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MAPK Pathway Inhibitors
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ALX-350-299 Revised 25-May-07
S14-95
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Other Natural Products for Inflammation Research
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ALX-350-299-MC05   0.5 mg 250.00 USD Add To Cart
Product Specification
FORMULA: C28H34O5
MW: 450.6
SOURCE/HOST: Isolated from Penicillium sp.
PURITY: ≥95% (HPLC)
APPEARANCE: Yellow powder.
SOLUBILITY: Soluble in methanol.
SHIPPING: AMBIENT
SHORT TERM STORAGE: +4°C
LONG TERM STORAGE: -20°C

Product Description
Potent inhibitor of cytokine-induced activation of STAT1α leading to the inhibition of inducible expression of proinflammatory enzymes (COX-2, iNOS (NOS II)) and cytokines (TNF-α).
Product Specific Literature References
S14-95, a novel inhibitor of the JAK/STAT pathway from a Penicillium species: G. Erkel, et al.; J. Antibiot. 56, 337 (2003) Abstract
Sporogen, S14-95, and S-curvularin, three inhibitors of human inducible nitric-oxide synthase expression isolated from fungi: Y. Yao, et al.; Mol. Pharmacol. 63, 383 (2003) Abstract; Full Text
Further Categories Containing This Product:
NOS Inhibitors (NOS Induction & Enzyme Activity) • MAPK Pathway Inhibitors • Natural Products - Protein Kinase Inhibitors • Natural Products - Nitric Oxide Pathway Modulators • COX Inhibitors
 
 
ALX-350-346 Revised 12-Sep-08
Silybin
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SYNONYMS Silibinin
2,3-Dihydro-3-(4-hydroxy-3-methoxyphenyl)-2-(hydroxymethyl)-6-(3,5,7-trihydroxy-4-oxobenzopyran-2-yl)benzodioxin
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Chemopreventive Agents
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-346-G001   1 g 10.00 USD Add To Cart
ALX-350-346-G005   5 g 35.00 USD Add To Cart
Product Specification
FORMULA: C25H22O10
MW: 482.4
CAS NUMBER: 22888-70-6; 65666-07-1
MERCK INDEX: 14: 8532
RTECS: DJ2981770
SOURCE/HOST: Originally isolated from Silybum marianum.
PURITY: ≥98%
APPEARANCE: White to light yellow solid.
SOLUBILITY: Soluble in 100% ethanol (0.1mg/ml), DMSO (10mg/ml), dimethyl formamide (20mg/ml), acetone or methanol; 0.5mg/ml soluble in a 1:9 solution of dimethyl formamide:PBS (pH 7.2) (dilute the dimethyl formamide solution with PBS).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: We do not recommend storing aqueous solutions for more than one day.
HAZARD: IRRITANT.

Product Description
Mixture of silybin A and silybin B. Major active constituent of silymarin. Anti-inflammatory, cytoprotective and anti-cancer compound. Shows chemopreventive effect against skin cancer. Inhibits mitogen-activated protein kinase (MAPK). Inhibits P-glycoprotein (Pgp)-mediated cellular efflux. Inhibits cytochrome P450 enzymes. Apoptosis inducer. Blocks the production of superoxide in Kupffer cells (EC50=100µM). Antioxidant. Free radical scavenger.
Product Specific Literature References
[On the chemistry of silymarin (silybin), the active principle of the fruits from Silybum marianum (L.) Gaertn. (Carduus marianus L.)]: H. Wagner, et al.; Arzneimittelforschung 18, 688 (1968) Abstract
Inhibition of Kupffer cell functions as an explanation for the hepatoprotective properties of silibinin: C. Dehmlow, et al.; Hepatology 23, 749 (1996) Abstract; Full Text
Silibinin decreases prostate-specific antigen with cell growth inhibition via G1 arrest, leading to differentiation of prostate carcinoma cells: implications for prostate cancer intervention: X. Zi & R. Agarwal; PNAS 96, 7490 (1999) Abstract; Full Text
The flavanolignan silybin and its hemisynthetic derivatives, a novel series of potential modulators of P-glycoprotein: M. Maitrejean, et al.; Bioorg. Med. Chem. Lett. 10, 157 (2000) Abstract
Silibinin inhibits constitutive and TNFalpha-induced activation of NF-kappaB and sensitizes human prostate carcinoma DU145 cells to TNFalpha-induced apoptosis: S. Dhanalakshmi, et al.; Oncogene 21, 1759 (2002) Abstract; Full Text
Silibinin upregulates the expression of cyclin-dependent kinase inhibitors and causes cell cycle arrest and apoptosis in human colon carcinoma HT-29 cells: C. Agarwal, et al.; Oncogene 22, 8271 (2003) Abstract; Full Text
Epidermal growth factor receptor mediates silibinin-induced cytotoxicity in a rat glioma cell line: L. Qi, et al.; Cancer Biol. Ther. 2, 526 (2003) Abstract; Full Text
Silibinin down-regulates survivin protein and mRNA expression and causes caspases activation and apoptosis in human bladder transitional-cell papilloma RT4 cells: A.K. Tyagi, et al.; BBRC 312, 1178 (2003) Abstract
Silibinin causes cell cycle arrest and apoptosis in human bladder transitional cell carcinoma cells by regulating CDKI-CDK-cyclin cascade, and caspase 3 and PARP cleavages: A. Tyagi, et al.; Carcinogenesis 25, 1711 (2004) Abstract; Full Text
Silibinin protects against photocarcinogenesis via modulation of cell cycle regulators, mitogen-activated protein kinases, and Akt signaling: G. Mallikarjuna, et al.; Cancer Res. 64, 6349 (2004) Abstract; Full Text
Silibinin up-regulates DNA-protein kinase-dependent p53 activation to enhance UVB-induced apoptosis in mouse epithelial JB6 cells: S. Dhanalakshmi, et al.; J. Biol. Chem. 280, 20375 (2005) Abstract; Full Text
Silibinin inhibits invasion of oral cancer cells by suppressing the MAPK pathway: P.N. Chen, et al.; J. Dent. Res. 85, 220 (2006) Abstract; Full Text
Pilot study of oral silibinin, a putative chemopreventive agent, in colorectal cancer patients: silibinin levels in plasma, colorectum, and liver and their pharmacodynamic consequences: C. Hoh, et al.; Clin. Cancer Res. 12, 2944 (2006) Abstract; Full Text
Silibinin prevents UV-induced HaCaT cell apoptosis partly through inhibition of caspase-8 pathway: L.H. Li, et al.; Biol. Pharm. Bull. 29, 1096 (2006) Abstract; Full Text
Silibinin inhibits UVB- and epidermal growth factor-induced mitogenic and cell survival signaling involving activator protein-1 and nuclear factor-kappaB in mouse epidermal JB6 cells: R.P. Singh, et al.; Mol. Cancer Ther. 5, 1145 (2006) Abstract; Full Text
Silibinin activates p53-caspase 2 pathway and causes caspase-mediated cleavage of Cip1/p21 in apoptosis induction in bladder transitional-cell papilloma RT4 cells: evidence for a regulatory loop between p53 and caspase 2: A. Tyagi, et al.; Carcinogenesis 27, 2269 (2006) Abstract; Full Text
Silibinin inhibits constitutive activation of Stat3, and causes caspase activation and apoptotic death of human prostate carcinoma DU145 cells: C. Agarwal, et al.; Carcinogenesis 28, 1463 (2007) Abstract
Effects and mechanisms of silibinin on human hepatoma cell lines: J.J. Lah, et al.; World J. Gastroenterol. 13, 5299 (2007) Abstract; Full Text
Silibinin suppresses PMA-induced MMP-9 expression by blocking the AP-1 activation via MAPK signaling pathways in MCF-7 human breast carcinoma cells: S.O. Lee, et al.; BBRC 354, 165 (2007) Abstract
Immunosuppressive effect of silibinin in experimental autoimmune encephalomyelitis: K. Min, et al.; Arch. Pharm. Res. 30, 1265 (2007) Abstract
Silibinin sensitizes human glioma cells to TRAIL-mediated apoptosis via DR5 up-regulation and down-regulation of c-FLIP and survivi: Y.G. Son, et al.; Cancer Res. 67, 8274 (2007) Abstract
Silibinin impairs constitutively active TGFalpha-EGFR autocrine loop in advanced human prostate carcinoma cells: A. Tyagi, et al.; Pharm. Res. Epub ahead of print, (2008) Abstract
Further Categories Containing This Product:
Free Radical Scavengers • Flavanones • MAPK Pathway Inhibitors • Cytochrome P450 [CYP450] / Related Products • Natural Products - Antioxidants • MDR Inhibitors • P-glycoprotein [Pgp] / Related Products • Natural Products - Anti-inflammatory Agents • Antitumor Agents (Enzyme Inhibitors)
 
 
ALX-380-116 Revised 07-Apr-08
Hypothemycin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Antifungal
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ALX-380-116-C250   250 µg 140.00 USD Add To Cart
ALX-380-116-M001   1 mg 420.00 USD Add To Cart
Product Specification
FORMULA: C19H22O8
MW: 378.4
CAS NUMBER: 76958-67-3
SOURCE/HOST: Isolated from Phoma sp.
PURITY: ≥98% (HPLC)
APPEARANCE: Off-white solid.
SOLUBILITY: Soluble in DMSO or acetone; insoluble in methanol or water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Exhibits antifungal and cytotoxic activity against some tumor cell lines partly attributed to inhibition of Ras-inducible genes. Inhibits proliferation of mouse and human T cells and modulates production of cytokines during T cell activation. Facilitates the ubiquitinylation process of cyclin D1. Has been identified as a potent and selective inhibitor of threonine/tyrosine-specific kinase, MEK, and other protein kinases that contain a conserved cysteine residue in the ATP-binding site in both in vitro and in vivo studies.
Product Specific Literature References
Metabolites of pyrenomycetes XIII: Structure of (+) hypothemycin, an antibiotic macrolide from hypomyces trichothecoides: M.S.R. Nair & S.T. Carey; Tetrahedron Lett. 21, 2011 (1980)
Metabolites of pyrenomycetes. XIV: Structure and partial stereochemistry of the antibiotic macrolides hypothemycin and dihydrohypothemycin: M.S.R. Nair, et al.; Tetrahedron 37, 2445 (1981)
Revised structure and stereochemistry of hypothemycin: T. Agatsuma et al.; Chem. Pharm. Bull. 41, 373 (1993)
Antitumor efficacy of hypothemycin, a new Ras-signaling inhibitor: H. Tanaka, et al.; Jpn. J. Cancer Res. 90, 1139 (1999) Abstract
Hypothemycin inhibits the proliferative response and modulates the production of cytokines during T cell activation: R. Camacho, et al.; Immunopharmacology 44, 255 (1999) Abstract
Suppression of oncogenic transformation by hypothemycin associated with accelerated cyclin D1 degradation through ubiquitin-proteasome pathway: H. Sonoda, et al.; Life Sci. 65, 381 (1999) Abstract
Resorcylic acid lactones: naturally occurring potent and selective inhibitors of MEK: A. Zhao, et al.; J. Antibiot. 52, 1086 (1999) Abstract
Targeted covalent inactivation of protein kinases by resorcylic acid lactone polyketides: A. Schirmer, et al.; PNAS 103, 4234 (2006) Abstract; Full Text
Chemistry and biology of resorcylic acid lactones: N. Winssinger, et al.; Chem. Commun. (Camb). 1, 22 (2007), (Review) Abstract
Further Categories Containing This Product:
MAPK Pathway Inhibitors • Antibiotics - Protein Kinase Inhibitors • Tyrosine Kinase Inhibitors • Antitumor Agents (DNA Interaction & Gene Regulation) • Antitumor Antibiotics • Antibiotics - Proteasome / Ubiquitin Modulators • Ubiquitination Other Products • CDKs & Cyclins Other Products • Ras Signalling Pathway Other Products
 
 
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
Further Categories Containing This Product:
MAPK Pathway Inhibitors • Hypoxia-inducible Factor [HIF] / Related Products • VEGFs & VEGF-Rs Other Products • Natural Products for Angiogenesis Research • Natural Products - Protein Kinase Inhibitors • Natural Products - Chemopreventive Agents • Natural Products - Antitumor Reagents • Antitumor Agents (Anti-proliferative) • Natural Products - Apoptosis Inducers & Inhibitors • Natural Products - Antioxidants • Antitumor Agents (Enzyme Inhibitors)
 
 
ALX-385-023 Revised 04-Jan-08
PD 98,059
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SYNONYMS 2'-Amino-3'-methoxyflavone
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY MAPK Pathway Inhibitors
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ALX-385-023-M001   1 mg 10.00 USD Add To Cart
ALX-385-023-M005   5 mg 35.00 USD Add To Cart
ALX-385-023-M010   10 mg 60.00 USD Add To Cart
ALX-385-023-M100   100 mg 490.00 USD Add To Cart
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Product Specification
FORMULA: C16H13NO3
MW: 267.3
CAS NUMBER: 167869-21-8
SOURCE/HOST: Synthetic.
PURITY: ≥95%
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in anhydrous DMSO (25mg/ml), methanol or dichloromethane; slightly soluble in 100% ethanol (0.6mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Potent, cell permeable and selective inhibitor of MEK (MAP kinase kinase). Blocks the activity of MEK and thereby inhibits the phosphorylation and activation of MAP kinase.
Product Specific Literature References
PD 098059 is a specific inhibitor of the activation of mitogen- activated protein kinase kinase in vitro and in vivo: D.R. Alessi, et al.; J. Biol. Chem. 270, 27489 (1995) Abstract; Full Text
A synthetic inhibitor of the mitogen-activated protein kinase cascade: D.T. Dudley, et al.; PNAS 92, 7686 (1995) Abstract
Negative feedback regulation and desensitization of insulin- and epidermal growth factor-stimulated p21ras activation: W.J. Langlois, et al.; J. Biol. Chem. 270, 25320 (1995) Abstract; Full Text
Inhibition of MAP kinase kinase blocks the differentiation of PC-12 cells induced by nerve growth factor: L. Pang, et al.; J. Biol. Chem. 270, 13585 (1995) Abstract; Full Text
Desensitization of Ras activation by a feedback disassociation of the SOS-Grb2 complex: S.B. Waters, et al.; J. Biol. Chem. 270, 20883 (1995) Abstract; Full Text
A phosphatidylinositol 3-kinase inhibitor induces a senescent-like growth arrest in human diploid fibroblast: M. Tresini, et al.; Cancer Res. 58, 1 (1998) Abstract
Inhibition of T cell activation by pharmacologic disruption of the MEK1/ERK MAP kinase or calcineurin signaling pathways results in different modulation of cytokine production: F.J. Dumont, et al.; J. Immunol. 160, 2579 (1998) Abstract
IL-4-induced priming of human intestinal mast cells for enhanced survival and Th2 cytokine generation is reversible and associated with increased activity of ERK1/2 and c-Fos: A. Lorentz, et al.; J. Immunol. 174, 6751 (2005) Abstract; Full Text
Further Categories Containing This Product:
Flavones
 
 
ALX-430-142 Revised 30-Nov-06
Locostatin
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SYNONYMS UIC-1005
(4S)-3-[(E)-But-2-enoyl]-4-benzyl-2-oxazolidinone
(4S)-3-[(E)-1-Oxo-2-butenyl]-4-(phenylmethyl)-2-oxazolidinone
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY MAPK Pathway Inhibitors
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ALX-430-142-M005   5 mg 80.00 USD Add To Cart
Product Specification
FORMULA: C14H15NO3
MW: 245.3
PURITY: ≥95%
APPEARANCE: White solid.
SOLUBILITY: Soluble in DMSO (10mg/ml) or methanol (50mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: HARMFUL. MAY BE MUTAGENIC.
IDENTITY: Identity determined by 1H-NMR and MS.

Product Description
Cell permeable, potent inhibitor of interaction of Raf kinase inhibitor protein (RKIP) with Raf1 kinase. Blocks eukaryotic cell migration (IC50=14µM for inhibition of wound closure in MDCK cell monolayers). Inhibitor of early development in frog embryos and tissue dynamics in embryonic explants. Displays no antibacterial activity.
Product Specific Literature References
A non-antibacterial oxazolidinone derivative that inhibits epithelial cell sheet migration: K.T. Mc Henry, et al.; ChemBioChem 3, 1105 (2002) Abstract
A chemical inhibitor reveals the role of Raf kinase inhibitor protein in cell migration: S. Zhu, et al.; Chem. Biol. 12, 981 (2005) Abstract
A role for RKIP in cell motility: W.M. Bement; Chem. Biol. 12, 953 (2005) Abstract
Sustained activation of Src-family tyrosine kinases by ischemia: A potential mechanism mediating extracellular signal-regulated kinase cascades in hippocampal dentate gyrus: J. Guo, et al.; Neuroscience 143, 827 (2006) Abstract
Further Categories Containing This Product:
Raf / Related Products
 
 
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