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Kinases / Related Products
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ALX-380-110 Revised 03-Apr-08
17-DMAG
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SYNONYMS 17-[2-(Dimethylamino)ethyl]amino-17-desmethoxygeldanamycin
NSC 707545
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics for Angiogenesis Research
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-380-110-C100   100 µg 50.00 USD Add To Cart
ALX-380-110-M001   1 mg 150.00 USD Add To Cart
Product Specification
FORMULA: C32H48N4O8
MW: 616.8
CAS NUMBER: 150270-08-9
SOURCE/HOST: Semisynthetic from geldanamycin (Prod. No. ALX-380-054).
PURITY: ≥99%
APPEARANCE: Purple to black powder.
SOLUBILITY: Soluble in water, 100% ethanol (10mg/ml) or DMSO (>25mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description

Less toxic, more potent synthetic derivative of geldanamycin. Inhibitor of angiogenesis. Inhibitor of heat shock protein 90 (HSP90). Inducer of apoptosis with higher antitumor activity than 17-AAG (Prod. No. ALX-380-091).

Product Specific Literature References
Pharmacokinetics, tissue distribution, and metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin (NSC 707545) in CD2F1 mice and Fischer 344 rats: M.J. Egorin, et al.; Cancer Chemother. Pharmacol. 49, 7 (2002) Abstract
Biliary excretion of 17-(allylamino)-17-demethoxygeldanamycin (NSC 330507) and metabolites by Fischer 344 rats: S.M. Musser, et al.; Cancer Chemother. Pharmacol. 52, 139 (2003) Abstract
Crystal structure and molecular modeling of 17-DMAG in complex with human Hsp90: J.M. Jez, et al.; Chem. Biol. 10, 361 (2003) Abstract
Synthesis and biological activities of novel 17-aminogeldanamycin derivatives: Z.Q. Tian, et al.; Bioorg. Med. Chem. 12, 5317 (2004) Abstract
Antiangiogenic properties of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin: an orally bioavailable heat shock protein 90 modulator: G. Kaur, et al.; Clin. Cancer Res. 10, 4813 (2004) Abstract
Enhanced tumor cell radiosensitivity and abrogation of G2 and S phase arrest by the Hsp90 inhibitor 17-(Dimethylaminoethylamino)-17-demethoxygeldanamycin: E.E. Bull, et al.; Clin. Cancer Res. 10, 8077 (2004) Abstract
ErbB3 expression predicts tumor cell radiosensitization induced by Hsp90 inhibition: H. Dote, et al.; Cancer Res. 65, 6967 (2005) Abstract
In vivo antitumor efficacy of 17-DMAG (17-dimethylaminoethylamino-17-demethoxygeldanamycin hydrochloride), a water-soluble geldanamycin derivative: M. Hollingshead, et al.; Cancer Chemother. Pharmacol. 56, 115 (2005) Abstract
Comparison of 17-dimethylaminoethylamino-17-demethoxy-geldanamycin (17DMAG) and 17-allylamino-17-demethoxygeldanamycin (17AAG) in vitro: effects on Hsp90 and client proteins in melanoma models: V. Smith, et al.; Cancer Chemother. Pharmacol. 56, 126 (2005) Abstract
Preclinical toxicity of a geldanamycin analog, 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin (17-DMAG), in rats and dogs: potential clinical relevance: E.R. Glaze, et al.; Cancer Chemother. Pharmacol. 56, 637 (2005) Abstract
17-Allyamino-17-demethoxygeldanamycin and 17-NN-dimethyl ethylene diamine-geldanamycin have cytotoxic activity against multiple gynecologic cancer cell types: D.R. Gossett, et al.; Gynecol. Oncol. 96, 381 (2005) Abstract
Structure-based design of 7-carbamate analogs of geldanamycin: G. Rastelli, et al.; Biooorg. Med. Chem. Lett. 15, 5016 (2005) Abstract
Generation of a novel anti-geldanamycin antibody: E. Barzilay, et al.; BBRC 330, 561 (2005) Abstract
Determination of the heat shock protein 90 inhibitor 17-dimethylaminoethylamino-17-demethoxygeldanamycin in plasma by liquid chromatography-electrospray mass spectrometry: K. Hwang, et al.; J. Chromatogr. B Analyt. Technol. Biomed. Life Sci. 830, 35 (2006) Abstract
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ALX-270-097 Revised 07-Sep-06
Ebselen
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SYNONYMS 2-Phenyl-1,2-benzisoselenazol-3-(2H)-one
PRODUCT LINE Oxidative Stress
PRODUCT CATEGORY Peroxynitrite / Scavengers / Detection
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-097-M001   1 mg 12.00 USD Add To Cart
ALX-270-097-M005   5 mg 20.00 USD Add To Cart
ALX-270-097-M025   25 mg 60.00 USD Add To Cart
Product Specification
FORMULA: C13H9NOSe
MW: 274.2
CAS NUMBER: 60940-34-3
PURITY: ≥98% (NMR)
APPEARANCE: White to off-white crystalline solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Selenium-based inhibitor of protein kinase C, NADPH, 5-lipoxygenase, cyclooxygenase (COX) and NADPH oxidase. Anti-inflammatory antioxidant. Mimics glutathione peroxidase. Inhibits oxidative modifications of low density lipoproteins (LDL).
Product Specific Literature References
A novel biologically active seleno-organic compound--III. Effects of PZ 51 (Ebselen) on glutathione peroxidase and secretory activities of mouse macrophages: M.J. Parnham & S. Kindt; Biochem. Pharmacol. 33, 3247 (1984) Abstract
Seleno-organic compounds and the therapy of hydroperoxide-linked pathological conditions: M.J. Parnham & E. Graf; Biochem. Pharmacol. 36, 3095 (1987) Abstract
Kinetic mechanism and substrate specificity of glutathione peroxidase activity of ebselen (PZ51): M. Maiorino, et al.; Biochem. Pharmacol. 37, 2267 (1988) Abstract
Studies on the anti-inflammatory activity of ebselen. Ebselen interferes with granulocyte oxidative burst by dual inhibition of NADPH oxidase and protein kinase C?: I.A. Cotgreave, et al.; Biochem. Pharmacol. 38, 649 (1989) Abstract
T. Nikawa, et al.; Biochem. Pharmacol. 47, 1007 (1994) Abstract
Effects of ebselen and probucol on oxidative modifications of lipid and protein of low density lipoprotein induced by free radicals: N. Noguchi, et al.; Biochim. Biophys. Acta 1213, 176 (1994) Abstract
Strong inhibition of mammalian lipoxygenases by the antiinflammatory seleno-organic compound ebselen in the absence of glutathione: C. Schewe, et al.; Biochem. Pharmacol. 48, 65 (1994) Abstract
Ebselen: a glutathione peroxidase mimic: H. Sies; Meth. Enzymol. 234, 476 (1994) Abstract
Molecular actions of ebselen-an antiinflammatory antioxidant: T. Schewe; Gen. Pharmacol. 26, 1153 (1995) Abstract
Ebselen: H. Sies; Meth. Enzymol. 252, 341 (1995) Abstract
Ebselen as a glutathione peroxidase mimic and as a scavenger of peroxynitrite: H. Sies & H. Masumoto; Adv. Pharmacol. 38, 229 (1997) Abstract
Free radical generation by selenium compounds and their prooxidant toxicity: J.E. Spallholz; Biomed. Environ. Sci. 10, 260 (1997) Abstract
Protection against peroxynitrite by selenoproteins: H. Sies, et al.; Z. Naturforsch. [C] 53, 228 (1998) Abstract
Ebselen protects mice against T cell-dependent, TNF-mediated apoptotic liver injury: G. Tiegs, et al.; J. Pharmacol. Exp. Ther. 287, 1098 (1998) Abstract; Full Text
 
 
ALX-155-021 Revised 29-Jun-05
EGF Receptor (human) (651-658)
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SYNONYMS Epidermal Growth Factor Receptor (human) (651-658)
EGFR (human) (651-658)
HER-1 (human) (651-658)
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY EGF / EGF Receptor [EGFR] Kinase Other Products
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-155-021-M001   1 mg 50.00 USD Add To Cart
ALX-155-021-M005   5 mg 200.00 USD Add To Cart
Product Specification
SEQUENCE: H-Arg-Lys-Arg-Thr-Leu-Arg-Arg-Leu-OH
FORMULA: C46H91N21O10
MW: 1098.4
PURITY: ≥97%
APPEARANCE: White lyophilized powder.
SOLUBILITY: Soluble in water.
LONG TERM STORAGE: -20°C
Product Description
Substrate for protein kinase C (PKC).
Product Specific Literature References
A novel N-myristylated synthetic octapeptide inhibits protein kinase C activity and partially reverses murine fibrosarcoma cell resistance to adriamycin: C.A. O'Brian, et al.; Invest. New Drugs 9, 169 (1991) Abstract
Further Categories Containing This Product:
PeptidesPKC Substrates
 
 
ALX-155-022 Revised 29-Jun-05
EGF Receptor (human) (651-658) (N-Myristoylated)
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SYNONYMS Epidermal Growth Factor Receptor (human) (651-658) (N-Myristoylated)
EGFR (human) (651-658) (N-Myristoylated)
HER-1 (human) (651-658) (N-Myristoylated)
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY EGF / EGF Receptor [EGFR] Kinase Other Products
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-155-022-M001   1 mg 60.00 USD Add To Cart
ALX-155-022-M005   5 mg 240.00 USD Add To Cart
Product Specification
SEQUENCE: Myr-Arg-Lys-Arg-Thr-Leu-Arg-Arg-Leu-OH
FORMULA: C60H117N21O11
MW: 1308.7
PURITY: ≥97%
APPEARANCE: White lyophilized powder.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
Product Description
Potent, cell permeable and possibly selective inhibitor of protein kinase C (PKC). This product is the N-terminal myristoylated form of Prod. No. ALX-155-021.
Product Specific Literature References
A novel N-myristylated synthetic octapeptide inhibits protein kinase C activity and partially reverses murine fibrosarcoma cell resistance to adriamycin: C.A. O'Brian, et al.; Invest. New Drugs 9, 169 (1991) Abstract
Cyanobacteria secondary metabolites-the cyanotoxins: W.W. Carmichael; J. Appl. Bacteriol. 72, 445 (1992) Abstract
Inhibition of protein kinase C by N-myristoylated peptide substrate analogs: N.G. Ward & C.A. O'Brian; Biochemistry 32, 11903 (1993) Abstract
Further Categories Containing This Product:
PeptidesPKC Inhibitors
 
 
ALX-155-023 Revised 29-Jun-05
EGF Receptor (human) (652-657)
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SYNONYMS Epidermal Growth Factor Receptor (human) (652-657)
EGFR (human) (652-657)
HER-1 (human) (652-657)
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY EGF / EGF Receptor [EGFR] Kinase Other Products
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-155-023-M001   1 mg 45.00 USD Add To Cart
ALX-155-023-M005   5 mg 180.00 USD Add To Cart
Product Specification
SEQUENCE: H-Lys-Arg-Thr-Leu-Arg-Arg-OH
FORMULA: C34H68N16O8
MW: 829.0
PURITY: ≥97%
APPEARANCE: White lyophilized powder.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
Product Description
Specific substrate (aa 652-657 of mature EGF receptor, without signal peptide (aa 1-24)) for protein kinase C (PKC).
Product Specific Literature References
Regulation of protein kinase C by nerve growth factor, epidermal growth factor, and phorbol esters in PC12 pheochromocytoma cells: L. Heasley & G.L. Johnson; J. Biol. Chem. 264, 8646 (1989) Abstract; Full Text
Further Categories Containing This Product:
PeptidesPKC Substrates
 
 
ALX-850-266 Revised 11-Apr-08
EGF Receptor, Soluble (active) (human) ELISA Kit
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY EGF / EGF Receptor [EGFR] Kinase Other Products
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-850-266-KI01   1 Kit 664.00 USD Add To Cart
Product Specification
SENSITIVITY: 0.05fmol/ml (range 0.8 to 5fmol/ml)
QUANTITY: 96 wells (~80 tests)
APPLICATION: For the quantitative determination of soluble human epidermal growth factor receptor (hsEGF-R) in cell culture lysate, serum and other body fluids.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: +4°C
General Information
MANUFACTURER Manufactured by Bender MedSystems.
Further Categories Containing This Product:
ELISA & EIA Kits
 
 
ALX-270-389 Revised 11-Sep-08
Elbfluorene
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SYNONYMS 3-Acetyl-6-hydroxy-4-phenylbenzo[4,5]furo[2,3-b]pyridine
1-Aza-9-oxafluorene 5b
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY DNA Repair Other Products
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-389-M001   1 mg 75.00 USD Add To Cart
ALX-270-389-M005   5 mg 300.00 USD Add To Cart
Product Specification
FORMULA: C19H13NO3
MW: 303.3
PURITY: ≥95% (HPLC)
APPEARANCE: Off-white to brownish powder.
SOLUBILITY: Soluble in DMSO. Insoluble in water or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Selective inhibitor of CDK1/cyclin B (IC50=4.2µM) with some P-glycoprotein-modulating properties (inhibitory activity ratio 1.26 at 7µM). Weakly inhibits CDK5/p25 (6% inhibition at 10µM) with no effect on CDK2/cyclin E and CDK4/cyclin D1 (IC50>100µM).
Product Specific Literature References
Evaluation of the first cytostatically active 1-aza-9-oxafluorenes as novel selective CDK1 inhibitors with P-glycoprotein modulating properties: K. Brachwitz, et al.; J. Med. Chem. 46, 876 (2003) Abstract
Novel CDK inhibition profiles of structurally varied 1-aza-9-oxafluorenes: B. Voigt, et al.; Bioorg. Med. Chem. Lett. 15, 823 (2005) Abstract
Further Categories Containing This Product:
CDK & Cyclin Inhibitors
 
 
ALX-350-057 Revised 20-Feb-08
Emodin
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SYNONYMS 6-Methyl-1,3,8-trihydroxyanthraquinone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
Ordering Information
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ALX-350-057-M025   25 mg 45.00 USD Add To Cart
Product Specification
FORMULA: C15H10O5
MW: 270.2
CAS NUMBER: 518-82-1
MERCK INDEX: 14: 3561
RTECS: CB7920600
SOURCE/HOST: Isolated from Frangula bark.
PURITY: ≥96% (HPLC)
APPEARANCE: Orange to red solid.
SOLUBILITY: Soluble in DMSO, 100% ethanol or 1N dilute aqueous ammonia; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HAZARD: IRRITANT.

Product Description
Inhibitor of p56lck tyrosine kinase. Has mutagenic and genotoxic effects, mainly in bacterial systems. Anticancer agent. Exhibits anti-proliferative effects in various cancer cell lines by efficient induction of apoptosis. Has inhibitory effects on angiogenic and metastasis regulatory processes. Anti-inflammatory compound. Suppresses NF-κB activation. 
Product Specific Literature References
Emodin, a protein tyrosine kinase inhibitor from Polygonum cuspidatum: H. Jayasuriya, et al.; J. Nat. Prod. 55, 696 (1992) Abstract
Selective inhibition of the growth of ras-transformed human bronchial epithelial cells by emodin, a protein-tyrosine kinase inhibitor: T.C.K. Chan, et al.; BBRC 193, 1152 (1993) Abstract
Molecular mechanism of emodin action: transition from laxative ingredient to an antitumor agent: G. Srinivas, et al.; Med. Res. Rev. 27, 591 (2007), (Review) Abstract
 
 
ALX-270-263 Revised 03-Apr-08
(-)-Epigallocatechin gallate
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SYNONYMS EGCG
(2R,3R)-2-(3,4,5-Trihydroxyphenyl)-3,4-dihydro-1[2H]-benzopyran-3,5,7-triol 3-(3,4,5-trihydroxybenzoate)
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antioxidants
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-263-M010   10 mg 20.00 USD Add To Cart
ALX-270-263-M050   50 mg 60.00 USD Add To Cart
Product Specification
FORMULA: C22H18O11
MW: 458.4
CAS NUMBER: 989-51-5
MERCK INDEX: 14: 3526
SOURCE/HOST: Isolated from green tea.
PURITY: ≥98% (HPLC)
APPEARANCE: Off-white to yellow powder.
SOLUBILITY: Soluble in 100% ethanol, dimethyl formamide or DMSO; slightly soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Stock solutions in DMSO are stable for up to 3 months when stored at -20°C.
HANDLING: After reconstitution, prepare aliquots and store at -20°C. Keep under inert gas. Protect from light.

Product Description
Antitumor reagent. Antioxidant. Protects cells from lipid peroxidation and DNA damage induced by reactive free radicals. Inhibits inducible nitric oxide synthase (iNOS; NOS II). Chemopreventive anticancer agent. Induces apoptosis in human cancer cell lines. Inhibits MAP kinase mediated signalling pathways. Inhibits angiogenesis. Inhibits telomerase and DNA methyltransferase. Anti-inflammatory agent.
Product Specific Literature References
Inhibitory effect of topical application of a green tea polyphenol fraction on tumor initiation and promotion in mouse skin: M.T. Huang, et al.; Carcinogenesis 13, 947 (1992) Abstract
Inhibition of 12-O-tetradecanoylphorbol-13-acetate and other skin tumor-promoter-caused induction of epidermal interleukin-1 alpha mRNA and protein expression in SENCAR mice by green tea polyphenols: S.K. Katiyar, et al.; J. Invest. Dermatol. 105, 394 (1995) Abstract
Growth inhibition and regression of human prostate and breast tumors in athymic mice by tea epigallocatechin gallate: S. Liao, et al.; Cancer Lett. 96, 239 (1995) Abstract
Inhibition of N-methyl-N'-nitro-N-nitrosoguanidine-induced carcinogenesis by (-)-epigallocatechin gallate in the rat glandular stomach: T. Yamane, et al.; Cancer Res. 55, 2081 (1995) Abstract
(-)-Epigallocatechin gallate, a polyphenolic tea antioxidant, inhibits peroxynitrite-mediated formation of 8-oxodeoxyguanosine and 3-nitrotyrosine: E.S. Fiala, et al.; Experientia 52, 922 (1996) Abstract
Green tea constituent epigallocatechin-3-gallate and induction of apoptosis and cell cycle arrest in human carcinoma cells: N. Ahmad, et al.; J. Natl. Cancer Inst. 89, 1881 (1997) Abstract
Inhibition of inducible nitric oxide synthase gene expression and enzyme activity by epigallocatechin gallate, a natural product from green tea: M.M. Chan, et al.; Biochem. Pharmacol. 54, 1281 (1997) Abstract
(-)-Epigallocatechin-3-gallate blocks the induction of nitric oxide synthase by down-regulating lipopolysaccharide-induced activity of transcription factor nuclear factor-kappaB: Y.L. Lin & J.K. Lin; Mol. Pharmacol. 52, 465 (1997) Abstract
Telomerase inhibition, telomere shortening, and senescence of cancer cells by tea catechins: I. Naasani, et al.; BBRC 249, 391 (1998) Abstract
Epigallocatechin suppression of proliferation of vascular smooth muscle cells: correlation with c-jun and JNK: L.H. Lu, et al.; Br. J. Pharmacol. 124, 1227 (1998) Abstract
ESR study on the structure-antioxidant activity relationship of tea catechins and their epimers: Q. Guo, et al.; Biochim. Biophys. Acta 1427, 13 (1999) Abstract
Pharmacokinetics of the green tea derivative, EGCG, by the topical route of administration in mouse and human skin: K. Dvorakova, et al.; Cancer Chemother. Pharmacol. 43, 331 (1999)