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Histones & Histone Modification
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ALX-270-484 Revised 07-Apr-08
AGK2
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SYNONYMS 2-Cyano-3-[5-(2,5-dichlorophenyl)-2-furanyl]-N-5-quinolinyl-2-propenamide
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY Sirtuins / Related Products
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ALX-270-484-M001   1 mg 40.00 USD Add To Cart
ALX-270-484-M005   5 mg 130.00 USD Add To Cart
Product Specification
FORMULA: C23H13Cl2N3O2
MW: 434.3
CAS NUMBER: 304896-28-4
PURITY: ≥95%
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO (>5mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
IDENTITY: Identity determined by 1H-NMR.

Product Description
Potent, selective and cell permeable inhibitor of sirtuin 2 (SIRT2) (IC50=3.5μM). Rescues α-synuclein-mediated toxicity. Modifies inclusion morphology in a cellular model of Parkinson’s disease. Protects against dopaminergic cell death. Leads to an increase in acetylated tubulin.
Product Specific Literature References
Sirtuin 2 inhibitors rescue alpha-synuclein-mediated toxicity in models of Parkinson’s disease: T.F. Outeiro, et al.; Science 317, 516 (2007) Abstract
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Further Categories Containing This Product:
Parkinson's Disease Other Products
 
 
ALX-270-381 Revised 28-Sep-07
Anacardic acid
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SYNONYMS 2-Hydroxy-6-pentadecylbenzoic acid
6-Pentadecylsalicylic acid
AA
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY Histone Acetyl- & Methyl-Transferases / Related Products
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ALX-270-381-M005   5 mg 40.00 USD Add To Cart
ALX-270-381-M025   25 mg 140.00 USD Add To Cart
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Product Specification
FORMULA: C22H36O3
MW: 348.5
MERCK INDEX: 14: 621
SOURCE/HOST: Synthetic.
PURITY: ≥95% (1H-NMR)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in 100% ethanol, methanol, DMSO, dichloromethane or ethylacetate.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Stock solutions are stable for up to 3 months when stored at -20°C.
HANDLING: Protect from light. After reconstitution, prepare aliquots and store at -20°C. Packaged under inert gas.

Product Description
Cell permeable salicylic acid analog that acts as a potent, non-competitive inhibitor of p300 and PCAF (p300/CBP-associated factor) histone acetyltransferase (HAT) activities (IC50~8.5µM and ~5µM, respectively). Displays a variety of other biological activities, such as antibacterial, antimicrobial, prostaglandin synthase inhibition, tyrosinase, and lipoxygenase inhibition.
Product Specific Literature References
Anacardic Acid: molluscicide in cashew nut shell liquid: J.T. Sullivan, et al.; Planta Med. 44, 175 (1982) Abstract
Inhibition of lipoxygenase and prostaglandin endoperoxide synthase by anacardic acids: R. Grazzini, et al.; BBRC 176, 775 (1991) Abstract
Antibacterial activity of anacardic acid and totarol, alone and in combination with methicillin, against methicillin-resistant Staphylococcus aureus: H. Muroi & I. Kubo; J. Appl. Bacteriol. 80, 387 (1996) Abstract
Small molecule modulators of histone acetyltransferase p300: K. Balasubramanyam, et al.; J. Biol. Chem. 278, 19134 (2003) Abstract; Full Text
Inhibition of histone acetyltransferase activity by anacardic acid sensitizes tumor cells to ionizing radiation: Y. Sun, et al.; FEBS Lett. 580, 4353 (2006) Abstract
General Literature References
Antibacterial activity of anacardic acid and totarol, alone and in combination with methicillin, against methicillin-resistant Staphylococcus aureus: H. Muroi and I. Kubo; J. Appl. Bacteriol. 80, 387 (1996) Abstract
Synthesis of sildenafil analogues from anacardic acid and their phosphodiesterase-5 inhibition: R. Paramashivappa, et al.; J. Agric. Food Chem. 50, 7709 (2002) Abstract
Further Categories Containing This Product:
Prostaglandin Synthases / Related Products • Lipoxygenases / Related Products • Antibiotics Other Products
 
 
ALX-350-095 Revised 03-Apr-08
Apicidin
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SYNONYMS cyclo-L-(2-Amino-8-oxodecanoyl)-L-(N-methoxy-tryptophan)-L-isoleucyl-D-pipecolinyl
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Other Natural Products - DNA Regulation / Transcription
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ALX-350-095-M001   1 mg 50.00 USD Add To Cart
ALX-350-095-M005   5 mg 200.00 USD Add To Cart
Product Specification
FORMULA: C34H49N5O6
MW: 623.8
CAS NUMBER: 183506-66-3
SOURCE/HOST: Isolated from Fusarium sp.
PURITY: ≥95% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: VERY TOXIC.

Product Description
Potent inhibitor of histone deacetylase (HDAC). Inhibits proliferation. Induces cell cycle arrest. Stimulates apoptosis of cancer cells. Antiprotozoal.
Product Specific Literature References
Apicidin: a novel antiprotozoal agent that inhibits parasite histone deacetylase: S.J. Darkin-Rattray, et al.; PNAS 93, 13143 (1996) Abstract
Apicidin, a histone deacetylase inhibitor, inhibits proliferation of tumor cells via induction of p21WAF1/Cip1 and gelsolin: J.W. Han, et al.; Cancer Res. 60, 6068 (2000) Abstract
Transcriptional activation of p21(WAF1/CIP1) by apicidin, a novel histone deacetylase inhibitor: J.S. Kim, et al.; BBRC 281, 866 (2001) Abstract
Broad spectrum antiprotozoal agents that inhibit histone deacetylase: structure-activity relationships of apicidin. Part 1: S.L. Colletti, et al.; Bioorg. Med. Chem. Lett. 11, 107 (2001) Abstract
Broad spectrum antiprotozoal agents that inhibit histone deacetylase: structure-activity relationships of apicidin. Part 2: S.L. Colletti, et al.; Bioorg. Med. Chem. Lett. 11, 113 (2001) Abstract
Structure and chemistry of apicidins, a class of novel cyclic tetrapeptides without a terminal alpha-keto epoxide as inhibitors of histone deacetylase with potent antiprotozoal activities: S.B. Singh, et al.; J. Org. Chem. 67, 815 (2002) Abstract
Apicidin, a histone deacetylase inhibitor, induces differentiation of HL-60 cells: J. Hong, et al.; Cancer Lett. 189, 197 (2003) Abstract
Activation of NF-kappaB by HDAC inhibitor apicidin through Sp1-dependent de novo protein synthesis: its implication for resistance to apoptosis: Y.K. Kim, et al.; Cell Death Differ. 13, 2033 (2006) Abstract
Apicidin, a novel histone deacetylase inhibitor, has profound anti-growth activity in human endometrial and ovarian cancer cells: T. Ueda, et al.; Int. J. Mol. Med. 19, 301 (2007) Abstract
Further Categories Containing This Product:
Cell Cycle Blockers & Inhibitors / Related Products • HDAC Inhibitors • Natural Products for Cell Cycle Research • Natural Products - Other Anti-infective Agents • Parasitic Diseases Other Products • Natural Products - Apoptosis Inducers & Inhibitors
 
 
ALX-350-129 Revised 04-Dec-07
Aristoforin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Apoptosis Inducers & Inhibitors
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ALX-350-129-M001   1 mg 190.00 USD Add To Cart
Product Specification
FORMULA: C37H54O6
MW: 594.8
CAS NUMBER: 849215-53-8
PURITY: ≥95%
APPEARANCE: White to yellow oil.
SOLUBILITY: Soluble in DMSO or 100mM sodium hydrogen carbonate/2% DMSO.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: TOXIC.

Product Description
Stable and water-soluble derivative of hyperforin (Prod. No. ALX-350-097) inducing apoptosis. Antitumor agent. Inhibits sirtuins.
Product Specific Literature References
Aristoforin, a novel stable derivative of hyperforin, is a potent anticancer agent: M. Gartner, et al.; Chembiochem. 6, 171 (2005) Abstract
Phloroglucinol Derivatives Guttiferone G, Aristoforin, and Hyperforin: Inhibitors of Human Sirtuins SIRT1 and SIRT2: C. Gey, et al.; Angew. Chem. Int. Ed. Engl. 46, 5219 (2007) Abstract
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Further Categories Containing This Product:
Antitumor Agents (Apoptosis Inducers) • Sirtuins / Related Products • Natural Products - Antitumor Reagents
 
 
ALX-270-485 Revised 07-Apr-08
B2
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SYNONYMS CPNQ
5-[4-(4-Chlorobenzoyl)-1-piperazinyl]-8-nitroquinoline
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY Sirtuins / Related Products
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ALX-270-485-MC05   0.5 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C20H17ClN4O3
MW: 396.8
CAS NUMBER: 115687-05-3
PURITY: ≥95%
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO (>5mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light and oxygen.
HAZARD: TOXIC.
IDENTITY: Identity determined by 1H-NMR.

Product Description
Cell permeable inhibitor of sirtuin 2 (SIRT2) (IC50=35μM). Promotes inclusion formation in cellular models of both Huntington’s disease and Parkinson’s disease. Prevents huntingtin-mediated proteasome dysfunction and reduces α-synuclein-mediated toxicity.
Product Specific Literature References
Pharmacological promotion of inclusion formation: a therapeutic approach for Huntington’s and Parkinson’s diseases: R.A. Bodner, et al.; PNAS 103, 4246 (2006) Abstract; Full Text
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Further Categories Containing This Product:
Parkinson's Disease Other Products
 
 
ALX-270-473 Revised 13-Jun-08
BIX 01294
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SYNONYMS 2-(Hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-[1-(phenylmethyl)-4-piperidinyl]4-quinazolinamine
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY Histone Acetyl- & Methyl-Transferases / Related Products
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ALX-270-473-M002   2 mg 190.00 USD Add To Cart
Product Specification
FORMULA: C28H38N6O2
MW: 490.6
CAS NUMBER: 935693-62-2
PURITY: ≥95%
APPEARANCE: Light brown to brown solid.
SOLUBILITY: Soluble in DMSO (5mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
IDENTITY: Determined by 1H-NMR, 13C-NMR and MS.

Product Description
Selective and cell permeable inhibitor of G9a histone methyltransferase.
Product Specific Literature References
Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase: S. Kubicek, et al.; Mol. Cell 25, 473 (2007) Abstract
 
 
ALX-350-246 Revised 07-Oct-08
Butein
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SYNONYMS 2',3,4,4'-Tetrahydroxychalcone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-246-M010   10 mg 190.00 USD Add To Cart
Product Specification
FORMULA: C15H12O5
MW: 272.3
CAS NUMBER: 487-52-5
PURITY: ≥98% (HPLC)
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO (>50mg/ml) or methanol; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light. Keep cool and dry under inert gas.
IDENTITY: Identity determined by 1H-NMR, 13C-NMR and MS.

Product Description
Plant polyphenol. Specific tyrosine kinase inhibitor. Potently inhibits the tyrosine kinase activity of the EGF receptor and p60c-src. Potent antioxidant and anti-inflammatory agent. Inhibits glutathione reductase and rat liver glutathione S-transferase. Activator of human deacetylase SIRT1. Inhibits aromatase, showing chemopreventive properties. Directly inhibits IKK.
Product Specific Literature References
Inhibition of 12-O-tetradecanoylphorbol-13-acetate-mediated epidermal ornithine decarboxylase induction and skin tumor promotion by new lipoxygenase inhibitors lacking protein kinase C inhibitory effects: E. Aizu, et al.; Carcinogenesis 7, 1809 (1986) Abstract
Protective effects of hydroxychalcones on free radical-induced cell damage: S. Sogawa, et al.; Biol. Pharm. Bull. 17, 251 (1994) Abstract
Cytotoxic effect of butein on human colon adenocarcinoma cell proliferation: C.C. Yit & N.P. Das; Cancer Lett. 82, 65 (1994) Abstract
Inhibitory effects of plant polyphenols on rat liver glutathione S-transferase: K. Zhang & N.P. Das; Biochem. Pharmacol. 47, 2063 (1994) Abstract
Endothelium-dependent relaxation of rat aorta by butein, a novel cyclic AMP-specific phosphodiesterase inhibitor: S.M. Yu, et al.; Eur. J. Pharmacol. 280, 69 (1995) Abstract
Butein (3,4,2',4'-tetrahydroxychalcone) ameliorates experimantal anti-glomerular basement membrane antibody-associated glomerulonephritis (3): K. Hayashi, et al.; Eur. J. Pharmacol. 316, 297 (1996) Abstract
Inhibition of glutathione reductase by plant polyphenols: K. Zhang, et al.; Biochem. Pharmacol 54, 1047 (1997) Abstract
Butein, a specific protein tyrosine kinase inhibitor: E.-B. Yang, et al.; BBRC 245, 435 (1998) Abstract
Antioxidant properties of butein isolated from Dalbergia odorifera: Z.J. Cheng, et al.; Biochim. Biophys. Acta 1392, 291 (1998) Abstract
Flavonoids inhibit cell growth and induce apoptosis in B16 melanoma 4A5 cells: K. Iwashita, et al.; Biosci. Biotechnol. Biochem. 64, 1813 (2000) Abstract
Butein, a plant polyphenol, induces apoptosis concomitant with increased caspase-3 activity, decreased Bcl-2 expression and increased Bax expression in HL-60 cells: N.Y. Kim, et al.; Pharmacol. Toxicol. 88, 261 (2001) Abstract
Small molecule activators of sirtuins extend Saccharomyces cerevisiae lifespan: K.T. Howitz, et al.; Nature 425, 191 (2003) Abstract
The plant polyphenol butein inhibits testosterone-induced proliferation in breast cancer cells expressing aromatase: Y. Wang, et al.; Life Sci. 77, 39 (2005) Abstract
Butein, a tetrahydroxychalcone, inhibits nuclear factor (NF)-kappaB and NF-kappaB-regulated gene expression through direct inhibition of IkappaBalpha kinase beta on cysteine 179 residue: M.K. Pandey, et al.; J. Biol. Chem. 282, 17340 (2007) Abstract
Further Categories Containing This Product:
Tyrosine Kinase Inhibitors • Natural Products - Anti-inflammatory Agents • EGFR Kinase Inhibitors • Glutathione / Related Products • Chalcones • Phosphodiesterases / Related Products • Natural Products - Chemopreventive Agents • Glutathione S-Transferase • Natural Products - Antioxidants • Sirtuins / Related Products • IkB Kinases [IKKs] / Related Products
 
 
ALX-270-411 Revised 01-Apr-08
Butyrolactone 3
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SYNONYMS Gcn5 Inhibitor 1
MB-3
3-Methylene-4-hydroxycarbonyl-5-(1-propyl)-tetrahydrofuran-2-one
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY Histone Acetyl- & Methyl-Transferases / Related Products
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ALX-270-411-M005   5 mg 190.00 USD Add To Cart
Product Specification
FORMULA: C9H12O4
MW: 184.2
CAS NUMBER: 778649-18-6
SOURCE/HOST: Synthetic.
PURITY: ≥95% (1H-NMR)
APPEARANCE: White solid.
SOLUBILITY: Soluble in DMSO or methanol.
SHIPPING: AMBIENT
SHORT TERM STORAGE: +4°C
LONG TERM STORAGE: -20°C
USE/STABILITY: Stock solutions in DMSO are stable for at least 2 months when stored at -20°C.

Product Description
Racemic. Inhibitor of human histone acetyltransferase Gcn5.
Product Specific Literature References
Design, synthesis, and biological evaluation of a small-molecule inhibitor of the histone acetyltransferase Gcn5: M. Biel, et al.; Angew. Chem. Int. Ed. Engl. 43, 3974 (2004) Abstract
 
 
ALX-201-283 Revised 18-Mar-08
CARM1 (human) (recombinant) (His)
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SYNONYMS Coactivator-associated Arginine Methyltransferase 1 (human) (recombinant) (His)
PRMT4 (human) (recombinant) (His)
Protein Arginine N-Methyltransferase 4 (human) (recombinant) (His)
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY Histone Acetyl- & Methyl-Transferases / Related Products
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ALX-201-283-C002   2 µg 280.00 USD Add To Cart
Product Specification
EC: EC 2.1.1.125
SOURCE/HOST: Produced in SF21 cells. Fused to a His-tag.
CONCENTRATION: 0.5mg/ml
PURITY: ≥90% (SDS-PAGE)
FORMULATION: Liquid. In 50mM TRIS-HCl, pH 7.5, containing 100mM sodium chloride, 0.2% NP-40, 50mM imidazole and 10% glycerol.
SPECIFIC ACTIVITY: ~50-100ng are required for standard HAT assay.
SHIPPING: SHIPPED ON DRY ICE
SHORT TERM STORAGE: -80°C
HANDLING: After opening, prepare aliquots and store in liquid nitrogen. Avoid freeze/thaw cycles.
Product Specific Literature References
Arginine methyltransferase CARM1 is a promoter-specific regulator of NF-kappaB-dependent gene expression: M. Covic, et al.; EMBO J. 24, 85 (2005) Abstract; Full Text
General Information
BACKGROUND/TECHNICAL INFORMATION Swiss-Prot link Q86X55: CARM1 (human)
Further Categories Containing This Product:
Recombinant Proteins / Fusion Proteins
 
 
ALX-270-437 Revised 07-Oct-08
6-Chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide
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PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY Sirtuins / Related Products
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ALX-270-437-M001   1 mg 110.00 USD Add To Cart
Product Specification
FORMULA: C13H13ClN2O
MW: 248.7
CAS NUMBER: 49843-98-3
PURITY: ≥95%
APPEARANCE: White to beige powder.
SOLUBILITY: Soluble in DMSO (10mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least 6 months when stored at -20°C in the dark.
HANDLING: Protect from light.
IDENTITY: Identity determined by 1H-NMR, 13C-NMR and MS.

Product Description
Potent cell permeable and metabolically stable specific inhibitor of hSIRT1 (IC50=98nM in vivo / IC50=38nM in vitro; compared to hSIRT2: IC50=19µM and hSIRT3: IC50=48µM) with no effect on human histone deacetylases (HDACs) class I and class II, nor NAD glycohydrolase (IC50>100µg). Inhibits the deacetylation of p53 (IC50=1µM).
Product Specific Literature References
Discovery of indoles as potent and selective inhibitors of the deacetylase SIRT1: A.D. Napper, et al.; J. Med. Chem. 48, 8045 (2005) Abstract
Small molecule activators of SIRT1 as therapeutics for the treatment of type 2 diabetes: J.C. Milne, et al.; Nature 450, 712 (2007) Abstract
Further Categories Containing This Product:
p53 Other Products
 
 
ALX-201-279 Revised 18-Mar-08
CREB Binding Protein (mouse) (recombinant) (His)
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SYNONYMS CBP (mouse) (recombinant) (His)
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY CREB & CREB Binding Protein / Related Products
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ALX-201-279-C002   2 µg 280.00 USD Add To Cart
Product Specification
EC: EC 2.3.1.48
SOURCE/HOST: Produced in SF21 cells. Fused to a His-tag.
CONCENTRATION: 0.5mg/ml
PURITY: ≥95% (SDS-PAGE)
FORMULATION: Liquid. In 50mM TRIS-HCl, pH 7.5, containing 100mM sodium chloride, 0.2% NP-40, 50-100mM imidazole and 10% glycerol.
SPECIFIC ACTIVITY: ~50-100ng are required for standard HAT assay.
SHIPPING: SHIPPED ON DRY ICE
SHORT TERM STORAGE: -80°C
HANDLING: Avoid freeze/thaw cycles. After opening, prepare aliquots and store in liquid nitrogen.
General Information
BACKGROUND/TECHNICAL INFORMATION Swiss-Prot link P45481: CREB Binding Protein (mouse)