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Transcription Regulators / Related Products
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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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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
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:
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-380-068 Revised 09-Apr-08
Trichostatin A
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SYNONYMS TSA
[R-(E,E)]-7-[4-(Dimethylamino)phenyl]-N-hydroxy-4,6-dimethyl-7-oxo-2,4-heptadienamide]
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Other Antibiotics - DNA Regulation / Transcription
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ALX-380-068-M001   1 mg 115.00 USD Add To Cart
ALX-380-068-M005   5 mg 385.00 USD Add To Cart
Product Specification
FORMULA: C17H22N2O3
MW: 302.4
CAS NUMBER: 58880-19-6
MERCK INDEX: 14: 9649
SOURCE/HOST: Isolated from Streptomyces hygroscopicus.
PURITY: ≥98% (HPLC)
APPEARANCE: Whitish film adhered to inside of vial.
SOLUBILITY: Soluble in DMSO, dimethyl formamide, acetonitrile, methanol or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: HARMFUL.

Product Description
Potent, reversible inhibitor of histone deacetylase (HDAC). Mediates the activation of O6-methylguanine-DNA methyltransferase (MGMT). May be involved in cell cycle progression of several cell types. Induces cell growth arrest at both G1 and G2/M phases. May induce apoptosis in some cases. Induces acetylation of histone-3/4 and expression of p300.
Product Specific Literature References
A new antifungal antibiotic, trichostatin: N. Tsuji, et al.; J. Antibiot. 29, 1 (1976) Abstract
Potent and specific inhibition of mammalian histone deacetylase both in vivo and in vitro by trichostatin A: M. Yoshida, et al.; J. Biol. Chem. 265, 17174 (1990) Abstract; Full Text
Trichostatin A induces morphological changes and gelsolin expression by inhibiting histone deacetylase in human carcinoma cell lines: Y. Hoshikawa, et al.; Exp. Cell Res. 214, 189 (1994) Abstract
Trichostatin A inhibits both ras-induced neurite outgrowth of PC12 cells and morphological transformation of NIH3T3 cells: M. Futamura, et al.; Oncogene 10, 1119 (1995) Abstract
Trichostatin A and trapoxin: novel chemical probes for the role of histone acetylation in chromatin structure and function: M. Yoshida, et al.; Bioessays 17, 423 (1995) Abstract
Selective inhibition of IL-2 gene expression by trichostatin A, a potent inhibitor of mammalian histone deacetylase: I. Takahashi, et al.; J. Antibiot. 49, 453 (1996) Abstract
A mammalian histone deacetylase related to the yeast transcriptional regulator Rpd3p: J. Taunton, et al.; Science 272, 408 (1996) Abstract
Transcriptional activation and chromatin remodeling of the HIV-1 promoter in response to histone acetylation: C. Van Lint, et al.; EMBO J. 15, 1112 (1996) Abstract
Induction of caspase-3 protease activity and apoptosis by butyrate and trichostatin A (inhibitors of histone deacetylase): dependence on protein synthesis and synergy with a mitochondrial/cytochrome c- dependent pathway:: V. Medina, et al.; Cancer Res. 57, 3697 (1997) Abstract
A histone deacetylase inhibitor potentiates retinoid receptor action in embryonal carcinoma cells: S. Minucci, et al.; PNAS 94, 11295 (1997) Abstract; Full Text
Histone deacetylase inhibitor activates the WAF1/Cip1 gene promoter through the Sp1 sites: Y. Sowa, et al.; BBRC 241, 142 (1997) Abstract
Retinoblastoma protein recruits histone deacetylase to repress transcription: A. Brehm, et al.; Nature 391, 597 (1998) Abstract
Effects of cell density and trichostatin A on the expression of HDAC1 and p57Kip2 in Hep 3B cells: S.G. Gray & T.J. Ekstrom; BBRC 245, 423 (1998) Abstract
Regulation of the human O6-methylguanine-DNA methyltransferase gene by transcriptional coactivators cAMP response element-binding protein- binding protein and p300: K.K. Bhakat & S. Mitra; J. Biol. Chem. 275, 34197 (2000) Abstract; Full Text
Histone deacetylase inhibitors: inducers of differentiation or apoptosis of transformed cells: P.A. Marks, et al.; J. Natl. Cancer Inst. 92, 1210 (2000) Abstract
Trichostatin A is a histone deacetylase inhibitor with potent antitumor activity against breast cancer in vivo: D.M. Vigushin, et al.; Clin. Cancer Res. 7, 971 (2001) Abstract
Chromatin remodeling agent trichostatin A: a key-factor in the hepatic differentiation of human mesenchymal stem cells derived of adult bone marrow: S. Snykers, et al.; BMC Dev. Biol. 7, 24 (2007) Abstract
Trichostatin A induces myocardial differentiation of monkey ES cells: M. Hosseinkhani, et al.; BBRC 356, 386 (2007) Abstract
Further Categories Containing This Product:
Cell Cycle Blockers & Inhibitors / Related Products • Antibiotics - Other Signal Transduction Pathway Modulators • Antibiotics - Apoptosis Inducers & Inhibitors • HDAC Inhibitors • PKC Activators • Antitumor Antibiotics • Antibiotics for Cell Cycle Research • DNA Repair Other Products • DNA & RNA Methyl & Alkyl Transferases / Related Products • Antibiotics - Antifungal
 
 
ALX-380-070 Revised 25-Jun-08
Sinefungin
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SYNONYMS 6,9-Diamino-1-(6-amino-9H-purin-9-yl)-1,5,6,7,8,9-hexadeoxy-D-glycero-α-L-talo-decafuranuronic acid
A-9145
Adenosylornithine
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Antifungal
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ALX-380-070-M001   1 mg 70.00 USD Add To Cart
ALX-380-070-M005   5 mg 280.00 USD Add To Cart
Product Specification
FORMULA: C15H23N7O5
MW: 381.4
CAS NUMBER: 58944-73-3
MERCK INDEX: 14: 8544
PURITY: ≥95% (HPLC)
APPEARANCE: White to yellow powder.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Strong competitive inhibitor of methyltransferases which uses S-adenosyl-1-methionine as the methyl group donor to yield methylated products such as 5-methylcytosine or N6-methyl adenosine on DNA and RNA. In addition, sinefungin is involved in a number of physiological processes.
Product Specific Literature References
A9145, a new adenine-containing antifungal antibiotic. I. Discovery and isolation: R.L. Hamil & M.M. Hoehn (Tokyo); J. Antibiot. 26, 463 (1973) Abstract
Sinefungin, a potent inhibitor or S-adenosylmethionine: protein O- methyltransferase: R.T. Borchardt, et al.; BBRC 89, 919 (1979) Abstract
Effects of S-adenosylhomocysteine and analogs on Epstein-Barr virus- induced transformation, expression of the Epstein-Barr virus capsid antigen, and methylation of Epstein-Barr virus DNA: W.K. Long, et al.; J. Virol. 61, 221 (1987) Abstract
Differential binding of S-adenosylmethionine S-adenosylhomocysteine and Sinefungin to the adenine-specific DNA methyltransferase M.TaqI: G. Schluckebier, et al.; J. Mol. Biol. 265, 56 (1997) Abstract
Two intertwined methylation activities of the MmeI restriction- modification class-IIS system from Methylophilus methylotrophus: J. Tucholski, et al.; Gene 223, 293 (1998) Abstract
Enzyme-mediated cytosine deamination by the bacterial methyltransferase M.MspI: J.M. Zingg, et al.; Biochem. J. 332, 223 (1998) Abstract
The 2.2 A structure of the rRNA methyltransferase ErmC' and its complexes with cofactor and cofactor analogs: implications for the reaction mechanism: G. Schluckebier, et al.; J. Mol. Biol. 289, 277 (1999) Abstract
Substrate binding in vitro and kinetics of RsrI [N6-adenine] DNA methyltransferase: S.S. Szegedi, et al.; Nucl. Acids Res. 28, 3962 (2000) Abstract
Identification of prenylcysteine carboxymethyltransferase in bovine adrenal chromaffin cells: H.M. De Busser, et al.; Int. J. Biochem. Cell Biol. 32, 1007 (2000) Abstract
Further Categories Containing This Product:
Other Antibiotics - DNA Regulation / Transcription • DNA & RNA Methyl & Alkyl Transferases / Related Products
 
 
ALX-380-242 Revised 03-Apr-08
Chaetocin (high purity)
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antitumor Antibiotics
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ALX-380-242-M001   1 mg 330.00 USD Add To Cart
Product Specification
FORMULA: C30H28N6O6S4
MW: 696.9
CAS NUMBER: 28097-03-2
RTECS: FM3032000
SOURCE/HOST: Isolated from Chaetomium sp. MST-FP2085.
PURITY: ≥99% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO, dimethyl formamide, methanol or 100% ethanol; poorly soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: HARMFUL.

Product Description
Antitumor antibiotic. Specific inhibitor of the lysine-specific methyltransferase SU(VAR)3-9 both in vitro and in vivo.
Product Specific Literature References
Isolation and configuration of Chaetocin: D. Hauser, et al.; Helv. Chim. Acta. 53, 1061 (1970)
Identification of a specific inhibitor of the histone methyltransferase SU(VAR)3-9: D. Greiner, et al.; Nat. Chem. Biol. 1, 143 (2005) Abstract
Chaetocin: a promising new antimyeloma agent with in vitro and in vivo activity mediated via imposition of oxidative stress: C.R. Isham, et al.; Blood 109, 2579 (2007) Abstract
Further Categories Containing This Product:
DNA & RNA Methyl & Alkyl Transferases / Related Products
 
 
ALX-480-019 Revised 17-Nov-08
O6-Benzylguanine
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PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY DNA & RNA Methyl & Alkyl Transferases / Related Products
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ALX-480-019-M010   10 mg 30.00 USD Add To Cart
ALX-480-019-M050   50 mg 95.00 USD Add To Cart
Product Specification
FORMULA: C12H11N5O
MW: 241.2
CAS NUMBER: 19916-73-5
PURITY: ≥99%
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in methanol (20mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
HAZARD: IRRITANT.
IDENTITY: Identity determined by 1H-NMR.

Product Description
Effective substrate and efficient inactivator of DNA alkyltransferase.
Product Specific Literature References
Activation of human O6-alkylguanine-DNA alkyltransferase by DNA: K. Goodtzova, et al.; Biochemistry 33, 8385 (1994) Abstract
Differential inactivation of mammalian and Escherichia coli O6-alkylguanine-DNA alkyltransferases by O6-benzylguanine: R.H. Elder, et al.; Biochem. J. 298, 231 (1994) Abstract
O6-benzylguanine and its role in chemotherapy: M.E. Dolan & A.E. Pegg; Cancer Res. 3, 837 (1997) Abstract
Prolonged inhibition of O(6)-methylguanine DNA methyltransferase in human tumor cells by O(6)-benzylguanine in vitro and in vivo: E.L. Kreklau, et al.; Pharmacol. Exp. Ther. 291, 1269 (1999) Abstract
 
 
ALX-480-096 Revised 18-Aug-08
5-Aza-2'-deoxycytidine
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SYNONYMS 5-Aza-CdR
5-Aza-dC
5-Deoxy-2'-azacytidine
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Nucleobases
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ALX-480-096-M005   5 mg 240.00 USD Add To Cart
Product Specification
FORMULA: C8H12N4O4
MW: 228.2
CAS NUMBER: 2353-33-5
RTECS: XZ3012000
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: 25mg/ml soluble in DMSO or 50% acetic acid; 1mg/ml soluble in methanol. (Warming may be required to achieve complete solubilization.)
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Packaged under inert gas. After reconstitution, prepare aliquots and store at -20°C.
HAZARD: HARMFUL.

Product Description
Inhibitor of DNA methyltransferase. Restores mRNA and protein expression of caspase-8 and TRAIL (tumor necrosis factor-related apoptosis inducing ligand) sensitivity of resistant cell lines. Enhances apoptosis induced by HDAC (histone deacetylase) inhibitors.
Product Specific Literature References
Incorporation of a potent antileukemic agent, 5-aza-2'-deoxycytidine, into DNA of cells from leukemic mice: J. Vesely and A. Cihak; Cancer Res. 37, 3684 (1977) Abstract
Cellular differentiation, cytidine analogs and DNA methylation: P.A. Jones and S.M. Taylor; Cell 20, 85 (1980) Abstract
The effects of 5-azacytidine and 5-azadeoxycytidine on chromosome structure and function: implications for methylation-associated cellular processes: T. Haaf; Pharmacol. Ther. 65, 19 (1995) Abstract
Loss of caspase-8 expression in highly malignant human neuroblastoma cells correlates with resistance to tumor necrosis factor-related apoptosis-inducing ligand-induced apoptosis: S. Hopkins-Donaldson, et al.; Cancer Res. 60, 4315 (2000) Abstract; Full Text
Resistance to tumor necrosis factor-related apoptosis-inducing ligand (TRAIL)-induced apoptosis in neuroblastoma cells correlates with a loss of caspase-8 expression: A. Eggert, et al.; Cancer Res. 61, 1314 (2001) Abstract; Full Text
5-Aza-2'-deoxycytidine induces histone hyperacetylation of mouse centromeric heterochromatin by a mechanism independent of DNA demethylation: S. Takebayashi, et al.; BBRC 288, 921 (2001) Abstract
DNA methyltransferase inhibition enhances apoptosis induced by histone deacetylase inhibitors: W.G. Zhu, et al.; Cancer Res. 61, 1327 (2001) Abstract; Full Text
Further Categories Containing This Product:
DNA & RNA Methyl & Alkyl Transferases / 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
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-350-014 Revised 03-Apr-08
Calyculin A
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Other Signal Transduction Pathway Modulators
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-014-C010   10 µg 65.00 USD Add To Cart
ALX-350-014-C025   25 µg 110.00 USD Add To Cart
ALX-350-014-C050   50 µg 190.00 USD Add To Cart
ALX-350-014-C100   100 µg 320.00 USD Add To Cart
Product Specification
FORMULA: C50H81N4O15P
MW: 1009.2
CAS NUMBER: 101932-71-2
SOURCE/HOST: Isolated from Discodermia calyx.
PURITY: ≥95%
APPEARANCE: Lyophilized.
SOLUBILITY: Soluble in DMSO, 100% ethanol, methanol, acetonitrile, chloroform, methylene chloride or benzene. Insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: May by subject to isomerization when in solution. Biological activity is not affected by isomerization.
HANDLING: Protect from light and moisture.
HAZARD: TOXIC. MAY BE CARCINOGENIC.

Product Description
Potent cell permeable inhibitor with high specificity for protein phosphatase 1 (PP1) and 2A (PP2A). Inhibits p130cas tyrosine phosphorylation. Enhances the phosphorylation level of NF-κB. Affects intracellular signalling processes that require 14-3-3. Potent non-phorbol type tumor promoter. Prevents γ-radiation induced apoptosis.
Product Specific Literature References
Okadaic acid: an additional non-phorbol-12-tetradecanoate-13-acetate- type tumor promoter: M. Suganuma, et al.; PNAS 85, 1768 (1988) Abstract
Protein phosphatases come of age: P.Cohen & P.T. Cohen; J. Biol. Chem. 264, 21435 (1989) Abstract; Full Text
Calyculin A and okadaic acid: inhibitors of protein phosphatase activity: H. Ishihara,