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Tyrosine Kinase Inhibitors
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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
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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
Further Categories Containing This Product:
Tyrosine Kinase Inhibitors • Other Toxins • Src Family Kinases / Related Products • Kinases in T Cell Signal Transduction / Related Products • Natural Products - Anti-inflammatory Agents • Natural Products - NF-kB Pathway Inhibitors • Natural Products - Antitumor Reagents • Natural Products - Apoptosis Inducers & Inhibitors • NF-kB Pathway Inhibitors
 
 
ALX-350-084 Revised 07-Apr-08
Lavendustin C methyl ester
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SYNONYMS Compound 5 methyl ester
5-Amino-N-(2,5-dihydroxybenzyl)methyl salicylate
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-084-M001   1 mg 50.00 USD Add To Cart
ALX-350-084-M005   5 mg 200.00 USD Add To Cart
Product Specification
FORMULA: C15H15NO5
MW: 289.3
SOURCE/HOST: Synthetic.
PURITY: ≥97%
APPEARANCE: Off-white solid.
SOLUBILITY: Soluble in DMSO or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: TOXIC.

Product Description
Inhibitor of EGFR tyrosine kinase with improved bioavailability over lavendustin C (Prod. No. ALX-270-066).
Product Specific Literature References
Synthesis and structure-activity studies of a series of [(hydroxybenzyl)amino]salicylates as inhibitors of EGF receptor- associated tyrosine kinase activity: H. Chen, et al.; J. Med. Chem. 36, 4094 (1993) Abstract
Structure-activity relationships in a series of 5-[(2,5- dihydroxybenzyl)amino]salicylate inhibitors of EGF-receptor-associated tyrosine kinase: importance of additional hydrophobic aromatic interactions: H. Chen, et al.; J. Med. Chem. 37, 845 (1994) Abstract
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Further Categories Containing This Product:
Tyrosine Kinase Inhibitors • EGFR Kinase Inhibitors
 
 
ALX-350-091 Revised 14-Jan-08
Lavendustin A methyl ester
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-091-M001   1 mg 50.00 USD Add To Cart
ALX-350-091-M005   5 mg 190.00 USD Add To Cart
Product Specification
FORMULA: C22H21NO6
MW: 395.4
PURITY: ≥97%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Cell permeable ester of lavendustin A (Prod. No. ALX-350-007).
Product Specific Literature References
Inhibition of tyrosine kinase and epidermal growth factor receptor internalization by lavendustin A methyl ester in cultured A431 cells: T. Onoda, et al.; Drugs Exp. Clin. Res. 16, 249 (1990) Abstract
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Further Categories Containing This Product:
Tyrosine Kinase Inhibitors • EGFR Kinase Inhibitors
 
 
ALX-350-226 Revised 22-Sep-08
Caffeic acid methyl ester
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SYNONYMS Methyl caffeate
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-226-M050   50 mg 60.00 USD Add To Cart
Product Specification
FORMULA: C10H10O4
MW: 194.2
CAS NUMBER: 3843-74-1
SOURCE/HOST: Synthetic.
PURITY: ≥98% (HPLC)
APPEARANCE: Slightly yellowish solid.
SOLUBILITY: Soluble in DMSO, methanol or acetone.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
IDENTITY: Identity determined by 1H-NMR.

Product Description
Inhibitor of ornithine decarboxylase and protein tyrosine kinases. Has a strong inhibitory effect on human platelet aggregation. Shows antioxidant, antiproliferative and cytotoxic properties.
Product Specific Literature References
Effect of caffeic acid esters on carcinogen-induced mutagenicity and human colon adenocarcinoma cell growth: C.V. Rao, et al.; Chem. Biol. Interactions 84, 277 (1992) Abstract
Inhibition of platelet activation and endothelial cell injury by polyphenolic compounds isolated from Lonicera japonica Thunb: W.C. Chang & F.L. Hsu; Prostaglandins Leukot. Essent. Fatty Acids 45, 307 (1992) Abstract
Phenolic compounds from Duchesnea chrysantha and their cytotoxic activities in human cancer cell: I.R. Lee & M.Y. Yang; Arch. Pharm. Res. 17, 476 (1994) Abstract
Anti-platelet effect of the constituents isolated from the barks and fruits of Magnolia obovata: M.K. Pyo, et al.; Arch. Pharm. Res. 25, 325 (2002) Abstract
Black cohosh (Cimicifuga racemosa L.) protects against menadione-induced DNA damage through scavenging of reactive oxygen species: bioassay-directed isolation and characterization of active principles: J.E. Burdette, et al.; J. Agric. Food Chem. 50, 7022 (2002) Abstract
Phenolic acid derivatives with potential anticancer properties--a structure-activity relationship study. Part 1: methyl, propyl and octyl esters of caffeic and gallic acids: S.M. Fiuza, et al.; Bioorg. Med. Chem. 12, 3581 (2004) Abstract
Further Categories Containing This Product:
Other Natural Products for Cancer Research • Tyrosine Kinase Inhibitors • Antithrombotic Agents / Platelet Aggregation Inhibitors / Related Products • Natural Products - Antioxidants • Antitumor Agents (Anti-proliferative) • Phenolic Acids
 
 
ALX-350-246 Revised 07-Oct-08
Butein
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SYNONYMS 2',3,4,4'-Tetrahydroxychalcone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-246-M010   10 mg 190.00 USD Add To Cart
Product Specification
FORMULA: C15H12O5
MW: 272.3
CAS NUMBER: 487-52-5
PURITY: ≥98% (HPLC)
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO (>50mg/ml) or methanol; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light. Keep cool and dry under inert gas.
IDENTITY: Identity determined by 1H-NMR, 13C-NMR and MS.

Product Description
Plant polyphenol. Specific tyrosine kinase inhibitor. Potently inhibits the tyrosine kinase activity of the EGF receptor and p60c-src. Potent antioxidant and anti-inflammatory agent. Inhibits glutathione reductase and rat liver glutathione S-transferase. Activator of human deacetylase SIRT1. Inhibits aromatase, showing chemopreventive properties. Directly inhibits IKK.
Product Specific Literature References
Inhibition of 12-O-tetradecanoylphorbol-13-acetate-mediated epidermal ornithine decarboxylase induction and skin tumor promotion by new lipoxygenase inhibitors lacking protein kinase C inhibitory effects: E. Aizu, et al.; Carcinogenesis 7, 1809 (1986) Abstract
Protective effects of hydroxychalcones on free radical-induced cell damage: S. Sogawa, et al.; Biol. Pharm. Bull. 17, 251 (1994) Abstract
Cytotoxic effect of butein on human colon adenocarcinoma cell proliferation: C.C. Yit & N.P. Das; Cancer Lett. 82, 65 (1994) Abstract
Inhibitory effects of plant polyphenols on rat liver glutathione S-transferase: K. Zhang & N.P. Das; Biochem. Pharmacol. 47, 2063 (1994) Abstract
Endothelium-dependent relaxation of rat aorta by butein, a novel cyclic AMP-specific phosphodiesterase inhibitor: S.M. Yu, et al.; Eur. J. Pharmacol. 280, 69 (1995) Abstract
Butein (3,4,2',4'-tetrahydroxychalcone) ameliorates experimantal anti-glomerular basement membrane antibody-associated glomerulonephritis (3): K. Hayashi, et al.; Eur. J. Pharmacol. 316, 297 (1996) Abstract
Inhibition of glutathione reductase by plant polyphenols: K. Zhang, et al.; Biochem. Pharmacol 54, 1047 (1997) Abstract
Butein, a specific protein tyrosine kinase inhibitor: E.-B. Yang, et al.; BBRC 245, 435 (1998) Abstract
Antioxidant properties of butein isolated from Dalbergia odorifera: Z.J. Cheng, et al.; Biochim. Biophys. Acta 1392, 291 (1998) Abstract
Flavonoids inhibit cell growth and induce apoptosis in B16 melanoma 4A5 cells: K. Iwashita, et al.; Biosci. Biotechnol. Biochem. 64, 1813 (2000) Abstract
Butein, a plant polyphenol, induces apoptosis concomitant with increased caspase-3 activity, decreased Bcl-2 expression and increased Bax expression in HL-60 cells: N.Y. Kim, et al.; Pharmacol. Toxicol. 88, 261 (2001) Abstract
Small molecule activators of sirtuins extend Saccharomyces cerevisiae lifespan: K.T. Howitz, et al.; Nature 425, 191 (2003) Abstract
The plant polyphenol butein inhibits testosterone-induced proliferation in breast cancer cells expressing aromatase: Y. Wang, et al.; Life Sci. 77, 39 (2005) Abstract
Butein, a tetrahydroxychalcone, inhibits nuclear factor (NF)-kappaB and NF-kappaB-regulated gene expression through direct inhibition of IkappaBalpha kinase beta on cysteine 179 residue: M.K. Pandey, et al.; J. Biol. Chem. 282, 17340 (2007) Abstract
Further Categories Containing This Product:
Tyrosine Kinase Inhibitors • Natural Products - Anti-inflammatory Agents • EGFR Kinase Inhibitors • Glutathione / Related Products • Chalcones • Phosphodiesterases / Related Products • Natural Products - Chemopreventive Agents • Glutathione S-Transferase • Natural Products - Antioxidants • Sirtuins / Related Products • IkB Kinases [IKKs] / Related Products
 
 
ALX-350-247 Revised 27-Oct-08
Genistin
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SYNONYMS Genistein-7-O-glucoside
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-247-M010   10 mg 180.00 USD Add To Cart
Product Specification
FORMULA: C21H20O10
MW: 432.4
CAS NUMBER: 529-59-9
MERCK INDEX: 14: 4391
RTECS: DJ3093000
PURITY: ≥98%
APPEARANCE: Off-white to light yellow powder.
SOLUBILITY: Soluble in DMSO or dilute aqueous base; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Glucoside of genistein (Prod. No. ALX-350-006) found in soy beans. Useful as a negative control for genistein and other tyrosine kinase inhibitors. Selective inhibitor of terminal deoxyribonucleotidyltransferase (TdT). Displays antioxidant and anticarcinogenic properties.
Product Specific Literature References
Soybean isoflavones, genistein and genistin, inhibit rat myoblast proliferation, fusion and myotube protein synthesis: S. Ji, et al.; J. Nutr. 129, 1291 (1999) Abstract
Daidzein and genistein but not their glucosides are absorbed from the rat stomach: M.K. Piskula, et al.; FEBS Lett. 447, 287 (1999) Abstract
Inhibition of CYP1A1 enzyme activity in mouse hepatoma cell culture by soybean isoflavones: H.G. Shertzer, et al.; Chem. Biol. Interact. 123, 31 (1999) Abstract
Selective inhibitors of terminal deoxyribonucleotidyltransferase (TdT): baicalin and genistin: Y. Uchiyama, et al.; Biochim. Biophys. Acta 1725, 298 (2005) Abstract
Genistin inhibits UV light-induced plasmid DNA damage and cell growth in human melanoma cells: A. Russo, et al.; J. Nutr. Biochem. 17, 103 (2006) Abstract
Pro-apoptotic effect and cytotoxicity of genistein and genistin in human ovarian cancer SK-OV-3 cells: E.J. Choi, et al.; Life Sci. 80, 1403 (2007) Abstract
Further Categories Containing This Product:
Tyrosine Kinase Inhibitors • Natural Products - Topoisomerase Inhibitors • Natural Products - Chemopreventive Agents • Natural Products - Antioxidants • Active Substances from Fruit and Vegetables • Isoflavones
 
 
ALX-350-256 Revised 07-Oct-08
(+)-Aeroplysinin-1
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-256-M001   1 mg 70.00 USD Add To Cart
Product Specification
FORMULA: C9H9Br2NO3
MW: 339.0
CAS NUMBER: 28656-91-9
SOURCE/HOST: Isolated from Aplysina aerophoba.
PURITY: ≥97%
APPEARANCE: Oil.
SOLUBILITY: Soluble in 100% ethanol or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Displays cytostatic and cytotoxic activity. Inhibitor of EGFR kinase. Shows antiangiogenic activity.
Product Specific Literature References
Aeroplysinin-1, an antibacterial bromo-compound from the sponge Verongia aerophoba: E. Fattorusso, et al.; J. Chem. Soc. 1, 16 (1972) Abstract
Cytostatic activity of aeroplysinin-1 against lymphoma and epithelioma cells: M.H. Kreuter, et al.; Z. Naturforsch. [C] 44, 680 (1989) Abstract
Inhibition of intrinsic protein tyrosine kinase activity of EGF-receptor kinase complex from human breast cancer cells by the marine sponge metabolite (+)-aeroplysinin-1: M.H. Kreuter, et al.; Comp. Biochem. Physiol. B 97, 151 (1990) Abstract
Production of the cytostatic agent aeroplysinin by the sponge Verongia aerophoba in in vitro culture: M.H. Kreuter, et al.; Comp. Biochem. Physiol. 101C, 183 (1992) Abstract
Antibiotic and cytotoxic activity of brominated compounds from the marine sponge Verongia aerophoba: R. Teeyapant, et al.; Z. Naturforsch. [C] 48, 939 (1993) Abstract
Cytotoxicity and mode of action of aeroplysinin-1 and a related dienonefrom the sponge Aplysina aerophoba: A. Koulman, et al.; J. Nat. Prod. 59, 591 (1996) Abstract
Antiangiogenic activity of aeroplysinin-1, a brominated compound isolated from a marine sponge: S. Rodriguez-Nieto, et al.; FASEB J. 16, 261 (2002) Abstract
Further Categories Containing This Product:
Tyrosine Kinase Inhibitors • EGFR Kinase Inhibitors • Natural Products with Antibiotic Activity • Natural Products - Antitumor Reagents • Natural Products for Angiogenesis Research • Marine Natural Products
 
 
ALX-350-292 Revised 26-Mar-05
Kahalalide F - Discontinued Due to Patent Restrictions
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antitumor Reagents
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ALX-350-292-C500   500 µg Inquire
Product Specification
FORMULA: C75H124N14O16
MW: 1477.9
CAS NUMBER: 149204-42-2
SOURCE/HOST: Isolated from marine mollusc Elysia rufescens.
PURITY: ≥95%
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Highly selective activity against prostate tumors in vitro. Disrupts lysosomal membranes. Inhibitor of c-erbB-2 (ErbB2).
Product Specific Literature References
The antitumoral compound Kahalalide F acts on cell lysosomes: M. Garcia-Rocha, et al.; Cancer Lett. 99, 43 (1996) Abstract
Synthesis and structure determination of kahalalide F (1,2): Synthesis and structure determination of kahalalide F (1,2); J. Am. Chem. Soc. 123, 11398 (2001) Abstract
Chemical and enzymatic stability of a cyclic depsipeptide, the novel, marine-derived, anti-cancer agent kahalalide F: R.W. Sparidans, et al.; Anticancer Drugs 12, 575 (2001) Abstract
Preclinical toxicity studies of kahalalide F, a new anticancer agent: single and multiple dosing regimens in the rat: A.P. Brown, et al.; Cancer Chemother. Pharmacol. 50, 333 (2002) Abstract
Quantitative analysis of the novel depsipeptide anticancer drug Kahalalide F in human plasma by high-performance liquid chromatography under basic conditions coupled to electrospray ionization tandem mass spectrometry: E. Stokvis, et al.; J. Mass. Spectrom. 37, 992 (2002) Abstract
Further Categories Containing This Product:
Tyrosine Kinase Inhibitors • Natural Products - Protein Kinase Inhibitors • erbB-2 / Related Products • Antitumor Agents (Enzyme Inhibitors)
 
 
ALX-350-325 Revised 25-Jun-07
Altenusin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Antifungal
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ALX-350-325-M001   1 mg 110.00 USD Add To Cart
ALX-350-325-M005   5 mg 380.00 USD Add To Cart
Product Specification
FORMULA: C15H14O6
MW: 290.3
CAS NUMBER: 31186-12-6
SOURCE/HOST: Isolated from Alternaria sp.
PURITY: ≥97% (HPLC)
APPEARANCE: Yellow to brown solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
IDENTITY: Identity determined by 1H-NMR, 13C-NMR and MS.

Product Description
Antifungal penicillide. Non-competitive, specific neutral sphingomyelinase (N-SMase) and strong pp60c-Src inhibitor. Inhibits cFMS receptor tyrosine kinase (CSF-1/m-CSF receptor tyrosine kinase) which is implicated in cancer and bone diseases. Myosin light chain kinase inhibitor. Exhibits anti-HIV-1 integrase activity.
Product Specific Literature References
Studies in the biochemistry of micro-organisms. 103. Metabolites of Alternaria tenuis Auct.: Culture filtrate products: T. Rosett, et al.; Biochem. J. 67, 390 (1957) Full Text
Studies in the biosynthesis of fungal metabolites. 4. Alternariol monomethyl ether and its relation to other phenolic metabolites of Alternaria tenuis: R. Thomas; Biochem. J. 80, 234 (1961) Abstract; Full Text
Metabolites of some Alternaria species. The structures of altenusin and dehydroaltenusin: R. G. Coombe, et al.; Aus. J. Chem. 23, 2343 (1970)
Host-specific toxins and chemical structures from alternaria species: S. Nishimura, et al.; Ann. Rev. Phytopathol. 21, 87 (1983)
The metabolites of Talaromycesflavus: Part 1. Metabolites of the organic extracts : W. A. Ayer, et al.; Can. J. Chem. 68, 2085 (1990)
Isolation of myosin light chain kinase inhibitors from microorganisms: dehydroaltenusin, altenusin, atrovenetinone, and cyclooctasulfur: S. Nakanishi, et al.; Biosci. Biotechnol. Biochem. 59, 1333 (1995) Abstract
Alutenusin, a specific neutral sphingomyelinase inhibitor, produced by Penicillium sp. FO-7436: R. Uchida, et al.; J. Antibiot. 52, 572 (1999) Abstract
Isolation, structure, and HIV-1-integrase inhibitory activity of structurally diverse fungal metabolites: S.B. Singh, et al.; J. Ind. Microbiol. Biotechnol. 30, 721 (2003) Abstract
Fungal metabolites as potent protein kinase inhibitors: Identification of a novel metabolite and novel activities of known metabolites : M. Oyama, et al.; Lett. Drug Design Discov. 1, 24 (2004)
New penicillide derivatives isolated from Penicillium simplicissimum: S. I. Komai, et al.; J. Nat. Med. 60, 185 (2006)
HIV-1 integrase inhibitors: 2003-2004 update: R. Dayam, et al.; Med. Res. Rev. 26, 271 (2006) Abstract
Further Categories Containing This Product:
Myosin Light Chain Kinase Inhibitors • Tyrosine Kinase Inhibitors • Antibiotics - Antiviral / Anti-HIV