OGA Inhibitor

Thiamet G is a potent and selective inhibitor of O-GlcNAcase (OGA), which acts to remove O-GlcNAc from modified proteins, with K_i of 20 nM for human OGA.

Ceperognastat (LY3372689) is an orally active O-GlcNAcase (OGA) enzyme inhibitor. Ceperognastat can be used for tauopathies research, including Alzheimer’s disease.

Egalognastat (ASN90) is a selective, brain-penetrant and orally active O-GlcNAcase (OGA) enzyme inhibitor with an IC₅₀ value of 10.2 nM. Egalognastat increases O-GlcNAcylation of intracellular proteins like tau and α-synuclein, preventing their aggregation and toxicity. Egalognastat does not inhibit hexosaminidase (Hex). Egalognastat can be used for the research of neurodegenerative diseases, such as tauopathies and α-synucleinopathies (e.g., Alzheimer’s disease and Parkinson’s disease).

O-GlcNAcase-IN-6 is an orally active, blood-brain barrier-permeable O-GlcNAcase (OGA) inhibitor with an IC₅₀ of 5.4 nM. O-GlcNAcase-IN-6 inhibits OGA activity, thereby increasing the level of O-GlcNAc glycosylation in brain tissues. O-GlcNAcase-IN-6 can be used for the research of Alzheimer's disease.

NAG-thiazoline is a O-GlcNAcase inhibitor with a K_i of 180 nM. NAG-thiazoline is a potent GH20 GlcNAcase (VhGlcNAcase) inhibitor with an IC₅₀ of 11.9 μM and a K_i of 62 µM.

Hydroxyectoin (Pyrostatin A) is a competitive inhibitor of GlcNAcase, with the K_i of 1.7 μM.

O-GlcNAcase-IN-2 (compound 81) is an orally effective, blood-brain barrier-permeable OGA inhibitor (IC₅₀=4.93 nM). O-GlcNAcase-IN-2 can increase the O-GlcNAcylation level of proteins and phosphorylation of tau (p-Ser199, p-Thr205 and p-Ser396) in the OA-damaged SH-SY5Y cell model. O-GlcNAcase-IN-2 can also improve cognitive impairment in APP/PS1 mice and has potential anti-Alzheimer's disease (AD) effects.

JNJ-65355394 (Compound 28), a chemical probe, is an O-GlcNAc hydrolase (OGA) inhibitor.

rel-Ceperognastat (rel-LY3372689) (Compound Formula Ic) is a O-GlcNAcase (OGA) inhibitor that can be used to study the neurodegenerative diseases and disorders, such as Alzheimer's disease.

O-GlcNAcase-IN-4 (compound T-110) is a O-GlcNAcase inhibitor with an IC₅₀ of 11.59 nM. O-GlcNAcase-IN-4 modulates the activity of O-GlcNAcase. O-GlcNAcase-IN-4 is applicable to the research of neurodegenerative diseases and disorders, Alzheimer's disease, and tau-mediated neurodegenerative diseases or disorders.

O-GlcNAcase-IN-3 (Compound I) is an OGA inhibitor. O-GlcNAcase-IN-3 can be used for Alzheimer's Disease (AD) research.

O-GlcNAcase-IN-5 (Compound 1) is a selective O-GlcNAcase inhibitor. O-GlcNAcase-IN-5 can prevent the enzyme from removing the O-GlcNAc modification on tau protein, thus avoiding excessive phosphorylation of tau protein. O-GlcNAcase-IN-5 can be used for the research of Alzheimer's disease.