histone deacetylase: M.A. Lea & N. Tulsyan; Anticancer Res. 15, 879 (1995) Abstract
Therapeutic targeting of transcription in acute promyelocytic leukemia by use of an inhibitor of histone deacetylase: R.P. Warrell, Jr., et al.; J. Natl. Cancer Inst. 90, 1621 (1998) Abstract
Modifying histones to tame cancer: clinical development of sodium phenylbutyrate and other histone deacetylase inhibitors: S.D. Gore & M.A. Carducci; Expert Opin. Investig. Drugs 9, 2923 (2000), (Review) Abstract
Butyrate as a model for "gene-regulating chemoprevention and chemotherapy.": Y. Sowa & T. Sakai; Biofactors 12, 283 (2000) Abstract
Further Categories Containing This Product:
Antitumor Agents (Anti-proliferative)
 
 
ALX-270-308 Revised 10-Apr-08
Sirtinol
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SYNONYMS Sir Two Inhibitor Naphthol
2-[(2-Hydroxynaphthalen-1-yl-methylene)amino]-N-(1-phenethyl)benzamide
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY Sirtuins / Related Products
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ALX-270-308-M001   1 mg 53.00 USD Add To Cart
ALX-270-308-M005   5 mg 160.00 USD Add To Cart
Product Specification
FORMULA: C26H22N2O2
MW: 394.5
PURITY: ≥97% (HPLC)
APPEARANCE: Off-white to yellow crystals.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Relatively unstable in aqueous solution, especially at acidic pH.
HANDLING: Protect from light.

Product Description
Specific cell permeable inhibitor of the sirtuin family of NAD-dependent deacetylases (ySir2: IC50=48µM; hSIRT1: IC50=131µM; hSIRT2: IC50=58µM) with no effect on human HDAC1. Reported to inhibit Sir2p transcriptional silencing activity in vivo (IC50=25µM) and NAD-dependent histone deacetylase activity of purified recombinant yeast Sir2p (IC50=70µM) and hSIRT2 (IC50=40µM) in vitro.
Product Specific Literature References
Identification of a class of small molecule inhibitors of the sirtuin family of NAD-dependent deacetylases by phenotypic screening: C.M. Grozinger, et al.; J. Biol. Chem. 276, 38837 (2001) Abstract; Full Text
Human telomeric position effect is determined by chromosomal context and telomeric chromatin integrity: C.E. Koering, et al.; EMBO Rep. 3, 1055 (2002) Abstract; Full Text
Design, synthesis, and biological evaluation of sirtinol analogues as class III histone/protein deacetylase (Sirtuin) inhibitors: A. Mai, et al.; J. Med. Chem. 48, 7789 (2005) Abstract
Sirt1 inhibitor, Sirtinol, induces senescence-like growth arrest with attenuated Ras-MAPK signaling in human cancer cells: H. Ota, et al.; Oncogene 25, 176 (2006) Abstract
Further Categories Containing This Product:
NAD+ Metabolism / Related Products
 
 
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-270-312 Revised 03-Jan-08
Formononetin (high purity)
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SYNONYMS 7-Hydroxy-4’-methoxyisoflavone (high purity)
7-Hydroxy-3-(4’-methoxyphenyl)-4H-benzopyran-4-one (high purity)
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Isoflavones
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ALX-270-312-M005   5 mg 140.00 USD Add To Cart
Product Specification
FORMULA: C16H12O4
MW: 268.3
CAS NUMBER: 485-72-3
MERCK INDEX: 14: 4244
PURITY: ≥97%
APPEARANCE: White to greyish powder.
SOLUBILITY: Soluble in DMSO (200mg/ml) or methanol (2mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Place in a desiccator under vacuum for 48 hours before use.
HANDLING: Protect from light.

Product Description
Interacts with human estrogen receptors with low potency. Enhances IL-4 production in a dose-dependent manner. Inhibits lecithin peroxidation induced by hydroxyl radicals. Selective inhibitor of the γ-isoform of alcohol dehydrogenase. Antioxidant.
Product Specific Literature References
Interaction of naturally occurring nonsteroidal estrogens with expressed recombinant human estrogen receptor: R.J. Miksicek; J. Steroid Biochem. Mol. Biol. 49, 153 (1994) Abstract
Dietary estrogenic isoflavones are potent inhibitors of beta-hydroxysteroid dehydrogenase of P. testosteronii: W.M. Keung; BBRC 215, 1137 (1995) Abstract
Proliferative response of mammary glandular tissue to formononetin: W. Wang, et al.; Nutr. Cancer 23, 131 (1995) Abstract
Antioxidant activity of phytoestrogenic isoflavones: M.B. Ruiz-Larrea, et al.; Free Radic. Res. 26, 63 (1997) Abstract
Inhibitory effects of isoflavones on lipid peroxidation by reactive oxygen species: S. Toda and Y. Shirataki; Phytother. Res. 13, 163 (1999) Abstract
Isoflavonoids and lignans have different potentials to modulate oxidative genetic damage in human colon cells: B.L. Pool-Zobel, et al.; Carcinogenesis 21, 1247 (2000) Abstract
Disposition of flavonoids via enteric recycling: enzyme-transporter coupling affects metabolism of biochanin A and formononetin and excretion of their phase II conjugates: X. Jia, et al.; J. Pharmacol. Exp. Ther. 310, 1103 (2004) Abstract
Formononetin, a phyto-oestrogen, and its metabolites up-regulate interleukin-4 production in activated T cells via increased AP-1 DNA binding activity: J. Park, et al.; Immunology 116, 71 (2005) Abstract
Further Categories Containing This Product:
Estrogen & Estrogen Receptors / Related Products • Interleukins Other Products • Natural Products - Antioxidants • Active Substances from Fruit and Vegetables • Other Natural Products for Inflammation Research
 
 
ALX-270-344 Revised 05-Feb-05
MC 1293
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SYNONYMS 3-(4-Toluoyl-1-methyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamide
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY HDAC Inhibitors
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ALX-270-344-M005   5 mg 150.00 USD Add To Cart
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Product Specification
FORMULA: C16H16N2O3
MW: 284.3
APPEARANCE: Off-white powder.
SOLUBILITY: Soluble in DMSO.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Inhibitor of histone deacetylase 1 (HDAC1) (IC50 = 4.5µM) [2] and maize histone deacetylase HD2 (IC50=1.9µM) [1].
Product Specific Literature References
[1] 3-(4-aroyl-1H-pyrrol-2-yl)-N-hydroxy-2-propenamides, a new class of synthetic histone deacetylase inhibitors: S. Massa, et al.; J. Med. Chem. 44, 2069 (2001) Abstract
[2] Binding mode analysis of 3-(4-benzoyl-1-methyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamide: a new synthetic histone deacetylase inhibitor inducing histone hyperacetylation, growth inhibition, and terminal cell differentiation: A. Mai, et al.; J. Med. Chem. 45, 1778 (2002) Abstract
 
 
ALX-270-346 Revised 28-May-08
Ratjadone A (synthetic)
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics for Cell Cycle Research
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ALX-270-346-C002   2 µg 150.00 USD Add To Cart
Product Specification
FORMULA: C28H40O5
MW: 456.6
CAS NUMBER: 163564-92-9
SOURCE/HOST: Synthetic.
PURITY: ≥95%
FORMULATION: Liquid. Solution in methanol.
SOLUBILITY: Soluble in methanol (20mg/ml) or aqueous buffers (<100µM).
SHIPPING: SHIPPED ON DRY ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Sensitive to acids and bases. Unstable in acidic buffer systems (pH<6). Stable in substance as oil and in solution in methanol at -20°C.
HANDLING: Protect from light.
HAZARD: TOXIC.

Product Description
Represents a new class of natural compounds, which inhibit proliferation in eukaryotes by blocking nuclear export. As potent as leptomycin B (Prod. No. ALX-380-100) and specific for G1/S checkpoint. Cytotoxic secondary metabolite (IC50=50pg/ml in mouse cell line L929) that arrests tumor cells in the G1 phase at remarkably low concentrations (50pg/ml in HeLa cell line KB3.1). Inhibits the binding between the nuclear export signal (NES) of proteins and the chromosome maintenance region protein (CRM1). Anticancer compound. Belongs to the family of orphan ligands which include polyketides like leptomycin B, callystatin A and other related compounds.
Product Specific Literature References
Antibiotics from gliding bacteria, LXIII. Ratjadone: a new antifungal metabolite from Sorangium cellulosum: D. Schummer, et al.; Liebigs Ann. 685 (1995)
Ratjadon: a new antifungal compound from Sorangium cellulosum (myxobacteria) production, physio-chemical and biological properties: J. Gerth, et al.; J. Antibiot. 48, 973 (1995) Abstract
The chemistry and biology of ratjadone: M. Kalesse, et al.; ChemBioChem. 9, 709 (2001) Abstract
The chemistry and biology of the leptomycin family: M. Kalesse & M. Christmann; Synthesis 8, 981 (2002) Abstract
Ratjadone and leptomycin B block CRM1-dependent nuclear export by identical mechanisms: T. Meissner, et al.; FEBS Lett. 576, 27 (2004)
Nuclear targeting of adenovirus type 2 requires CRM1-mediated nuclear export: S. Strunze, et al.; Mol. Biol. Cell 16, 2999 (2005) Abstract
Further Categories Containing This Product:
Antitumor Antibiotics • Antibiotics - Antifungal • Cell Cycle Blockers & Inhibitors / Related Products • Nuclear Envelope & Nuclear Transport • Antitumor Agents (Anti-proliferative)
 
 
ALX-270-353 Revised 16-Feb-07
BADGE
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SYNONYMS Bisphenol A diglycidyl ether
2,2'-[(1-Methylethylidene)bis(4,1-phenyleneoxymethylene)]bis-oxirane
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY PPAR Antagonists
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ALX-270-353-G025   25 g 19.00 USD Add To Cart
Product Specification
FORMULA: C21H24O4
MW: 340.4
CAS NUMBER: 1675-54-3
PURITY: ≥85%
FORMULATION: Neat oil.
SOLUBILITY: Miscible in organic solvents as 100% ethanol, DMSO or dimethyl formamide. Insoluble in PBS, pH 7.2.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Stock solutions in 100% ethanol, DMSO or dimethyl formamide are stable for at least 1 year if stored at -20°C.

Product Description
Antagonist of PPARγ. Binds to PPARγ with an apparent Kd of 100µM.
Product Specific Literature References
A synthetic antagonist for the peroxisome proliferator-activated receptor gamma inhibits adipocyte differentiation: H.M. Wright, et al.; J. Biol. Chem. 275, 1873 (2000) Abstract; Full Text
Bisphenol A diglycidyl ether induces apoptosis in tumour cells independently of peroxisome proliferator-activated receptor-gamma, in caspase-dependent and -independent manners: S. Fehlberg, et al.; Biochem. J. 362, 573 (2002) Abstract; Full Text
Bisphenol a diglycidyl ether (BADGE) suppresses tumor necrosis factor-alpha production as a PPARgamma agonist in the murine macrophage-like cell line, RAW 264.7: M. Nakamuta, et al.; Cell Biol. Int. 26, 235 (2002) Abstract
Induction of apoptosis in human and rat glioma by agonists of the nuclear receptor PPARgamma: T. Zander, et al.; J. Neurochem. 81, 1052 (2002) Abstract
General Information
Interferes with the ability of 3T3-L1 and 3T3-F442A cells to undergo hormone-mediated cell differentiation.
 
 
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:
Apoptosis Inducers & Inhibitors Other Products • Antidiabetic Agents / Related Products
 
 
ALX-270-356 Revised 04-May-06
GW9662
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SYNONYMS 2-Chloro-5-nitrobenzanilide
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY PPAR Antagonists
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ALX-270-356-M001   1 mg 10.00 USD Add To Cart
ALX-270-356-M005   5 mg 35.00 USD Add To Cart
ALX-270-356-M025   25 mg 140.00 USD Add To Cart
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Product Specification
FORMULA: C13H9N2O3Cl
MW: 276.7
CAS NUMBER: 22978-25-2
PURITY: ≥98%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in 100% ethanol, DMSO or dimethyl formamide.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Blocks the PPARγ-induced differentiation of monocytes