o-glcnac

OSMI-1 is an O-GlcNAc transferase (OGT) inhibitor (IC50=2.7 μM) that is orally active and cell-permeable. OSMI-1 inhibits protein O-GlcNA acetylation without qualitatively altering cell-surface N- or O- linked glycans.

O-GlcNAcase-IN-5 (Compound 1) is a selective inhibitor of O-GlcNAcase. It prevents this enzyme from removing O-GlcNAc modifications from tau proteins, thereby inhibiting excessive phosphorylation of tau proteins. O-GlcNAcase-IN-5 is applicable in Alzheimer's disease research.

O-GlcNAcase-IN-3 (Compound I) is an OGA inhibitor useful for Alzheimer's disease (AD) research.

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].

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).

OSMI-4 is a low nanomolar O-GlcNAc transferase (OGT) inhibitor (EC50 of 3 μM in cells) that can be used to study OGT inhibition in different human cell lines.

OSMI-3 is a potent and cell-permeable inhibitor of O-GlcNAc transferase (OGT) for the study of cancer and cardiovascular disease.

LY3372689 (Formulaic Ia) is an oral, highly selective, CNS-permeable O-GlcNAcase (OGA) inhibitor. LY3372689 exerts a neuroprotective effect by inhibiting OGA enzymatic activity, increasing the O-GlcNAc glycosylation level of tau protein, and thereby reducing abnormal tau phosphorylation and the formation of neurofibrillary tangles. LY3372689 can be used in research on tau-related diseases, including Alzheimer’s disease.

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

OGT inhibitor 4a (OGT-IN-4) is a potent, selective O-GlcNAc transferase (OGT) inhibitor with a Kd of 8 nM, targeting the uridine-binding pocket of OGT. OGT inhibitor 4a can be used in research on O-GlcNAc modification, tumors, and neurological and immune diseases.

(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.

Thiamet G is a potent O-GlcNAcase inhibitor (Ki=20 nM) with selectivity. The role of O-GlcNAcase is to remove O-GlcNAc from the modified protein.

BZX1 is an O-Iinked N-acetylglucosaminyltransferase inhibitor, which can be used to study abnormal cell differentiation and cartilage degeneration.

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.

OGT-IN-2 is a potent O-GlcNAc transferase (OGT) inhibitor. OGT-IN-2 inhibits sOGT and ncOGT with IC50 values of 30 μM and 53 μM, respectively[1]. OGT-IN-2 can be used for the research of articular diseases[1].

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

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.

UDP-GlcNAc Disodium Salt (UDP-α-D-N-Acetylglucosamine Disodium Salt) is a nucleotide sugar synthesized from glucose through the hexosamine biosynthetic pathway (HBP).

Histone H2B (108-125) is a peptide fragment of histone H2B that corresponds to amino acid residues 109-126 of the human histone H2B sequence. It contains an N-terminal biotinylated lysine followed by a tryptophan linker. Histone H2B can be modified by addition of an O-linked N-acetylglucosamine (GlcNAc) moiety to the serine residue at position 112, which promotes monoubiquitination of the lysine at position 120.1 Both of these modifications are associated with active transcription. Histone H2B also has lysine residues at positions 108, 116, and 120 that are subject to acetylation.2References1. Fujiki, R., Hashiba, W., Sekine, H., et al. GlcNAcylation of histone H2B facilitates its monoubiquitination. Nature 480(7378), 557-560 (2011).2. Portela, A., and Esteller, M. Epigenetic modifications and human disease. Nat. Biotechnol. 28(10), 1057-1068 (2010). Histone H2B (108-125) is a peptide fragment of histone H2B that corresponds to amino acid residues 109-126 of the human histone H2B sequence. It contains an N-terminal biotinylated lysine followed by a tryptophan linker. Histone H2B can be modified by addition of an O-linked N-acetylglucosamine (GlcNAc) moiety to the serine residue at position 112, which promotes monoubiquitination of the lysine at position 120.1 Both of these modifications are associated with active transcription. Histone H2B also has lysine residues at positions 108, 116, and 120 that are subject to acetylation.2 References1. Fujiki, R., Hashiba, W., Sekine, H., et al. GlcNAcylation of histone H2B facilitates its monoubiquitination. Nature 480(7378), 557-560 (2011).2. Portela, A., and Esteller, M. Epigenetic modifications and human disease. Nat. Biotechnol. 28(10), 1057-1068 (2010).

PG 34 is a structural analogue of OSMI-1 and a weak inhibitor of O-GlcNAc translocase (OGT) with an IC50 value of 68 μM.

(Rac)-OSMI-1 is a racemate of OSMI-1. OSMI-1 is an inhibitor of O-GlcNAc transferase (OGT) (IC50: 2.7 μM). OSMI-1 inhibits protein O-linked N-acetylglucosaminoglycans (O-GlcNAcylation) in mammalian cell lines and does not qualitatively alter cell surface N- or O-linked glycans.

BZX2 is a novel inhibitor of O-GlcNAc transferase (OGT) activity.

UDP-3-O-acyl-GlcNAc (UDP-3-O-(3-hydroxytetradecanoyl)-N-acetylglucosamine), an E. coli metabolite, is involved in the 3-deoxy-D-manno-octulosonate (KDO) biosynthesis pathway [1].