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Antibiotics - DNA Regulation / Transcription
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ALX-380-023 Revised 19-Oct-07
Mitomycin C
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - DNA Replication Inhibitors
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ALX-380-023-M005   5 mg 98.00 USD Add To Cart
ALX-380-023-M010   10 mg 185.00 USD Add To Cart
Product Specification
FORMULA: C15H18N4O5
MW: 334.3
CAS NUMBER: 50-07-7
MERCK INDEX: 14: 6215
RTECS: CN0700000
SOURCE/HOST: Isolated from Streptomyces caespitosus.
PURITY: ≥98%
APPEARANCE: Blue-violet crystals.
SOLUBILITY: Soluble in water or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.
HAZARD: TOXIC. MAY BE CARCINOGENIC.

Product Description
Antitumor antibiotic. Inhibitor of DNA synthesis, nuclear division and cancer cells. DNA intercalating agent. Apoptosis inducer.
Product Specific Literature References
Mitomycin, a new antibiotic from Streptomyces. I: T. Hata, et al.; J. Antibiot. (Tokyo) 9, 141 (1956) Abstract
S.K. Carter & S.T. Crooke ; 'Mitomycin C. Current Status and New Developments', Academic Press, New York (1979)
Revised absolute configuration of mitomycin C. X-ray analysis of 1-N-(p-bromobenzoyl)mitomycin C: K. Shirahata & N. Hirayama; JACS 105, 7199 (1983)
Sequence-specific DNA damage induced by reduced mitomycin C and 7-N-(p- hydroxyphenyl)mitomycin C: K. Ueda and T. Komano; Nucl. Acids Res. 12, 6673 (1984) Abstract
Isolation and structure of a covalent cross-link adduct between mitomycin C and DNA: M. Tomasz, et al.; Science 235, 1204 (1987) Abstract
The chemistry of DNA modification by antitumor antibiotics: J.F. Fisher & P.A. Aristoff; Prog. Drug Res. 32, 411 (1988) Abstract
DNA sequence specificity of mitomycin cross-linking: S.P. Teng, et al.; Biochemistry 28, 3901 (1989) Abstract
Polyoxyethylene-modified superoxide dismutase reduces side effects of adriamycin and mitomycin C: S. Kawasaki, et al.; J. Cancer Res. 83, 899 (1992) Abstract
Genetic evidence for an activator required for induction of pectin lyase in Erwinia carotovora subsp. carotovora by DNA-damaging agents: J.L. McEvoy, et al.; J. Bacteriol. 174, 5471 (1992) Abstract
Elevated DT-diaphorase activity and messenger RNA content in human non- small cell lung carcinoma: relationship to the response of lung tumor xenografts to mitomycin Cl: A.M. Malkinson, et al.; Cancer Res. 52, 4752 (1992) Abstract
Mitomycins: J. Verweij, et al.; Cancer Chemother. Biol. Response Modif. 18, 46 (1999) Abstract
Mitomycin C induces apoptosis in a caspases-dependent and Fas/CD95- independent manner in human gastric adenocarcinoma cells: I.C. Park, et al.; Cancer Lett. 158, 125 (2000) Abstract
Selective inhibition of cyclooxygenase-2 enhances mitomycin-C-induced apoptosis: C.T. Hsueh, et al.; Cancer Chemother. Pharmacol. 45, 389 (2000) Abstract
DNA-damaging agents cause inactivation of translational regulators linked to mTOR signalling: A.R. Tee & C.G. Proud; Oncogene 19, 3021 (2000) Abstract
Re-evaluation of tumor-specific cytotoxicity of mitomycin C, bleomycin and peplomycin: M. Sasaki, et al.; Anticancer Res. 26, 3373 (2006) Abstract
Activation of the S phase DNA damage checkpoint by mitomycin C: E. Mladenov, et al.; J. Cell. Physiol. 211, 468 (2007) Abstract
 
 
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
 
 
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
 
 
ALX-380-055 Revised 13-Jun-08
Chromomycin A3
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SYNONYMS Toyomycin
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Other Antibiotics - DNA Regulation / Transcription
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ALX-380-055-M005   5 mg 65.00 USD Add To Cart
ALX-380-055-M025   25 mg 260.00 USD Add To Cart
Product Specification
FORMULA: C57H82O26
MW: 1183.3
CAS NUMBER: 7059-24-7
MERCK INDEX: 14: 2238
RTECS: GB7875000
SOURCE/HOST: Isolated from Streptomyces griseus.
PURITY: ≥97% (HPLC)
APPEARANCE: Off white to yellow powder.
SOLUBILITY: Soluble in ethyl acetate.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.
HAZARD: VERY TOXIC.

Product Description
Antibiotic. Inhibits RNA synthesis. Cell permeable fluorescent dye that can be used with Bisbenzimide H33258 (Prod. No. ALX-620-051) to distinguish chromosomes by their total DNA concentration and their DNA base composition. Binds to G:C pairs of helical DNA but does not intercalate. Ex(max): 445nm; Em(max): 575nm.
General Literature References
K. Mizuno; J. Antibiot. 16, 22 (1963)
Further Categories Containing This Product:
Transcription Inhibitors / Related Products
 
 
ALX-380-060 Revised 11-Jul-08
Tetracycline . hydrochloride
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Other Antibiotics - DNA Regulation / Transcription
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ALX-380-060-G005   5 g 20.00 USD Add To Cart
Product Specification
FORMULA: C22H24N2O8 . HCl
MW: 444.5 . 36.5
CAS NUMBER: 64-75-5
MERCK INDEX: 14: 9196
RTECS: QI9100000
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in water, methanol or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light and moisture.
HAZARD: IRRITANT.

Product Description
Broad-spectrum antibiotic with anti-inflammatory activity. Blocks bacterial protein synthesis by inhibiting binding of aminoacyl tRNA to A-site of ribosomes. Tetracycline-controlled systems are used to control gene expression on transgenic mice. Marker of bone formation.
Product Specific Literature References
Clinical and laboratory observations of a new antibiotic, tetracycline: M. Finland, et al.; J. Am. Med. Assoc. 154, 561 (1954) Abstract
Tetracycline antibiotics: mode of action, applications, molecular biology, and epidemiology of bacterial resistance: I. Chopra & M. Roberts; Microbiol. Mol. Biol. Rev. 65, 232 (2001) Abstract
Tetracyclines: nonantibiotic properties and their clinical implications: A. N. Sapadin & R. Fleischmajer; J. Am. Acad. Dermatol. 54, 258 (2006) Abstract
A novel tetracycline labeling schedule for longitudinal evaluation of the short-term effects of anabolic therapy with a single iliac crest bone biopsy: early actions of teriparatide: R. Lindsay, et al.; J. Bone Miner. Res. 21, 366 (2006) Abstract
Tetracycline-controlled genetic switches: R. Sprengel & M. T. Hasan; Handb. Exp. Pharmacol. 178, 49 (2007) Abstract
Anti-inflammatory activity of tetracyclines: G. Webster & J. Q. Del Rosso; Dermatol. Clin. 25, 133 (2007) Abstract
 
 
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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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
 
 
ALX-380-065 Revised 24-Sep-08
Fostriecin
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SYNONYMS Phosphotrienin
CI-920
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Topoisomerase Inhibitors
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ALX-380-065-C010   10 µg 150.00 USD Add To Cart
Product Specification
FORMULA: C19H26O9PNa
MW: 452.4
CAS NUMBER: 87860-39-7
RTECS: UQ0600000
SOURCE/HOST: Isolated from Streptomyces pulveraceous subsp. fostreus.
PURITY: ≥98% (HPLC)
APPEARANCE: Colorless solid.
SOLUBILITY: Soluble in water (50mg/ml), methanol (10mg/ml) or 100% ethanol (10mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least 1 year when stored at -20°C. Use fresh solution.
HANDLING: Protect from light. Packaged under inert gas. Hygroscopic.

Product Description
Antitumor antibiotic. Catalytic inhibitor of topoisomerase II. Strong protein phosphatase 2A (PP2A) inhibitor (IC50=3.2nM). Weak inhibitor for PP1 (IC50=131µM). No apparent effect on PP2B. The binding site for fostriecin on PP2A is different from that of okadaic acid (see Prod. No. ALX-350-003).
Product Specific Literature References
Novel antitumor agents CI-920, PD 113,270 and PD 113,271. II. Isolation and characterization: S.S. Stampwala, et al.; J. Antibiot. (Tokyo) 36, 1601 (1983) Abstract
Novel antitumor agents CI-920, PD 113,270 and PD 113,271. I. Taxonomy, fermentation and biological properties: J.B. Tunac, et al.; J. Antibiot. (Tokyo) 36, 1595 (1983) Abstract
Studies on the biochemical mechanism of the novel antitumor agent, CI- 920: D.W. Fry, et al.; Cancer Chemother. Pharmacol. 13, 171 (1984) Abstract
Anticancer activity of the structurally novel antibiotic Cl-920 and its analogues: W.R. Leopold, et al.; Cancer Res. 44, 1928 (1984) Abstract
Inhibition of type II topoisomerase by fostriecin: T.J. Boritzki, et al.; Biochem. Pharmacol. 37, 4063 (1988) Abstract
Comparison of effects of fostriecin, novobiocin, and camptothecin, inhibitors of DNA topoisomerases, on DNA replication and repair in human cells: C.M. Gedik & A.R. Collins; Nucl. Acids Res. 18, 1007 (1990) Abstract
The cell cycle related differences in susceptibility of HL-60 cells to apoptosis induced by various antitumor agents: W. Gorczyca, et al.; Cancer Res. 53, 3186 (1993) Abstract
Induction of DNA strand breaks associated with apoptosis during treatment of leukemias: W. Gorczyca, et al.; Leukemia 7, 659 (1993) Abstract
Antitumor drug fostriecin inhibits the mitotic entry checkpoint and protein phosphatases 1 and 2A: M. Roberge, et al.; Cancer Res. 54, 6115 (1994) Abstract
Fostriecin: a review of the preclinical data: R.S. de Jong, et al.; Anticancer Drugs 8, 413 (1997) Abstract
Fostriecin, an antitumor antibiotic with inhibitory activity against serine/threonine protein phosphatases types 1 (PP1) and 2A (PP2A), is highly selective for PP2A: A.H. Walsh, et al.; FEBS Lett. 416, 230 (1997) Abstract
Fostriecin, an inhibitor of protein phosphatase 2A, limits myocardial infarct size even when administered after onset of ischemia: C. Weinbrenner, et al.; Circulation 98, 899 (1998) Abstract
Phase I and pharmacokinetic study of the topoisomerase II catalytic inhibitor fostriecin: R.S. de Jong, et al.; Br. J. Cancer 79, 882 (1999) Abstract
Fostriecin: chemistry and biology: D.S. Lewy, et al.; Curr. Med. Chem. 9, 2005 (2002) Abstract
 
 
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: