o-glcnacase

Thiamet G is a potent, selective O-GlcNAcase inhibitor with Kiof 21 nM, while exhibiting 37, 000-fold selectivity over human lysosomal –hexosaminidase.

JNJ-65355394 is an effective O-GlcNAc hydrolase (OGA) inhibitor and an OGA chemical probe.

LY3372689 (Formulaic Ia) is an orally active O-GlcNAcase (OGA) enzyme inhibitor targeting tau protein-based disorders, including Alzheimer's disease.

O-GlcNAcase-IN-2 (compound 81) is an orally active, brain-penetrant inhibitor of O-GlcNAcase, demonstrating an IC50 value of 4.93 nM. It has shown potential in elevating protein O-GlcNAcylation levels and promoting phosphorylation of tau (p-Ser199, p-Thr205, p-Ser396) in an OA-impacted SH-SY5Y cell model. Additionally, O-GlcNAcase-IN-2 has been observed to ameliorate cognitive deficits in APP PS1 mice, suggesting its potential utility in combating Alzheimer's disease (AD).

O-GlcNAcase-IN-1 is a potent and novel inhibitor of O-GlcNAcase(OGA) with an IC 50 value of 46 nM.

O-GlcNAcase-IN-4 is an inhibitor of O-GlcNAcase. It holds potential for researching neurodegenerative diseases and disorders, including Alzheimer's disease [1].

N-Acetyl-D-Glucosamine (NAG) is a monosaccharide derivative of glucose. It is released by the action of O-GlcNAcase, in mammalian systems from proteins that have been post-translationally modified with O-GlcNAc.

MK-8719 is a highly potent and selective inhibitor of O-GlcNAcase (OGA) [hOGA], with a Ki value of 7.9 nM.

GlcNAcstatin, a selective glucoimidazole-based inhibitor of bacterial O-GlcNAcase, exhibits a K_i value of 4.6 pM and demonstrates a specificity that is 100,000-fold greater than that for HexA B [1].

NAG-thiazoline (GlcNAc-thiazoline) is an O-GlcNAcase inhibitor with Ki value of 180 nM. It is active against V. campbellii with MIC value of 0.5 μM.

(Z)-PUGNAc, a potent O-GlcNAcase inhibitor more active than (E)-PUGNAc, removes O-GlcNAc from proteins (peptide O-GlcNAc-β-N-acetylaminoglucosidase) and can be used to increase levels of O-GlcNAc on nuclear and cytoplasmic proteins in vivo.

ASN90 is a specific, orally active inhibitor of the O-GlcNAcase (OGA) enzyme, demonstrating an IC50 of 10.2 nM. It is utilized in the research of neurodegenerative disorders including tauopathies and α-synucleinopathies [1].