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TP-040 is an O-GlcNAcase (OGA) inhibitor (IC50 = 46 nM).1 It is selective for OGA over β-hexosaminidase (IC50 = >10 µM) and a panel of 277 kinases (IC50s = >1 µM for all). TP-040 increases the levels of O-GlcNAcylated proteins in SH-SY5Y neuroblastoma cells (EC50 = 450 nM).
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1. Discovery of a novel and brain-