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Natural Products - Protein Kinase Inhibitors
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ALX-350-310 Revised 03-Apr-08
3-O-Acetyl-11-keto-β-boswellic acid
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SYNONYMS AKβBA
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antitumor Reagents
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ALX-350-310-M005   5 mg 130.00 USD Add To Cart
Product Specification
FORMULA: C32H48O5
MW: 512.7
CAS NUMBER: 67416-61-9
SOURCE/HOST: Isolated from Boswellia serrata.
PURITY: ≥99% (HPLC, NMR)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in acetone, dichloromethane, diethyl ether or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stock solutions are stable for up to 3 months when stored at -20°C.
HANDLING: Protect from light.
HAZARD: MAY BE CARCINOGENIC. HARMFUL.

Product Description
Shows antitumor and anti-inflammatory activities. Potent non-redox, noncompetitive 5-lipoxygenase and topoisomerase I and IIa inhibitor leading to apoptosis. 10-times more potent than 3-O-acetyl-β-boswellic acid (Prod. No. ALX-350-308). Exhibits in vivo efficacy in tumor growth and inhibition.
Product Specific Literature References
Acetyl-11-keto-beta-boswellic acid induces apoptosis in HL-60 and CCRF-CEM cells and inhibits topoisomerase I: R.F. Hoernlein, et al.; J. Pharmacol. Exp. Ther. 288, 613 (1999) Abstract; Full Text
Boswellic acids activate p42(MAPK) and p38 MAPK and stimulate Ca(2+) mobilization: A. Altmann, et al.; BBRC 290, 185 (2002) Abstract
Coupling of boswellic acid-induced Ca2+ mobilisation and MAPK activation to lipid metabolism and peroxide formation in human leucocytes: A. Altmann, et al.; Br. J. Pharmacol. 141, 223 (2004) Abstract; Full Text
Inhibition of IkappaB kinase activity by acetyl-boswellic acids promotes apoptosis in androgen-independent PC-3 prostate cancer cells in vitro and in vivo: T. Syrovets, et al.; J. Biol. Chem. 280, 6170 (2005) Abstract; Full Text
Boswellic acids: biological actions and molecular targets: D. Poeckel & O. Werz; Curr. Med. Chem. 13, 3359 (2006), Review Abstract
Mechanisms underlying the anti-inflammatory actions of boswellic acid derivatives in experimental colitis: C. Anthoni, et al.; Am. J. Physiol. Gastrointest. Liver Physiol. 290, G1131 (2006) Abstract
Potentiation of antinociceptive effect of NSAIDs by a specific lipooxygenase inhibitor, acetyl 11-keto-beta boswellic acid: M. Bishnoi, et al.; Indian J. Exp. Biol. 44, 128 (2006) Abstract
 
 
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
 
 
ALX-385-008 Revised 13-Mar-08
Apigenin
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SYNONYMS 4',5,7-Trihydroxyflavone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Flavones
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ALX-385-008-M010   10 mg 35.00 USD Add To Cart
ALX-385-008-M050   50 mg 105.00 USD Add To Cart
Product Specification
FORMULA: C15H10O5
MW: 270.2
CAS NUMBER: 520-36-5
MERCK INDEX: 14: 730
SOURCE/HOST: Synthetic.
PURITY: ≥90% (HPLC)
APPEARANCE: Light yellow to slightly brown powder.
SOLUBILITY: Soluble in diluted potassium hydroxide or DMSO; slightly soluble in 100% ethanol (hot). Insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HAZARD: IRRITANT.

Product Description
Antioxidant flavonoid. Has chemopreventive and antitumor properties. Induces apoptosis. Inhibits the proliferation of malignant tumor cells by G2/M arrest. MAP kinase (MAPK/ERK) inhibitor. Inhibits hypoxia-inducible factor-1 (HIF-1) and vascular endothelial growth factor (VEGF) expression.
Product Specific Literature References
Apigenin and tangeretin enhance gap junctional intercellular communication in rat liver epithelial cells: C. Chaumontet, et al.; Carcinogenesis 15, 2325 (1994) Abstract
Apigenin induces morphological differentiation and G2-M arrest in rat neuronal cells: F. Sato, et al.; BBRC 204, 578 (1994) Abstract
Reversion of v-H-ras-transformed NIH 3T3 cells by apigenin through inhibiting mitogen activated protein kinase and its downstream oncogenes: M.L. Kuo and N.C. Yang; BBRC 212, 767 (1995) Abstract
Structure-antioxidant activity relationships of flavonoids and phenolic acids: C.A. Rice-Evans, et al.; Free Radical Biol. & Med. 20, 933 (1996), (Review) Abstract
Apigenin inhibits endothelial-cell proliferation in G(2)/M phase whereas it stimulates smooth-muscle cells by inhibiting P21 and P27 expression: V. Trochon, et al.; Int. J. Cancer 85, 691 (2000) Abstract
Induction of caspase-dependent, p53-mediated apoptosis by apigenin in human neuroblastoma: R. Torkin, et al.; Mol. Cancer Ther. 4, 1 (2005) Abstract
Apigenin and cancer chemoprevention: progress, potential and promise: D. Patel, et al.; Int. J. Oncol. 30, 233 (2007), (Review) Abstract
Apigenin inhibits tumor angiogenesis through decreasing HIF-1alpha and VEGF expression: J. Fang, et al.; Carcinogenesis 28, 858 (2007) Abstract
Apigenin-induced cell cycle arrest is mediated by modulation of MAPK, PI3K-Akt, and loss of cyclin D1 associated retinoblastoma dephosphorylation in human prostate cancer cells: S. Shukla & S. Gupta; Cell Cycle 6, 1102 (2007) Abstract
Apigenin blocks lipopolysaccharide-induced lethality in vivo and proinflammatory cytokines expression by inactivating NF-kappaB through the suppression of p65 phosphorylation: C. Nicholas, et al.; J. Immunol. 179, 7121 (2007) Abstract
 
 
ALX-385-022 Revised 07-Oct-08
Baicalein
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SYNONYMS 5,6,7-Trihydroxyflavone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Flavones
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ALX-385-022-M005   5 mg 25.00 USD Add To Cart
ALX-385-022-M025   25 mg 100.00 USD Add To Cart
Product Specification
FORMULA: C15H10O5
MW: 270.2
CAS NUMBER: 491-67-8
MERCK INDEX: 14: 942
PURITY: ≥97%
APPEARANCE: Yellow to yellow-green crystalline powder.
SOLUBILITY: Soluble in DMSO, 100% ethanol or methanol; almost insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: IRRITANT.

Product Description
Inhibitor of 12-lipoxygenase, leukotriene biosynthesis and the release of lysosomal enzymes. Inhibits cellular Ca2+ uptake and calcium mobilization. Inhibitor of protein tyrosine kinase in leukemia (CEM) cells. Induces cell cycle arrest and apoptosis. Anti-inflammatory compound. Has anti-thrombotic, anti-proliferative and anti-mitogenic effects.
Product Specific Literature References
Specific action of the lipoxygenase pathway in mediating angiotensin II- induced aldosterone synthesis in isolated adrenal glomerulosa cells: J.L. Nadler, et al.; J. Clin. Invest. 80, 1763 (1987) Abstract
Inhibition of reverse transcriptase activity by a flavonoid compound, 5,6,7-trihydroxyflavone: K. Ono, et al.; BBRC 160, 982 (1989) Abstract
Biliary excretion of metabolites of baicalin and baicalein in rats: K. Abe, et al.; Chem. Pharm. Bull. 38, 209 (1990) Abstract
Effects of baicalein and esculetin on transduction signals and growth factors expression in T-lymphoid leukemia cells: H.C. Huang, et al.; Eur. J. Pharmacol. 268, 73 (1994) Abstract
Protective effects of baicalein against cell damage by reactive oxygen species: D. Gao, et al.; Chem. Pharm. Bull. (Tokyo) 46, 1383 (1998) Abstract
Baicalein induces a dual growth arrest by modulating multiple cell cycle regulatory molecules
:
S.L. Hsu, et al.; Eur. J. Pharmacol. 425, 165 (2001) Abstract
Mechanisms in mediating the anti-inflammatory effects of baicalin and baicalein in human leukocytes: Y.C. Shen, et al.; Eur. J. Pharmacol. 465, 171 (2003) Abstract
Baicalein induced cell cycle arrest and apoptosis in human lung squamous carcinoma CH27 cells: H.Z. Lee, et al.; Anticancer Res. 25, 959 (2005) Abstract
Biological properties of baicalein in cardiovascular system: Y. Huang, et al.; Curr. Drug Targets Cardiovasc. Haematol. Disord. 5, 177 (2005), (Review) Abstract
Baicalein inhibition of hydrogen peroxide-induced apoptosis via ROS-dependent heme oxygenase 1 gene expression: H.Y. Lin, et al.; Biochim. Biophys. Acta 1773, 1073 (2007) Abstract
 
 
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
 
 
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
 
 
ALX-270-244 Revised 03-Apr-08
Caffeic acid phenylethyl ester
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SYNONYMS CAPE
Phenethyl caffeiate
Caffeic acid phenethyl ester
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Anti-inflammatory Agents
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ALX-270-244-M010   10 mg 20.00 USD Add To Cart
ALX-270-244-M050   50 mg 60.00 USD Add To Cart
Product Specification
FORMULA: C17H16O4
MW: 284.3
CAS NUMBER: 115610-29-2
SOURCE/HOST: Synthetic.
PURITY: ≥97% (HPLC)
APPEARANCE: White to off-white crystalline solid.
SOLUBILITY: Soluble in DMSO, 100% ethanol, methanol, acetone or acetonitrile; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least one year after receipt when stored at –20°C.
HANDLING: Protect from light and moisture.
HAZARD: IRRITANT.

Product Description
Active component of propolis from honeybee hives, known to have anti-mitogenic, anti-carcinogenic, anti-inflammatory, and immunomodulatory properties. Potent and specific inhibitor of NF-κB activation, induced by TNF-α (Prod. No. ALX-522-008 (human) or Prod. No. ALX-522-009 (mouse)), PMA (Prod. No. ALX-445-004) and other inflammatory agents. Exhibits inhibitory activity against HIV-1 integrase (IC50=7µM). Suppresses lipid peroxidation and inhibits ornithine decarboxylase, protein tyrosine kinase and lipoxygenase activities. Induces apoptosis.
Product Specific Literature References
Hydroxylated aromatic inhibitors of HIV-1 integrase: T.R. Burke Jr., et al.; J. Med. Chem. 38, 4171 (1995) Abstract
Apoptosis and altered redox state induced by caffeic acid phenethyl ester (CAPE) in transformed rat fibroblast cells: C. Chiao, et al.; Cancer Res. 55, 3576 (1995) Abstract
Caffeic acid phenethyl ester is a potent and specific inhibitor of activation of nuclear transcription factor NF-kappa B: K. Natarajan, et al.; PNAS 93, 9090 (1996) Abstract
Inhibitory effects of caffeic acid phenethyl ester on the activity and expression of cyclooxygenase-2 in human oral epithelial cells and in a rat model of inflammation: P. Michaluart, et al.; Cancer Res. 59, 2347 (1999) Abstract
Caffeic acid phenethyl ester induces leukocyte apoptosis, modulates nuclear factor-kappa B and suppresses acute inflammation: Z. Orban, et al.; Neuroimmunomodulation 7, 99 (2000) Abstract
Caffeic acid phenethyl ester inhibits T-cell activation by targeting both nuclear factor of activated T-cells and NF-kappaB transcription factors: N. Marquez, et al.; J. Pharmacol. Exp. Ther. 308, 993 (2004) Abstract
Caffeic acid derivatives: in vitro and in vivo anti-inflammatory properties: F.M. da Cunha, et al.; Free Radic. Res. 38, 1241 (2004) Abstract
Drastic effect of several caffeic acid derivatives on the induction of heme oxygenase-1 expression revealed by quantitative real-time RT-PCR: K. Suzuki, et al.; Biofactors 28, 151 (2006) Abstract
 
 
ALX-350-027 Revised 19-Aug-08
Calphostin C
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SYNONYMS UCN-1028C
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-027-C100   100 µg 85.00 USD Add To Cart
ALX-350-027-M001   1 mg 595.00 USD Add To Cart
Product Specification
FORMULA: C44H38O14
MW: 790.8
CAS NUMBER: 121263-19-2
SOURCE/HOST: Isolated from Cladosporium cladosporioides MST-FP1798.
PURITY: ≥95% (HPLC)
APPEARANCE: Dark red solid.
SOLUBILITY: Soluble in 100% ethanol, methanol, DMSO or dimethyl formamide; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Stock solutions are stable for 3 months when stored at -20°C.
HANDLING: Protect from light.

Product Description
Potent and selective inhibitor of the protein kinase C (PKC) regulatory site of diacylglycerol and phorbol esters. At higher