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DNA Regulation / Transcription
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ALX-480-039 Revised 20-Oct-08
1,5-Isoquinolinediol
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SYNONYMS 5-Hydroxy-1(2H)-isoquinolinone
1,5-Dihydroxyisoquinoline
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY PARP Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-480-039-M005   5 mg 20.00 USD Add To Cart
ALX-480-039-M025   25 mg 60.00 USD Add To Cart
Product Specification
FORMULA: C9H7NO2
MW: 161.2
CAS NUMBER: 5154-02-9
PURITY: ≥98%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in 0.1N NaOH, methanol or in DMSO; insoluble in water and 0.1N HCl.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.
HAZARD: IRRITANT.

Product Description

Potent inhibitor of inducible nitric oxide synthase (iNOS; NOS II) in mouse macropaghes. Potently blocks poly(ADP-ribose) polymerase-1 (PARP-1). Neuroprotectant.
Product Specific Literature References
Specific inhibitors of poly(ADP-ribose) synthetase and mono(ADP-ribosyl)transferase: M. Banasik, et al.; J. Biol. Chem. 267, 1569 (1992) Abstract; Full Text
Nitric oxide activation of poly(ADP-ribose) synthetase in neurotoxicity: J. Zhang, et al.; Science 263, 687 (1994) Abstract
Effects of inhibitors of the activity of poly (ADP-ribose) synthetase on the organ injury and dysfunction caused by haemorrhagic shock: M.C. McDonald, et al.; Br. J. Pharmacol. 128, 1339 (1999) Abstract
All trans retinoic acid induces apoptosis in acute promyelocytic NB4 cells when combined with isoquinolinediol, a poly(ADP-ribose) polymerase inhibitor: D.M. Berry, et al.; Leuk. Res. 24, 307 (2000) Abstract
Inhibition of NOS-2 induction in LPS-stimulated J774.2 cells by 1, 5-isoquinolinediol, an inhibitor of PARP: R. Olszanecki, et al.; J. Physiol. Pharmacol. 57, 109 (2006) Abstract
Substrate-assisted catalysis by PARP10 limits its activity to mono-ADP-ribosylation: H. Kleine, et al.; Mol. Cell 32, 57 (2008) Abstract
Further Categories Containing This Product:
NOS Inhibitors (NOS Induction & Enzyme Activity) • DNA Repair Other Products
 
 
ALX-400-036 Revised 31-Oct-06
Peroxynitrite . tetramethylammonium
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SYNONYMS ONOO- . C4H12N
Oxoperoxonitrate(1-) . C4H12N
PRODUCT LINE Oxidative Stress
PRODUCT CATEGORY Peroxynitrite / Scavengers / Detection
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-400-036-L001   1 ml 152.00 USD Add To Cart
ALX-400-036-5001   5x1 ml 475.00 USD Add To Cart
Product Specification
FORMULA: NO3 . C4H12N
MW: 62.0 . 74.1
CAS NUMBER: 14042-01-4
CONCENTRATION: ~10mM
FORMULATION: Liquid. In 0.01M KOH.
SHIPPING: SHIPPED ON DRY ICE
LONG TERM STORAGE: -80°C
USE/STABILITY: Stable for at least 1 month after receipt when stored at -80°C.
HANDLING: Protect from light.
HAZARD: OXIDIZING. CORROSIVE.

Product Description
Produced from the reaction of nitrogen monoxide with tetramethylammonium superoxide according to the method of D.S. Bohle, et al. described in Meth. Enzymol. 269, 302 (1996), and dissolved in 0.01M potassium hydroxide (KOH). This formulation of peroxynitrite has a low nitrite content (~1%), no hydrogen peroxide.
Product Specific Literature References
DNA damage induced by peroxynitrite: subsequent biological effects: C. Szabo & H. Ohshima; Nitric Oxide 1, 373 (1997), (Review) Abstract
Peroxynitrite: a biologically significant oxidant: M.P. Murphy, et al.; Gen. Pharmacol. 31, 179 (1998), (Review) Abstract
Peroxynitrite: an endogenous oxidizing and nitrating agent: C. Ducrocq, et al.; Cell. Mol. Life Sci. 55, 1068 (1999), (Review) Abstract
The chemistry of DNA damage from nitric oxide and peroxynitrite: S. Burney, et al.; Mutat. Res. 424, 37 (1999), (Review) Abstract
Reactions of *NO, *NO2 and peroxynitrite in membranes: physiological implications: S.P. Goss, et al.; Free Radic. Res. 31, 597 (1999), (Review) Abstract
Peroxynitrite: reactive, invasive and enigmatic: J.T. Groves; Curr. Opin. Chem. Biol. 3, 226 (1999), (Review) Abstract
Nitric oxide and peroxynitrite. The ugly, the uglier and the not so good: a personal view of recent controversies: B. Halliwell, et al.; Free Radic. Res. 31, 651 (1999), (Review) Abstract
Assessment of peroxynitrite scavengers in vitro: B. Halliwell, et al.; Meth. Enzymol. 301, 333 (1999), (Review) Abstract
Chemistry of peroxynitrite and its relevance to biological systems: W.H. Koppenol; Met. Ions Biol. Syst. 36, 597 (1999), (Review) Abstract
Conformation of peroxynitrite: determination by crystallographic analysis: M. Worle, et al.; Chem. Res. Toxicol 12, 305 (1999) Abstract
Peroxynitrite scavenging by metalloporphyrins and thiolates: J.P. Crow; Free Radic. Biol. Med. 28, 1487 (2000), (Review) Abstract
Interaction of peroxynitrite with selenoproteins and glutathione peroxidase mimics: H. Sies & G.E. Arteel; Free Radic. Biol. Med. 28, 1451 (2000), (Review) Abstract
Reactions of Peroxynitrite with Phenolic and Carbonyl Compounds: Flavonoids are not Scavengers of Peroxynitrite: S. Tibi & W.H. Koppenol; Helv. Chim. Acta 83, 2412 (2000)
BCL-2 protects peroxynitrite-treated thymocytes from poly(ADP-ribose) synthase (PARS)-independent apoptotic but not from PARS-mediated necrotic cell death: L. Virag & C. Szabo; Free Radic. Biol. Med. 29, 704 (2000) Abstract
Peroxynitrite promotes mitochondrial permeability transition-dependent rapid u937 cell necrosis: survivors proliferate with kinetics superimposable on those of untreated cells: P. Sestili, et al.; Free Radic Res. 34, 513 (2001) Abstract
Peroxynitrite-induced cytotoxicity: mechanism and opportunities for intervention: L. Virag, et al.; Toxicol. Lett. 140-141, 113 (2003), (Review) Abstract
Preventing nitrite contamination in tetramethylammonium peroxynitrite solutions: P. Latal, et al.; Inorg. Chem. 43, 6519 (2004) Abstract
Further Categories Containing This Product:
PARP Other Products • DNA Repair Other Products
 
 
ALX-350-364 Revised 08-Apr-08
Psoralen
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SYNONYMS Ficusin
7H-Furo[3,2-g]benzopyran-7-one
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products with Antibiotic Activity
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ALX-350-364-M025   25 mg 95.00 USD Add To Cart
ALX-350-364-M100   100 mg 285.00 USD Add To Cart
Product Specification
FORMULA: C11H6O3
MW: 186.2
CAS NUMBER: 66-97-7
MERCK INDEX: 14: 7928
RTECS: LV0944000
SOURCE/HOST: Isolated from Psoralea corylifolia.
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white crystalline solid.
SOLUBILITY: Soluble in ethyl acetate or acetone; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: MAY BE MUTAGENIC. HARMFUL.

Product Description
Shows antiviral, antibacterial, antifungal and insecticidal properties. Binds DNA through single and double-stranded cross-linking after photoactivation. Used as photochemical probe in studies of DNA mutation and repair mechanisms. Causes photosensitization in human.
Product Specific Literature References
Psoralen phototoxicity: correlation with serum and epidermal 8-methoxypsoralen and 5-methoxypsoralen in the guinea pig: A. Kornhauser, et al.; Science 217, 733 (1982) Abstract
Psoralens as photoactive probes of nucleic acid structure and function: organic chemistry, photochemistry, and biochemistry: G.D. Cimino, et al.; Annu. Rev. Biochem. 54, 1151 (1985), (Review) Abstract
Electron microscopic identification of supercoiled regions in complex DNA structures: R.B. Inman & M. Schnos; J. Mol. Biol. 193, 377 (1987) Abstract
Probing DNA structure with psoralen in vitro: D.W. Ussery, et al.; Meth. Enzymol. 212, 242 (1992) Abstract
DNA interstrand cross-links induced by psoralen are not repaired in mammalian mitochondria: C. Cullinane & V.A. Bohr; Cancer Res. 58, 1400 (1998) Abstract; Full Text
Psoralen photocrosslinking, a tool to study the chromatin structure of RNA polymerase I--transcribed ribosomal genes: M. Toussaint, et al.; Biochem. Cell Biol. 83, 449 (2005) Abstract
Psoralen-induced DNA adducts are substrates for the base excision repair pathway in human cells: S. Couve-Privat, et al.; Nucl. Acids Res. 35, 5672 (2007) Abstract; Full Text
Site-directed gene mutation at mixed sequence targets by psoralen-conjugated pseudo-complementary peptide nucleic acids: K.H. Kim, et al.; Nucl. Acids Res. 35, 7604 (2007) Abstract; Full Text
Further Categories Containing This Product:
Natural Products - Antiviral / anti-HIV Agents • Natural Products - Antifungal Agents • Pesticides / Related Products • DNA Intercalators & Crosslinkers
 
 
ALX-380-042 Revised 05-May-08
Doxorubicin . hydrochloride
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SYNONYMS DXR . HCl
14-Hydroxydaunomycin . HCl
Adriamycin . HCl
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antitumor Antibiotics
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-380-042-M005   5 mg 60.00 USD Add To Cart
ALX-380-042-M010   10 mg 110.00 USD Add To Cart
ALX-380-042-M025   25 mg 250.00 USD Add To Cart
Product Specification
FORMULA: C27H29NO11 . HCl
MW: 543.5 . 36.5
CAS NUMBER: 25316-40-9
MERCK INDEX: 14: 3439
RTECS: QI9295900
SOURCE/HOST: Isolated from Streptomyces peucetius var. caesius.
PURITY: ≥98%
APPEARANCE: Red solid.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HAZARD: MAY BE CARCINOGENIC. MAY BE TERATOGENIC. TOXIC. MAY BE MUTAGENIC.

Product Description
Antitumor antibiotic. Induces DNA damage by intercalating into DNA and inhibiting topoisomerase II. Binds covalently to DNA. Inhbibits reverse transcriptase, RNA polymerase and the catalytic activity of Dnmt1. Immunosuppressive. Antineoplastic. Induces apoptosis.
Product Specific Literature References
Adriamycin and daunomycin induce programmed cell death (apoptosis) in tumour cells: A. Skladanowski & J. Konopa; Biochem. Pharmacol. 46, 375 (1993) Abstract
A critical evaluation of the mechanisms of action proposed for the antitumor effects of the anthracycline antibiotics adriamycin and daunorubicin: D.A. Gewirtz; Biochem. Pharmacol. 57, 727 (1999) Abstract
Doxorubicin treatment activates a Z-VAD-sensitive caspase, which causes deltapsim loss, caspase-9 activity, and apoptosis in Jurkat cells: S. Gamen, et al.; Exp. Cell Res. 258, 223 (2000) Abstract
Involvement of cyclin-dependent kinases in doxorubicin-induced apoptosis in human tumor cells: Y. Lu, et al.; Mol. Carcinog. 29, 1 (2000) Abstract
Characterization of Adriamycin-Induced G2 Arrest and Its Abrogation by Caffeine in FL-Amnion Cells with or without p53: Y. Minemoto, et al.; Exp. Cell Res. 262, 37 (2001) Abstract
Enhancement of Fas-mediated apoptosis in renal cell carcinoma cells by adriamycin: X.X. Wu, et al.; Cancer Res. 60, 2912 (2000) Abstract
Doxorubicin-induced apoptosis in endothelial cells and cardiomyocytes is ameliorated by nitrone spin traps and ebselen. Role of reactive oxygen and nitrogen species: S. Kotamraju, et al.; J. Biol. Chem. 275, 33585 (2000) Abstract; Full Text
The power and potential of doxorubicin-DNA adducts: S.M. Cutts, et al.; IUBMB Life 57, 73 (2005), Review Abstract
Adriamycin-induced interference with cardiac mitochondrial calcium homeostasis: K.B. Wallace; Cardiovasc. Toxicol. 7, 101 (2007), Review Abstract
Doxorubicin-induced cardiomyopathy from the cardiotoxic mechanisms to managemen: G. Takemura & H. Fujiwara; Prog. Cardiovasc. Dis. 49, 330 (2007), Review Abstract
Further Categories Containing This Product:
Other Toxins • Antibiotics - Immunomodulators • Antitumor Agents (Apoptosis Inducers) • Antitumor Agents (Enzyme Inhibitors) • Antibiotics - Topoisomerase Inhibitors • Antibiotics - Apoptosis Inducers & Inhibitors • DNA Intercalators & Crosslinkers • Antitumor Agents (DNA Interaction & Gene Regulation)
 
 
ALX-380-043 Revised 03-Apr-08
Daunorubicin . hydrochloride
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SYNONYMS Daunomycin . HCl
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antitumor Antibiotics
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ALX-380-043-M010   10 mg 95.00 USD Add To Cart
Product Specification
FORMULA: C27H29NO10 . HCl
MW: 527.5 . 36.5
CAS NUMBER: 23541-50-6
MERCK INDEX: 14: 2832
SOURCE/HOST: Isolated from Streptomyces spec.
PURITY: ≥98% (HPLC)
APPEARANCE: Orange to red solid.
SOLUBILITY: Soluble in water or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: TOXIC.

Product Description

Anthracycline anticancer antibiotic. Induces DNA damage by intercalating into DNA and inhibiting topoisomerase I and II. Inhibits RNA and DNA synthesis. Induces DNA single strand breaks and apoptosis in tumor cells.
Product Specific Literature References
Ceramide synthase mediates daunorubicin-induced apoptosis: an alternative mechanism for generating death signals: R. Bose, et al.; Cell 82, 405 (1995) Abstract
Daunorubicin activates NFkappaB and induces kappaB-dependent gene expression in HL-60 promyelocytic and Jurkat T lymphoma cells: M.P. Boland, et al.; J. Biol. Chem. 272, 12952 (1997) Abstract; Full Text
Alteration of the daunorubicin-triggered sphingomyelin-ceramide pathway and apoptosis in MDR cells: influence of drug transport abnormalities: M.G. Come, et al.; Int. J. Cancer 81, 580 (1999) Abstract
A critical evaluation of the mechanisms of action proposed for the antitumor effects of the anthracycline antibiotics adriamycin and daunorubicin: D.A. Gewirtz; Biochem. Pharmacol. 57, 727 (1999) Abstract
Altered multidrug resistance phenotype caused by anthracycline analogues and cytosine arabinoside in myeloid leukemia: X.F. Hu, et al.; Blood 93, 4086 (1999) Abstract
Implication of radical oxygen species in ceramide generation, c-Jun N- terminal kinase activation and apoptosis induced by daunorubicin: V. Mansat-de Mas, et al.; Mol. Pharmacol. 56, 867 (1999) Abstract
The phosphoinositide 3-kinase/Akt pathway is activated by daunorubicin in human acute myeloid leukemia cell lines: I. Plo, et al.; FEBS Lett 452, 150 (1999) Abstract
Caspase-3-like activity is necessary but not sufficient for daunorubicin-induced apoptosis in Jurkat human lymphoblastic leukemia cells: K.J. Turnbull, et al.; Leukemia 13, 1056 (1999) Abstract
Regulation of phospholipase D activity and ceramide production in daunorubicin-induced apoptosis in A-431 cells: J. Chen, et al.; Biochim. Biophys. Acta. 1488, 219 (2000) Abstract
Signaling pathways activated by daunorubicin:: G. Laurent & J. P. Jaffrezou; Blood 98, 913 (2001), Review Abstract
Further Categories Containing This Product:
Antibiotics - Immunomodulators • Antitumor Agents (Apoptosis Inducers) • Antitumor Agents (Enzyme Inhibitors) • Antibiotics - Topoisomerase Inhibitors • Antibiotics - Apoptosis Inducers & Inhibitors • DNA Intercalators & Crosslinkers • Antitumor Agents (DNA Interaction & Gene Regulation)
 
 
ALX-380-064 Revised 08-Oct-08
WP631 . dihydrochloride
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Other Antibiotics - DNA Regulation / Transcription
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-380-064-C100   100 µg 60.00 USD Add To Cart
ALX-380-064-M001   1 mg 240.00 USD Add To Cart
Product Specification
FORMULA: C62H64O20N2 . 2HCl
MW: 1157.2 . 73.0
PURITY: ≥95%
APPEARANCE: Off-white to red powder.
SOLUBILITY: Soluble in DMSO or dimethyl formamide.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Dissolve the compound in DMSO or dimethyl formamide at 20mg/ml, then add water (or 5% dextrose, PBS, etc.) to bring it to a final concentration of 1mg/ml (5% DMSO or dimethyl formamide).
HANDLING: Keep cool and dry.
HAZARD: HARMFUL. MAY BE CARCINOGENIC.

Product Description
Synthetic fluorescent bisintercalating anthracycline antibiotic with ultratight binding properties to DNA. Inhibits Sp1-initiated transcription at nanomolar concentrations. Appears to overcome MRP-mediated multidrug resistance. Induces apoptosis. Licenced product covered by US Patent 5,874,412. Sold with permission of Houston Pharmaceuticals, Inc.
Product Specific Literature References
Structure-based design of a new bisintercalating anthracycline antibiotic: J.B. Chaires, et al.; J. Med. Chem. 40, 261 (1997) Abstract
Structure of a DNA-bisdaunomycin complex: G.G. Hu, et al.; Biochemistry 36, 5940 (1997) Abstract
Bisanthracycline WP631 inhibits basal and Sp1-activated transcription initiation in vitro: B. Martin, et al.; Nucl. Acids Res. 27, 3402 (1999) Abstract; Full Text
Analysis of the effects of Daunorubicin and WP631 on transcription: J. Portugal, et al.; Curr. Med. Chem. 8, 1 (2001), (Review) Abstract
Identification of a critical Sp1 site within the endoglin promoter and its involvement in the transforming growth factor-beta stimulation: L.M. Botella, et al.; J. Biol. Chem. 276, 34486 (2001) Abstract; Full Text
Exploiting anthracycline scaffold for designing DNA-targeting agents: W. Priebe; Methods Enzymol. 340, 529 (2001) Abstract
Induction of G(2)/M arrest and inhibition of c-myc and p53 transcription by WP631 in Jurkat T lymphocytes: S. Villamarin, et al.; Biochem. Pharmacol. 63, 1251 (2002) Abstract
Evidence that activation of nuclear factor-kappaB is essential for the cytotoxic effects of doxorubicin and its analogues: K. Ashikawa, et al.; Biochem. Pharmacol. 67, 353 (2004) Abstract
Bis-anthracycline antibiotics inhibit human immunodeficiency virus type 1 transcription: O. Kutsch, et al.; Antimicrob. Agents. Chemother. 48, 1652 (2004) Abstract
Circumvention of the multidrug-resistance protein (MRP-1) by an antitumor drug through specific inhibition of gene transcription in breast tumor cells: S. Mansilla, et al.; Biochem. Pharmacol. 73, 934 (2007) Abstract
Further Categories Containing This Product:
MDR Inhibitors • Antibiotics - Apoptosis Inducers & Inhibitors • Sp Protein Family / Related Products • DNA Intercalators & Crosslinkers
 
 
ALX-380-074 Revised 12-Oct-07
WP631 . dimethanesulfonate
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Other Antibiotics - DNA Regulation / Transcription
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ALX-380-074-C500   500 µg 150.00 USD Add To Cart
Product Specification
FORMULA: C62H64N2O20 . 2CH3SO3
MW: 1157.2 . 191.2
PURITY: ≥95%
APPEARANCE: Red powder.
SOLUBILITY: Soluble in DMSO (10mg/ml) or water (1mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HAZARD: HARMFUL. MAY BE CARCINOGENIC.

Product Description
Synthetic fluorescent bisintercalating anthracycline antibiotic with ultratight binding properties to DNA. Inhibits Sp1-initiated transcription at nanomolar concentrations. Appears to overcome multidrug resistance protein (MRP) mediated multidrug resistance (MDR). More water soluble than WP631 . dihydrochloride (Prod. No. ALX-380-064). Licenced product covered by US Patent 5,874,412. Sold with permission of Houston Pharmaceuticals, Inc.
Product Specific Literature References
Structure-based design of a new bisintercalating anthracycline antibiotic: J.B. Chaires, et al.; J. Med. Chem. 40, 261 (1997) Abstract
Structure of a DNA-bisdaunomycin complex: G.G. Hu, et al.; Biochemistry 36, 5940 (1997) Abstract
Binding of two novel bisdaunorubicins to DNA studied by NMR spectroscopy: H. Robinson, et al.; Biochemistry 36, 8663 (1997) Abstract
Ultratight DNA binding of a new bisintercalating anthracycline antibiotic: F. Leng, et al.; Biochemistry 37, 1743 (1998) Abstract
Drug-DNA interactions: J.B. Chaires; Curr. Opin. Struct. Biol. 8, 314 (1998) Abstract
Bisanthracycline WP631 inhibits basal and Sp1-activated transcription initiation in vitro: B. Martin, et al.; Nucleic Acids Res. 27, 3402 (1999) Abstract
Analysis of the effects of daunorubicin and WP631 on transcription: J. Portugal, et al.; Curr. Med. Chem. 8, 1 (2001) Abstract
Inhibition of basal and transforming growth factor-beta-induced stimulation of COL1A1 transcription by the DNA intercalators, mitoxantrone and WP631, in cultured human dermal fibroblasts: S. Gaidarova and S.A. Jimenez; J. Biol. Chem. 277, 38737 (2002) Abstract
Sequence selective binding of bis-daunorubicin WP631 to DNA: K.R. Fox, et al.; Eur. J. Biochem. 271, 3556 (2004) Abstract
Further Categories Containing This Product:
DNA Intercalators & Crosslinkers • MDR Inhibitors • Sp Protein Family / Related Products • Antibiotics - Apoptosis Inducers & Inhibitors
 
 
ALX-380-119 Revised 21-May-08
Becatecarin
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SYNONYMS 6-N-[2-(Diethylamino)ethyl]rebeccamycin
NSC 655649
BMY-27557-14
BMS-181176
XL 119
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antitumor Antibiotics
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ALX-380-119-C250   250 µg 155.00 USD Add To Cart
ALX-380-119-M001   1 mg 465.00 USD Add To Cart
Product Specification
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FORMULA: C33H34Cl2N4O7
MW: 669.6
CAS NUMBER: 119673-08-4
PURITY: ≥98% (HPLC)
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in water (pH-dependent) or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C