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Natural Products - Protein Kinase Inhibitors
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ALX-350-113 Revised 28-May-08
Gossypol
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SYNONYMS 2,2’-bis[8-Formyl-1,6,7-trihydroxy-5-isopropyl-3-
methylnaphthalene]
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antitumor Reagents
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ALX-350-113-M100   100 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C30H30O8
MW: 518.6
CAS NUMBER: 303-45-7
MERCK INDEX: 14: 4528
RTECS: DU3100000
SOURCE/HOST: Isolated from Gossypium genus, Malvaceae.
PURITY: ≥90%
APPEARANCE: Off-white to yellow solid.
SOLUBILITY: Soluble in acetone or DMSO; sparingly soluble in 100% ethanol (2mg/ml) or methanol (2mg/ml). Insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.
HAZARD: MAY BE CARCINOGENIC. HARMFUL.

Product Description
Mixture of ~65% (+)- and ~35% (-)-enantiomers. Male antifertility agent. Shows antitumor, antiviral and antioxidant actions. Small molecule inhibitor of Bcl-2/Bcl-XL. Induces apoptosis. Synergizes with radiation and chemotherapy in vitro. Reversible inhibitor of protein phosphatase 2B (PP2B; calcineurin). Protein kinase C (PKC) inhibitor.
Product Specific Literature References
Binding of gossypol to purified tubulin and inhibition of its assembly into microtubules: F.J. Medrano and J.M. Andreu; Eur. J. Biochem. 158, 63 (1986) Abstract
Differential inhibition of protein kinase C subtypes: J.M. Pelosin, et al.; BBRC 169, 1040 (1990) Abstract
Induction of apoptotic DNA fragmentation and cell death in HL-60 human promyelocytic leukemia cells by pharmacological inhibitors of protein kinase C: W.D. Jarvis, et al.; Cancer Res. 54, 1707 (1994) Abstract
Gossypol arrests human benign prostatic hyperplastic cell growth at G0/G1 phase of the cell cycle: F. Shidaifat, et al.; Anticancer Res. 17, 1003 (1997) Abstract
Inhibition of huntingtin fibrillogenesis by specific antibodies and small molecules: implications for Huntington’s disease therapy: V. Heiser, et al.; PNAS 97, 6739 (2000) Abstract; Full Text
Cytotoxic effect of gossypol on colon carcinoma cells: X. Wang, et al.; Life Sci. 67, 2663 (2000) Abstract
Reversible inhibition of calcineurin by the polyphenolic aldehyde gossypol: R. Baumgrass, et al.; J. Biol. Chem. 276, 47914 (2001) Abstract; Full Text
Toxicity of (+)- and (-)-gossypol to the plant pathogen, Rhizoctonia solani: L.S. Puckhaber, et al.; J. Agric. Food Chem. 50, 7017 (2002) Abstract
Telomerase inhibitors in anticancer therapy: gossypol as a potential telomerase inhibitor: M. Mego; Bratisl. Lek. Listy 103, 378 (2002) Abstract
An in vitro study of inhibitory activity of gossypol, a cottonseed extract, in human carcinoma cell lines: M. Le Blanc, et al.; Pharmacol. Res. 46, 551 (2002) Abstract
Gossypol induces chloride secretion in rat proximal colon: G. Kuhn, et al.; Eur. J. Pharmacol. 457, 187 (2002) Abstract
Determination of the absolute configuration and solution conformation of gossypol by vibrational circular dichroism: T.B. Freedman, et al.; Chirality 15, 196 (2003) Abstract
In vitro effects of the BH3 mimetic, (-)-gossypol, on head and neck squamous cell carcinoma cells: C.L. Oliver, et al.; Clin. Cancer Res. 10, 7757 (2004) Abstract; Full Text
The inhibitory effects of gossypol on human prostate cancer cells-PC3 are associated with transforming growth factor beta1 (TGFbeta1) signal transduction pathway: J. Jiang, et al.; Anticancer Res. 24, 19 (2004) Abstract
(-)-Gossypol enhances response to radiation therapy and results in tumor regression of human prostate cancer: L. Xu, et al.; Mol. Cancer Ther. 4, 197 (2005) Abstract; Full Text
Investigations on gossypol: past and present developments: K. Dodou; Expert Opin. Investig. Drugs 14, 1419 (2005) Abstract
An in vitro study of cytotoxic effects of gossypol on human epidermoid larynx carcinoma cell line (HEp-2): E. Konac, et al.; Exp. Oncol. 27, 81 (2005) Abstract; Full Text
Further Categories Containing This Product:
Bcl-2 Family Modulators • Natural Products - Protein Kinase Inhibitors • PKC Inhibitors • Natural Products - Apoptosis Inducers & Inhibitors • PP2B [Calcineurin] / Related Products • Natural Products - Antioxidants • Polyphenols Other Products • Natural Products - Antiviral / anti-HIV Agents • Antitumor Agents (Apoptosis Inducers)
 
 
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 - Chemopreventive Agents • Natural Products - Topoisomerase Inhibitors • 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 for Angiogenesis Research • Natural Products - Antitumor Reagents • Marine Natural Products
 
 
ALX-350-258 Revised 08-Apr-08
Parthenolide
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SYNONYMS (1aR-[1aR*,4E,7aS*,-10aS*,-10bR*])-2,3-6,7,7a,8,10a,10b-Octahydro-1a,5-dimethyl-8-methyleneoxireno[9,10]cyclo deca[1,2-b]furan-9(1aH)-one
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-258-M005   5 mg 15.00 USD Add To Cart
ALX-350-258-M025   25 mg 30.00 USD Add To Cart
Product Specification
FORMULA: C15H20O3
MW: 248.3
CAS NUMBER: 20554-84-1
MERCK INDEX: 14: 7048
RTECS: LY4220000
SOURCE/HOST: Isolated from feverfew leaves.
PURITY: ≥99% (TLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO (100mg/ml), dichloromethane (50mg/ml) or 100% ethanol (20mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description

Sesquiterpene lactone. Anti-inflammatory compound. Specifically inhibits activation of NF-κB by preventing the degradation of IκBα and IκBβ. Inhibits activation of MAP kinase (MAPK/ERK) and generation of leukotriene B4 and thromboxane B2. Potent anticancer agent. Induces apoptosis in various cancer cell lines. Specifically inhibits histone deacetylase 1 (HDAC1) without affecting other class I/II HDACs. Inhibits tubulin carboxypeptidase (TCP) activity.
Product Specific Literature References
A comparison of the effects of an extract of feverfew and parthenolide, a component of feverfew, on human platelet activity in-vitro: W.A. Groenewegen & S. Heptinstall; J. Pharm. Pharmacol. 42, 553 (1990) Abstract
Feverfew extracts and parthenolide irreversibly inhibit vascular responses of the rabbit aorta: R.W. Barsby, et al.; J. Pharm. Pharmacol. 44, 737 (1992) Abstract
Inhibition of 5-lipoxygenase and cyclo-oxygenase in leukocytes by feverfew. Involvement of sesquiterpene lactones and other components: H. Sumner, et al.; Biochem. Pharmacol. 43, 2313 (1992) Abstract
Inhibition of the expression of inducible cyclooxygenase and proinflammatory cytokines by sesquiterpene lactones in macrophages correlates with the inhibition of MAP kinases: D. Hwang, et al.; BBRC 226, 810 (1996) Abstract
Sesquiterpene lactones specifically inhibit activation of NF-kappa B by preventing the degradation of I kappa B-alpha and I kappa B-beta: S.P. Hehner, et al.; J. Biol. Chem. 273, 1288 (1998) Abstract
Sesquiterpene lactones inhibit inducible nitric oxide synthase gene expression in cultured rat aortic smooth muscle cells: H.R. Wong & I.Y. Menendez; BBRC 262, 375 (1999) Abstract
The antiinflammatory sesquiterpene lactone parthenolide inhibits NF- kappa B by targeting the I kappa B kinase complex: S.P. Hehner, et al.; J. Immunol. 163, 5617 (1999) Abstract
Paclitaxel sensitivity of breast cancer cells with constitutively active NF-kappaB is enhanced by IkappaBalpha super-repressor and parthenolide: N.M. Patel, et al.; Oncogene 19, 4159 (2000) Abstract
Antitumor agent parthenolide reverses resistance of breast cancer cells to tumor necrosis factor-related apoptosis-inducing ligand through sustained activation of c-Jun N-terminal kinase: H. Nakshatri, et al.; Oncogene 23, 7330 (2004) Abstract
Involvement of proapoptotic Bcl-2 family members in parthenolide-induced mitochondrial dysfunction and apoptosis: S. Zhang, et al.; Cancer Lett. 211, 175 (2004) Abstract
Parthenolide-induced apoptosis in multiple myeloma cells involves reactive oxygen species generation and cell sensitivity depends on catalase activity: W. Wang, et al.; Apoptosis 11, 2225 (2006) Abstract
Parthenolide inhibits tubulin carboxypeptidase activity: X. Fonrose, et al.; Cancer Res. 67, 3371 (2007) Abstract
Parthenolide specifically depletes histone deacetylase 1 protein and induces cell death through ataxia telangiectasia mutated: Y.N. Gopal, et al.; Chem. Biol. 14, 813 (2007) Abstract
Further Categories Containing This Product:
MAPK Pathway Inhibitors • Natural Products - NF-kB Pathway Inhibitors • Natural Products - Apoptosis Inducers & Inhibitors • NF-kB Pathway Inhibitors • COX Inhibitors • Other Natural Products for Inflammation Research
 
 
ALX-350-276 Revised 16-Jun-08
Pseudohypericin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-276-M001   1 mg 115.00 USD Add To Cart
ALX-350-276-M005   5 mg 460.00 USD Add To Cart
Product Specification
FORMULA: C30H16O9
MW: 520.5
CAS NUMBER: 55954-61-5
SOURCE/HOST: Isolated from Hypericum perforatum.
PURITY: ≥98%
APPEARANCE: Black to black-red powder.
SOLUBILITY: Soluble in methanol, 100% ethanol, DMSO, acetone and other organic solvents.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.
HAZARD: HARMFUL.

Product Description
Inhibitor of protein kinase C (PKC) (IC50=15µg/ml). Antiviral and antiretroviral activity. Potent inhibitor of dopamine-β-hydrolase (IC50=3µg/ml).
Product Specific Literature References
Zur Isolierung und Konstitution des Pseudohypericins : H. Brockmann, et al.; Tetrahedron Lett. 15, 1991 (1974)
Therapeutic agents with dramatic antiretroviral activity and little toxicity at effective doses: aromatic polycyclic diones hypericin and pseudohypericin: D. Meruelo, et al.; PNAS 85, 5230 (1988) Abstract
Studies of the mechanisms of action of the antiretroviral agents hypericin and pseudohypericin: G. Lavie, et al.; PNAS 86, 5963 (1989) Abstract
Hypericin and pseudohypericin specifically inhibit protein kinase C: possible relation to their antiretroviral activity: I. Takahashi, et al.; BBRC 165, 1207 (1989) Abstract
Biochemical activities of extracts from Hypericum perforatum L. 5th communication: dopamine-beta-hydroxylase-product quantification by HPLC and inhibition by hypericins and flavonoids: A. Denke, et al.; Arzneimittelforschung 50, 415 (2000) Abstract
Antagonist effect of pseudohypericin at CRF1 receptors: U. Simmen, et al.; Eur. J. Pharmacol. 458, 251 (2003) Abstract
Phototoxic and apoptosis-inducing capacity of pseudohypericin: C.M. Schempp, et al.; Planta Med. 68, 171 (2002) Abstract
Further Categories Containing This Product:
PKC Inhibitors • Natural Products - Antiviral / anti-HIV Agents • Natural Products for Neurological Research • Neuroactive Agents Other Products
 
 
ALX-350-289 Revised 18-Nov-08
10Z-Hymenialdisine
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SYNONYMS 4-(2-Amino-4-oxo-2-imidazolin-5-ylidene)-2-bromo-4,5,6,7-tetrahydropyrrolo[2,3-c]azepin-8-one
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-289-C500   500 µg 190.00 USD Add To Cart
ALX-350-289-M001   1 mg 340.00 USD Add To Cart
Product Specification
FORMULA: C11H10BrN5O2
MW: 324.1
CAS NUMBER: 82005-12-7
SOURCE/HOST: Isolated from sponge Axinella carteri.
PURITY: ≥97% (HPLC)
APPEARANCE: Yellow needles.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: TOXIC.
IDENTITY: Identity determined by 1H- NMR and MS.

Product Description
Originally isolated from the sponges Axinella verrucosa and Acantella aurantiaca. Potent inhibitor of mitogen-activated protein kinase kinase-1 (MEK-1) (IC50=6nM). Blocks the in vivo phosphorylation of the microtubule-binding protein tau at sites that are hyperphosphorylated by glycogen synthase kinase-β (GSK-3β) and CDK5/p35 in Alzheimer’s disease. Inhibitor of DNA damage checkpoint at G2 phase (IC50=6µM), cyclin-dependent kinases CDK1/cyclin B (IC50=22nM), CDK2/cyclin A (IC50=70nM), CDK2/cyclin E (IC50=40nM), CDK4/cyclin D1 (IC50=600nM), CDK5/p25 (IC50=28nM), GSK-3β (IC50=10nM), and casein kinase 1 (CK1) (IC50=35nM). Inhibitor of NF-κB activation and of various pro-inflammatory cytokines such as IL-1, IL-2 (IC50=2.4µM), IL-6, IL-8, TNF-α (IC50=1.4µM) and nitric oxide (NO) (IC50=0.8µM) in a variety of cell lines.
Product Specific Literature References
Isolation and x-ray crystal structure of a novel bromo-compound from two marine sponges: G. Cimino, et al.; Tetrahedron Lett. 23, 767 (1982)
Bioactive alkaloids from the tropical marine sponge Axinella carteri: A. Supriyono, et al.; Z. Naturforsch. [C] 50, 669 (1995)