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DNA Regulation / Transcription
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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-270-444 Revised 07-Apr-08
ABT-888
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SYNONYMS 2-[(2R)-2-Methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide . dihydrochloride
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY PARP Inhibitors
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ALX-270-444-M001   1 mg 50.00 USD Add To Cart
ALX-270-444-M005   5 mg 150.00 USD Add To Cart
Product Specification
FORMULA: C13H16N4O . 2HCl
MW: 244.3 . 73.0
CAS NUMBER: 912445-05-7
PURITY: ≥98% (HPLC)
APPEARANCE: Colorless to white crystalline solid.
SOLUBILITY: Soluble in water or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
IDENTITY: Identity determined by 1H-NMR.

Product Description

Potent inhibitor of PARP-1 and PARP-2 (potency ≤5nM in vitro). Does not inhibit other NAD-binding enzymes. Has minimal CYP450 inhibition and induction. Shows broad spectrum of chemo- and radiopotentiation. Enantiomeric purity ≥97% suitable for in vivo studies. Does not show inherent cytotoxicity and shows no single agent activity in tumor models. Has excellent bioavailability and good blood-brain permeation. Increases tumor growth delay resulting from radiation and DNA-damaging agents.
Product Specific Literature References
Inhibition of poly(ADP-ribose) polymerase enhances cell death and improves tumor growth delay in irradiated lung cancer models: J.M. Albert, et al.; Clin. Cancer Res. 13, 3033 (2007) Abstract
ABT-888, an orally active poly(ADP-ribose) polymerase inhibitor that potentiates DNA-damaging agents in preclinical tumor models: C.K. Donawho, et al.; Clin. Cancer Res. 13, 2728 (2007) Abstract
 
 
ALX-270-450 Revised 08-Jan-07
3-Methyl-5-AIQ . hydrochloride
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SYNONYMS 3-Methyl-5-aminoisoquinolinone . HCl
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY PARP Inhibitors
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ALX-270-450-M001   1 mg 50.00 USD Add To Cart
ALX-270-450-M005   5 mg 200.00 USD Add To Cart
Product Specification
FORMULA: C10H10N2O . HCl
MW: 174.2 . 36.4
PURITY: ≥98% (NMR)
APPEARANCE: Light brown solid.
SOLUBILITY: Soluble in water or DMSO; poorly soluble in 100% ethanol or methanol; insoluble in dichloromethane or ethyl acetate.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from moisture.
IDENTITY: Identity determined by IR, 1H-NMR, 13C-NMR.

Product Description
Water-soluble, potent inhibitor of poly(ADP-ribose) polymerase-1 (PARP-1) (IC50=0.23µM) in vitro. Exhibits outstanding therapeutic benefits in models of myocardial infarction, ischaemia-reperfusion of the liver and kidney, heart transplantation and acute lung inflammation.
Product Specific Literature References
Synthesis and PARP-1 inhibitory activity of 3-substituted analogues of the potent water-soluble PARP inihbitor 5-aminoisoquinolin-1-one (5-AIQ): E. C. Y. Woon, et al.; Bioorg. Med. Chem. (submitted), (2006)
 
 
ALX-270-452 Revised 27-Nov-06
DR2313
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SYNONYMS 2-Methyl-3,5,7,8-tetrahydrothiopyrano[4,3-d]pyrimidine-4-one
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY PARP Inhibitors
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ALX-270-452-M001   1 mg 20.00 USD Add To Cart
ALX-270-452-M005   5 mg 60.00 USD Add To Cart
ALX-270-452-M025   25 mg 180.00 USD Add To Cart
Product Specification
FORMULA: C8H10N2OS
MW: 182.2
CAS NUMBER: 284028-90-6
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO, methanol or water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stock solutions are stable for up to 3 months when stored at -20°C.
HANDLING: After reconstitution, prepare aliquots and store at -20°C. Protect from light.
HAZARD: HARMFUL.

Product Description
Potent, water soluble competitive PARP inhibitor (IC50=0.20µM and 0.24µM for PARP-1 and PARP-2 respectively).
Product Specific Literature References
A newly synthesized poly(ADP-ribose) polymerase inhibitor, DR2313 [2-methyl-3,5,7,8-tetrahydrothiopyrano[4,3-d]-pyrimidine-4-one]: pharmacological profiles, neuroprotective effects, and therapeutic time window in cerebral ischemia in rats: H. Nakajima, et al.; Pharmacol. Exp. Ther. 312, 472 (2005) Abstract; Full Text
 
 
ALX-270-458 Revised 15-Jan-08
PPM-18
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SYNONYMS 2-Benzoylamino-1,4-naphthoquinone
PRODUCT LINE Nitric Oxide Pathway
PRODUCT CATEGORY NOS Inhibitors (NOS Induction & Enzyme Activity)
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ALX-270-458-M010   10 mg 140.00 USD Add To Cart
Product Specification
FORMULA: C17H11NO3
MW: 277.3
CAS NUMBER: 65240-86-0
PURITY: ≥97% (HPLC)
APPEARANCE: Yellow to orange solid.
SOLUBILITY: Soluble in DMSO or acetonitrile.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY:

Stable for at least 3 years after receipt when stored at -20°C.
HANDLING: Packaged under inert gas. Protect from light. After reconstitution, prepare aliquots and store at -20°C.

Product Description
Cell permeable, anti-inflammatory agent that inhibits expression of iNOS (NOS II) (IC50~5mM). Blocks activation of NF-κB in vitro and in vivo. Does not directly affect enzymatic activities of iNOS (NOS II) or eNOS (NOS III).
Product Specific Literature References
Synthesis and antiplatelet, antiinflammatory and antiallergic activities of 2,3-disubstituted 1,4-naphthoquinones: J.C. Lien, et al.; Chem. Pharm. Bull. (Tokyo) 44, 1181 (1996) Abstract
Inhibition of nitric oxide synthase expression by PPM-18, a novel anti-inflammatory agent, in vitro and in vivo: S.M. Yu, et al.; Biochem. J. 328, 363 (1997) Abstract; Full Text
Shear stress regulates endothelial nitric-oxide synthase promoter activity through nuclear factor kappaB binding: M.E. Davis, et al.; J. Biol. Chem. 279, 163 (2004) Abstract; Full Text
Further Categories Containing This Product:
NF-kB Pathway Modulators • Anti-inflammatory Agents 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-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-270-475 Revised 17-Jan-08
Ciprofibrate
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SYNONYMS 2-[4-(2,2-Dichlorocyclopropyl)phenoxy]-2-methylpropanoic acid
PRODUCT LINE Obesity & Adipokines
PRODUCT CATEGORY Cholesterol & Lipid Transport / Related Products
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ALX-270-475-M025   25 mg 50.00 USD Add To Cart
ALX-270-475-M100   100 mg 150.00 USD Add To Cart
ALX-270-475-M250   250 mg 300.00 USD Add To Cart
Product Specification
FORMULA: C13H14Cl2O3
MW: 289.2
CAS NUMBER: 52214-84-3
MERCK INDEX: 14: 2313
RTECS: UF0880000
PURITY: ≥98% (HPLC)
APPEARANCE: White to light yellow powder.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: TOXIC. MAY BE CARCINOGENIC.

Product Description
Hypolipidemic compound. PPARα (peroxisome proliferator-activated receptor α) agonist.
Product Specific Literature References
Comparison of the effects of various peroxisome proliferators on peroxisomal enzyme activities, DNA synthesis, and apoptosis in rat and human hepatocyte cultures: V. Goll, et al.; Toxicol. Appl. Pharmacol. 160, 21 (1999) Abstract
Phosphorylation of peroxisome proliferator-activated receptor alpha in rat Fao cells and stimulation by ciprofibrate: P. Passilly, et al.; Biochem. Pharmacol. 58, 1001 (1999) Abstract
Differences in cell proliferation in rodent and human hepatic derived cell lines exposed to ciprofibrate: M.C. Clemencet, et al.; Cancer Lett. 222, 217 (2005) Abstract
P450 CYP2C epoxygenase and CYP4A ω-hydroxylase mediate ciprofibrate-induced PPARα-dependent peroxisomal proliferation: A. Gatica, et al.; J. Lipid Res. 48, 924 (2007) Abstract; Full Text
Related Products
Further Categories Containing This Product:
PPAR Agonists • Apoptosis Inducers & Inhibitors Other Products
 
 
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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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
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-270-480 Revised 10-Mar-08
Caffeic acid ethyl ester
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SYNONYMS CAEE
Ethyl caffeate
PRODUCT LINE Na