TP-040 | O-GlcNAcase inhibitor

TP-040 chemical structure

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TP-040 (2757254-99-0) is a potent and brain-penetrant inhibitor (IC50 = 46 nM) of O-GlcNAcase (OGA).  OGA catalyzes the cleavage of O-linked N-acetylglucosamine from serine and threonine residues. On tau proteins, this leads to a less soluble and less stable protein form that is prone to aggregation.  TP-040 is an interesting new tool for studying the effects of tau protein aggregation in neurodegenerative diseases.

References/Citations:

  1. Tawada et al. (2021), Discovery of a Novel and Brain-Penetrant O-GlcNAcase Inhibitor via Virtual Screening, Structure-Based Analysis, and Rational Lead Optimization; J. Med. Chem., 53 1103
2757254-99-0, O-GlcNAcase inhibitor, O-GlcNAcase-IN-1, O-GlcNAcase-IN-1 supplier, OGA inhibitor, TP-040, TP-040 supplier, TP040
Alternate Name:
O-GlcNAcase-IN-1

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TP-040 (2757254-99-0) is a potent and brain-penetrant inhibitor (IC50 = 46 nM) of O-GlcNAcase (OGA).  OGA catalyzes the cleavage of O-linked N-acetylglucosamine from serine and threonine residues. On tau proteins, this leads to a less soluble and less stable protein form that is prone to aggregation.  TP-040 is an interesting new tool for studying the effects of tau protein aggregation in neurodegenerative diseases.

References/Citations:

  1. Tawada et al. (2021), Discovery of a Novel and Brain-Penetrant O-GlcNAcase Inhibitor via Virtual Screening, Structure-Based Analysis, and Rational Lead Optimization; J. Med. Chem., 53 1103