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Hypothemycin

MEK inhibitor
 
ALX-380-116-C250 250 µg 365.00 USD
 
ALX-380-116-M001 1 mg 1,030.00 USD
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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. Hypothemycin inhibited the growth of HT29 and HCT116 cells in serum-free defined medium. IC50 at 0.078 mM and 0.90 mM, respectively.
Hypothemycin concurrently inhibitis Kit- and FcεRI-mediated signaling.

Product Specification

Formula:C19H22O8
 
MW:378.4
 
Source:Isolated from Phoma sp.
 
CAS:76958-67-3
 
Purity:≥97% (HPLC)
 
Identity:Determined by 1H-NMR.
 
Appearance:White to off-white solid.
 
Solubility:Soluble in DMSO or acetone; insoluble in methanol or water.
 
Shipping:Ambient
 
Short Term Storage:+4°C
 
Long Term Storage:-20°C
 
Use/Stability:Stable for at least 1 year after receipt when stored at -20°C.
 
Handling:After reconstitution protect from light at -20°C.
 
380-116
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380-116

Product Literature References

Hypothemycin inhibits tumor necrosis factor-α production by tristetraprolin-dependent down-regulation of mRNA stability in lipopolysaccharide-stimulated macrophages: K.H. Park, et al.; Int. Immunopharmacol. 29, 863 (2015), Application(s): Effects of hypothemycin on tumor necrosis factor-α production in macrophages, Abstract;
The resorcylic acid lactone hypothemycin selectively inhibits the mitogen-activated protein kinase kinase-extracellular signal-regulated kinase pathway in cells: H. Fukazawa, et al.; Biol. Pharm. Bull. 33, 168 (2010), Abstract;
Concurrent inhibition of kit- and FcepsilonRI-mediated signaling: coordinated suppression of mast cell activation: B.M. Jensen, et al.; J. Pharmacol. Exp. Ther. 324, 128 (2008), Abstract;
Chemistry and biology of resorcylic acid lactones: N. Winssinger & S. Barluenga; Chem. Commun. (Camb.) 1, 22 (2007), (Review), Abstract;
Targeted covalent inactivation of protein kinases by resorcylic acid lactone polyketides: A. Schirmer, et al.; PNAS 103, 4234 (2006), Abstract; Full Text
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;
Resorcylic acid lactones: naturally occurring potent and selective inhibitors of MEK: A. Zhao, et al.; J. Antibiot. 52, 1086 (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;
Revised structure and stereochemistry of hypothemycin: T. Agatsuma et al.; Chem. Pharm. Bull. 41, 373 (1993),
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),
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),

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