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ALX-420-039 Revised 14-Aug-08
Imiquimod
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SYNONYMS 1-(2-Methylpropyl)-1H-imidazo[4,5-c]quinolin-4-amine
R-837
PRODUCT LINE Inflammation
PRODUCT CATEGORY TLR Agonists Other Products
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ALX-420-039-M100   100 mg 55.00 USD Add To Cart
ALX-420-039-M250   250 mg 120.00 USD Add To Cart
Product Specification
FORMULA: C14H16N4
MW: 240.3
CAS NUMBER: 99011-02-6
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO (3mg/ml) or dimethyl formamide; slightly soluble in water (warm to 37°C, vortex); insoluble in 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for up to 1 year after receipt when stored at -20°C. Stock solutions are stable for up to 3 months when stored at -20°C.
HANDLING: After reconstitution, prepare aliquots and store at -20°C.

Product Description
Topical immune response modifier that inhibits angiogenesis. Up-regulates IL-18 and down-regulates MMP-9 through recognition of Toll-like receptor 7 (TLR7) and subsequent activation of MyD88-dependent pathway.
Product Specific Literature References
Imiquimod applied topically: a novel immune response modifier and new class of drug: R.L. Miller, et al.; Int. J. Immunopharmacol. 21, 1 (1999) Abstract
Small anti-viral compounds activate immune cells via the TLR7 MyD88-dependent signaling pathway: H. Hemmi, et al.; Nat. Immunol. 3, 196 (2002) Abstract
In vivo and in situ modulation of the expression of genes involved in metastasis and angiogenesis in a patient treated with topical imiquimod for melanoma skin metastases: C. Hesling, et al.; Br. J. Dermatol. 150, 761 (2004) Abstract
Imiquimod as an antiangiogenic agent: V.W. Li, et al.; J. Drugs Dermatol. 4, 708 (2005) Abstract
Imiquimod is a strong inhibitor of tumor cell-induced angiogenesis: S. Majewski, et al.; Int. J. Dermatol. 44, 14 (2005) Abstract
General Information
BACKGROUND/TECHNICAL INFORMATION Stimulation of TLR7 can be achieved with 1-10µg/ml of the compound for 6 to 24 hours.

Related Products:
- ddWater (endotoxin-free) (Prod. No. ALX-505-008)
- PBS (endotoxin-free) (Prod. No. ALX-505-007)
 
 
ALX-350-302 Revised 14-Dec-07
Imperatorin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Apoptosis Inducers & Inhibitors
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ALX-350-302-M002   2 mg 70.00 USD Add To Cart
Product Specification
FORMULA: C16H14O4
MW: 270.3
PURITY: ≥99% (HPLC)
APPEARANCE: White to off-white crystalline solid.
SOLUBILITY: Soluble in DMSO or dimethyl formamide; slightly soluble in methanol or water. Almonst insoluble in 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
The furanocoumarins heraclenin (Prod. No. ALX-350-303) and imperatorin (Prod. No. ALX-350-302) inhibit T cell-receptor-mediated proliferation in human primary T cells in a concentration-dependent manner. Both compounds also induce apoptosis. While imperatorin induces DNA fragmentation at the G1/S phase of the cell cycle, heraclenin induces DNA fragmentation at the G2/M phases of the cell cycle, thus despite a close structural similarity they induce apoptosis in mechanistically different ways. Imperatorin inhibits HIV-1 replication as well as the expression of ICAM-1 in U937 foam cells. Inhibits voltage-dependent calcium channel.
Product Specific Literature References
Expression of intercellular adhesion molecule-1 in U937 foam cells and inhibitory effect of imperatorin: P.Y. Yang, et al.; Acta Pharmacol. Sin. 23, 327 (2002) Abstract
Imperatorin, a furanocoumarin from Angelica dahurica (Umbelliferae), induces cytochrome c-dependent apoptosis in human promyelocytic leukaemia, HL-60 Cells: H.O. Pae, et al.; Pharmacol. Toxicol. 91, 40 (2002) Abstract
Coumarins from Opopanax chironium. New dihydrofuranocoumarins and differential induction of apoptosis by imperatorin and heraclenin: G. Appendino, et al.; J. Nat. Prod. 67, 532 (2004) Abstract
Imperatorin inhibits T-cell proliferation by targeting the transcription factor NFAT: N. Marquez, et al.; Planta Med. 70, 1016 (2004) Abstract
Imperatorin inhibits HIV-1 replication through an Sp1-dependent pathway: R. Sancho, et al.; J. Biol. Chem. 279, 37349 (2004) Abstract; Full Text
Imperatorin induces vasodilatation possibly via inhibiting voltage dependent calcium channel and receptor-mediated Ca2+ influx and release: J.Y. He, et al.; Eur. J. Pharmacol. 573, 170 (2007) Abstract
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ALX-270-278 Revised 01-Jul-08
5-Iodo-6-amino-1,2-benzopyrone
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SYNONYMS INH2BP
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY PARP Inhibitors
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ALX-270-278-M001   1 mg 25.00 USD Add To Cart
ALX-270-278-M005   5 mg 50.00 USD Add To Cart
Product Specification
FORMULA: C9H6INO2
MW: 287.1
CAS NUMBER: 137881-27-7
PURITY: ≥98%
APPEARANCE: Off-white to yellow solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light. Packaged under inert gas.

Product Description
Inhibitor of poly(ADP-ribose) polymerase-1 (PARP-1).
Product Specific Literature References
Reversion of malignant phenotype by 5-iodo-6-amino-1,2-benzopyrone a non-covalently binding ligand of poly(ADP-ribose) polymerase: P.I. Bauer, et al.; Biochimie 77, 374 (1995) Abstract
Protective effects of 5-iodo-6-amino-1,2-benzopyrone, an inhibitor of poly(ADP-ribose) synthetase against peroxynitrite-induced glial damage and stroke development: M. Endres, et al.; Eur. J. Pharmacol. 351, 377 (1998) Abstract
Poly(ADP-ribose) synthetase activation mediates increased permeability induced by peroxynitrite in Caco-2BBe cells: M. Kennedy, et al.; Gastroenterology 114, 510 (1998) Abstract
Potential role of the peroxynitrate-poly(ADP-ribose) synthetase pathway in a rat model of severe hemorrhagic shock: C. Szabó, et al.; Shock 9, 341 (1998) Abstract
Protection against peroxynitrite-induced fibroblast injury and arthritis development by inhibition of poly(ADP-ribose) synthase: C. Szabó, et al.; PNAS 95, 3867 (1998) Abstract; Full Text
Crucial role of apopain in the peroxynitrite-induced apoptotic DNA fragmentation: L. Virág, et al.; Free Radic. Biol. Med. 25, 1075 (1998) Abstract
Poly(ADP-ribose) synthetase activation mediates mitochondrial injury during oxidant-induced cell death: L. Virág, et al.; J. Immunol. 161, 3753 (1998) Abstract; Full Text
Novel roles of nitric oxide in hemorrhagic shock: C. Szabo & T.R. Billiar; Shock 12, 1 (1999) Abstract
Cancer cell selectivity of 5-iodo-6-aminobenzopyrone (INH2BP) and methyl-3,5-diiodo-4(4'-methoxyphenoxy) benzoate (DIME): E. Kirsten & E. Kun; Int. J. Mol. Med. 5, 279 (2000) Abstract
Role of poly(ADP-ribose) synthetase activation in the development of experimental allergic encephalomyelitis: G.S. Scott, et al.; J. Neuroimmunol. 117, 78 (2001) Abstract
Inhibition of poly (ADP-ribose) synthetase by gene disruption or inhibition with 5-iodo-6-amino-1,2-benzopyrone protects mice from multiple-low-dose-streptozotocin-induced diabetes: J.G. Mabley, et al.; Br. J. Pharmacol. 133, 909 (2001) Abstract
Further Categories Containing This Product:
DNA Repair Other Products
 
 
ALX-480-098 Revised 14-Dec-07
5-Iodocytidine
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Cytidine Derivatives Other Products
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ALX-480-098-M005   5 mg 70.00 USD Add To Cart
ALX-480-098-M025   25 mg 280.00 USD Add To Cart
Product Specification
FORMULA: C9H12IN3O5
MW: 369.1
CAS NUMBER: 1147-23-5
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white crystalline solid.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
IDENTITY: Determined by MS and UV.

Product Description
Key tool for research in the field of nucleic acids and nucleic acid-protein interactions. Has been used in structural elucidation of mispairs with natural bases to explain their mutagenic properties; in the study of cytosine methyltransferases; for photo-crosslinking of nucleoprotein complexes; in X-ray diffraction experiments of nucleic acids and nucleic acid binding proteins; as nonradioactive label and as alternative for mixed probes; for triple-helix stabilization; as antisense oligonucleotide; and in the study of the restriction endonucleases cleavage mechanism.
Product Specific Literature References
Complex of aspartate carbamoyltransferase from Escherichia coli with its allosteric inhibitor, cytidine triphosphate: electron density at 5.9-angstroms resolution: B.F. Edwards, et al.; PNAS 71, 4437 (1974) Abstract; Full Text
Properties of phenylalanine transfer ribonucleic acid with modified 3’-terminal end in protein biosynthesis using a rabbit reticulocyte cell-free system: effect of the replacement of cytidine residues from the CpCpA end of tRNA by 5-iodocytidine or : E.K. Baksht, et al.; Nucl. Acids Res. 4, 2205 (1977) Abstract; Full Text
Photocrosslinking of 5-iodouracil-substituted RNA and DNA to proteins: M.C. Willis, et al.; Science 262, 1255 (1993) Abstract
High yield photocrosslinking of a 5-iodocytidine (IC) substituted RNA to its associated protein: K.M. Meisenheimer, et al.; Nucl. Acids Res. 24, 981 (1996) Abstract; Full Text
Preparation and properties of oligodeoxynucleotides containing 5-iodouracil and 5-bromo- and 5-iodocytosine: E. Ferrer, et al.; Bioconjug. Chem. 8, 757 (1997) Abstract
 
 
ALX-430-139 Revised 20-Feb-08
Irinotecan . hydrochloride . trihydrate
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SYNONYMS Camptosar
7-ethyl-10-hydroxycamptothecin
CPT-11
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Topoisomerase Inhibitors
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ALX-430-139-M005   5 mg 90.00 USD Add To Cart
ALX-430-139-M025   25 mg 315.00 USD Add To Cart
Product Specification
FORMULA: C33H38N4O6 . HCl . 3H2O
MW: 586.7 . 36.4 . 54.0
CAS NUMBER: 100286-90-6; 136572-09-3
MERCK INDEX: 14: 5091
PURITY: ≥98% (HPLC)
APPEARANCE: Pale yellow powder.
SOLUBILITY: Slightly soluble in methanol or water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
A member of the camptothecin drug family, and an inhibitor of the nuclear enzyme topoisomerase I, which is involved in cellular DNA replication and transcription. During replication topoisomerase I mediates the relaxation of super coiled DNA, and its inhibition results in breakage of the DNA chain and likely induce apoptosis. Irinotecan is, therefore, an attractive target for anticancer drug development. Currently it is used for the treatment of small cell lung cancer and advanced colorectal cancer.
Product Specific Literature References
Induction of tumor necrosis factor by a camptothecin derivative, irinotecan, in mice and human mononuclear cells: S. Goto, et al.; Anticancer Res. 16, 2507 (1996) Abstract
The role of irinotecan in colorectal cancer: L.B. Saltz; Curr. Oncol. Rep. 1, 155 (1999) Abstract
Therapeutic advances in small cell lung cancer: F.P. Worden and G.P. Kalemkerian; Expert Opin. Investig. Drugs 9, 565 (2000) Abstract
Human DNA-Topoisomerases - Diagnostic and Therapeutic Implications for Cancer: U. Kellner, et al.; Onkologie 23, 424 (2000) Abstract
Irinotecan activates p53 with its active metabolite, resulting in human hepatocellular carcinoma apoptosis: Y. Takeba, et al.; J. Pharmacol. Sci. 104, 232 (2007) Abstract
Further Categories Containing This Product:
Antitumor Agents (Enzyme Inhibitors)Natural Products - Antitumor Reagents
 
 
ALX-350-145 Revised 28-Mar-07
Isobavachalcone
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SYNONYMS 2’,4’,4-Trihydroxy-3’-[3’’-methylbut-3’’-enyl]chalcone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antitumor Reagents
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ALX-350-145-M001   1 mg 190.00 USD Add To Cart
Product Specification
FORMULA: C20H20O4
MW: 324.4
CAS NUMBER: 20784-50-3
SOURCE/HOST: Isolated from plant Psoralea corylifolia.
PURITY: ≥97% (HPLC)
APPEARANCE: Yellow oil.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
IDENTITY: Determined by 1H-NMR, 13C-NMR and MS.

Product Description
Inhibits platelet aggregation. Inhibitor of Epstein-Barr virus early antigen (EBV-EA) induction. Exhibits potent inhibitory effect on skin tumor promotion. Potent inhibitor of MMP-2. Displays DNA strand-scission (cleaving) activity. Shows antifungal activity.
Product Specific Literature References
Antiplatelet flavonoids from seeds of Psoralea corylifolia: W.J. Tsai, et al.; J. Nat. Prod. 59, 671 (1996) Abstract
Antioxidative components of Psoralea corylifolia (Leguminosae): H. Haraguchi, et al.; Phytother. Res. 16, 539 (2002) Abstract
Chalcones, coumarins, and flavanones from the exudate of Angelica keiskei and their chemopreventive effects: T. Akihisa, et al.; Cancer Lett. 201, 133 (2003) Abstract
Antitrichomonal and antioxidant activities of Dorstenia barteri and Dorstenia convexa: N.O. Omisore, et al.; Braz. J. Med. Biol. Res. 38, 1087 (2005) Abstract
Chalcones and other compounds from the exudates of Angelica keiskei and their cancer chemopreventive effects: T. Akihisa, et al.; J. Nat. Prod. 69, 38 (2006) Abstract
Inhibition of matrix metalloproteinase-2 secretion by chalcones from the twigs of Dorstenia barteri Bureau.: B. Ngameni, et al.; Arkivoc ix, 91 (2007) Full Text
 
 
ALX-385-025 Revised 07-Apr-08
8-Isopentenylnaringenin
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SYNONYMS 8-Prenylnaringenin
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Flavanones
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ALX-385-025-M005   5 mg 155.00 USD Add To Cart
Product Specification
FORMULA: C20H20O5
MW: 340.4
SOURCE/HOST: Isolated from hops (Humulus lupulus L.).
PURITY: ≥97% (HPLC)
APPEARANCE: Light yellow powder
SOLUBILITY: Soluble in methanol or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Prenyl flavonoid. Phytoestrogen. Selective, non-steroidal estrogen receptor α (ERα) ligand. Potent inhibitor of angiogenesis in vitro and in vivo. Chemopreventive agent against cancer induced by heterocyclic amines.
Product Specific Literature References
Prenylflavonoids: a new class of non-steroidal phytoestrogen (Part 1). Isolation of 8-isopentenylnaringenin and an initial study on its structure-activity relationship: M. Kitaoka, et al.; Planta Med. 64, 511 (1998) Abstract
Prenylflavonoids: a new class of non-steroidal phytoestrogen (Part 2). Estrogenic effects of 8-isopentenylnaringenin on bone metabolism: M. Miyamoto, et al.; Planta Med. 64, 516 (1998) Abstract
Identification of a potent phytoestrogen in hops (Humulus lupulus L.) and beer: S.R. Milligan, et al.; J. Clin. Endocrinol. Metab. 84, 2249 (1999) Abstract
Prenylflavonoids from hops inhibit the metabolic activation of the carcinogenic heterocyclic amine 2-amino-3-methylimidazo[4, 5-f]quinoline, mediated by cDNA-expressed human CYP1A2: C.L. Miranda, et al.; Drug Metab. Dispos. 28, 1297 (2000) Abstract; Full Text
The endocrine activities of 8-prenylnaringenin and related hop (Humulus lupulus L.) flavonoids: S.R. Milligan, et al.; J. Clin. Endocrinol. Metab. 85, 4912 (2000) Abstract; Full Text
8-prenylnaringenin, a novel phytoestrogen, inhibits angiogenesis in vitro and in vivo: M.S. Pepper, et al.; J. Cell Physiol. 199, 98 (2004) Abstract
Xanthohumol and related prenylflavonoids from hops and beer: to your good health!: J.F. Stevens & J.E. Page; Phytochemistry 65, 1317 (2004), (Review) Abstract
Rapid yeast estrogen bioassays stably expressing human estrogen receptors alpha and beta, and green fluorescent protein: a comparison of different compounds with both receptor types: T.F. Bovee, et al.; J. Steroid Biochem. Mol. Biol. 91, 99 (2004) Abstract
8-Prenylnaringenin, inhibits estrogen receptor-alpha mediated cell growth and induces apoptosis in MCF-7 breast cancer cells: E. Brunelli, et al.; J. Steroid Biochem. Mol. Biol. 107, 140 (2007) Abstract
 
 
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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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-350-279 Revised 02-Jun-08
Isoxanthohumol
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Other Natural Products - DNA Regulation / Transcription
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ALX-350-279-M001   1 mg 60.00 USD