O-GlcNAc Transferase Inhibitors

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 TimTec assembled small targeted compound collection of over 500 compounds-analogs based on three validated O-GlcNAc Transferase inhibitors (following the results of the discovery at Department of Microbiology and Molecular Genetics, HUMS)

Reference:

Gross, B.J, Kraybill, B.C., Walker, S. Discovery of O-GlcNAc Transferase Inhibitors. Department of Microbiology and Molecular Genetics, Harvard Medical School. JACS Communications, published on Web 09/29/05; J. Am. Chem. Soc. 2005, 127, 14588-14589.

Compounds with proven activity are available from stock:

ST060266

289.67

phenyl 5-chloro-2-oxo-3-hydrobenzoxazole-3-carboxylate

ST078925

406.53

4-[(3-cyano-4-(2-thienyl)-2-5,6,7,8-tetrahydroquinolylthio)methyl]benzoic acid

ST078925 analog-substitute to validated inhibitor #6, Figure 3. of the paper

ST045849

447.00

3-(2-adamantanylethyl)-2-[(4-chlorophenyl)azamethylene]-4-oxo-1,3-thiazaperhyd roine-6-carboxylic acid

OGT inhibitor, ST045849, TT04, treatment reduces beta-cell development:

Reference:

Filhoulaud, G., et al. The hexosamine biosynthesis pathway is essential for pancreatic beta cell development. J Biol Chem. 2009 Sep 4;284(36):24583-94.