OGT Inhibitor

OSMI-1 is a cell-permeable O-GlcNAc transferase (OGT) inhibitor with an IC₅₀ value of 2.7 μM. OSMI-1 inhibits protein O-linked N-acetylglucosamine (O-GlcNAcylation) in several mammalian cell lines without qualitatively altering cell surface N- or O-linked glycans.

OSMI-4 is a low nanomolar O-GlcNAc transferase (OGT) inhibitor, with an EC₅₀ of 3 μM in cells.

ST045849 (OGT-IN-2) is a small-molecule OGT inhibitor with an IC₅₀ of 30 μM against sOGT and 53 μM against ncOGT. ST045849 is applicable to research on metabolism-related diseases.

Dammarenediol II is a ginsenoside precursor. Dammarenediol II reduces the activity of O-GlcNAc transferase (OGT) and downregulates the global O-GlcNAcylation level. Dammarenediol II inhibits the phosphorylation of Akt, mTOR and GSK3β. Dammarenediol II inhibits human carboxylesterase activity, VEGF-induced ROS production, stress fiber formation and vascular endothelial cadherin disruption. Dammarenediol II promotes cell apoptosis (apoptosis), increases the levels of cleaved PARP1 and p53, and inhibits retinal microvascular leakage. Dammarenediol II can be used in studies related to liver cancer and diabetic retinopathy.

OGT-IN-1 (Compound 5) is a potent OGT inhibitor. OGT-IN-1 inhibits sOGT and ncOGT with IC₅₀s of 27 and 10 μM, respectively.

OSMI-2 (Compound 1b) is a cell-permeable O-linked N-acetylglucosamine transferase (OGT) inhibitor. Cells contain a large nuclear pool of partially spliced OGT transcript, and OSMI-2 increases detained intron splicing in cells.

(Rac)-OSMI-1 is the racemate of OSMI-1. OSMI-1 is a cell-permeable O-GlcNAc transferase (OGT) inhibitor with an IC₅₀ value of 2.7 μM. OSMI-1 inhibits protein O-linked N-acetylglucosamine (O-GlcNAcylation) in several mammalian cell lines without qualitatively altering cell surface N- or O-linked glycans.

OGT-IN-4 (compound 4a) is an O-GlcNAc transferase (OGT) inhibitor with a K_d of 8 nM. OGT-IN-4 can be utilized in OGT related research.

OSMI-3 (Compound 2b) is a potent, long-lasting, and cell-permeable O-linked N-acetylglucosamine transferase (OGT) inhibitor. Cells contain a large nuclear pool of partially spliced OGT transcript, and OSMI-3 increases detained intron splicing in cells.

Ac4-5SGlcNAc is an O-GlcNAc transferase (OGT) inhibitor. Ac4-5SGlcNAc converts intracellularly to UDP-5SGlcNAc, which competes with native UDP-GlcNAc (HY-148596) to block OGT catalytic activity, reduces cellular UDP-GlcNAc pools, and limits global protein O-GlcNAcylation. Ac4-5SGlcNAc reduces OGA levels via feedback, alters lectin signal intensities and glycan-related band masses. Ac4-5SGlcNAc can be used for the research of breast cancer.

BZX2 is an irreversible covalent inhibitor of O-GlcNAc transferase (OGT) with an IC₅₀ of <10 µM. BZX2 is cell-permeable but exhibits multiple off-target effects.