Glycosyltransferase Inhibitor

Benzyl-α-GalNAc is a potent O-glycosylation inhibitor. Benzyl-α-GalNAc effectively inhibits the proliferation and activation of LX-2 cells and suppresses the expression of collagen I/III, which has good potential for investigation in liver fibrosis. Benzyl-α-GalNAc also significantly enhances the anti-tumour activity of 5-Fluorouracil (HY-90006) (e.g. pancreatic cancer) by inhibiting O-glycosylation.

2F-Peracetyl-Fucose (1,3,4-Tri-O-acetyl-2-deoxy-2-fluoro-L-fucopyranos) acts as a potent fucosyltransferase (FUT) inhibitor.

SGN-2FF is a potent and orally active inhibitor of fucosylation, directly inhibits fucosyltransferase activity. SGN-2FF possesses antitumor activity.

SU0268 is a potent and specific inhibitor of 8-Oxoguanine DNA glycosylase 1 (OGG1). SU0268 regulates inflammatory responses during Pseudomonas aeruginosa infection.

T3Inh-1 is a potent and selective inhibitor of ppGalNAc-T3 (IC₅₀=7 μM). T3Inh-1 reduces FGF23 hormone levels in both tissue cells and mice, without causing any toxic side effects. T3Inh-1 also prevents breast cancer cells. The enzyme ppGalNAc-T3 is implicated in at least two medically important pathways: cancer metastasis and stabilization of FGF23 (regulates phosphate levels in the bloodstream).

AG-205 is a progesterone receptor membrane component 1 (PGRMC1) antagonist and CGT inhibitor, with an IC₅₀ of 50 μM against rat CGT. AG-205 exhibits antimitotic, antimigratory and anti-invasive activities. AG-205 increases the expression of genes encoding cholesterol biosynthesis pathway or steroidogenic enzymes. AG-205 promotes the regulation of cell cycle by apoptosis and reduces the migratory and invasive capacities of ovarian and breast cancer cells. AG-205 can be used in research related to renal cancer and breast cancer.

yGsy2p-IN-1 is a potent inhibitor for yeast glycogen synthase 2 (yGsy2p). yGsy2p-IN-1 is a competitive human glycogen synthase 1 (hGYS1) inhibitor with an IC₅₀ of 2.75 μM and a K_i of 1.31 μM for wild-type hGYS1. yGsy2p-IN-H23 a pyrazole inhibitor, is used for glycogen storage diseases (GSDs).

PST3.1a is an orally active and brain-penetrant N-acetylglucosamine glycosyltransferase (MGAT5) inhibitor with a human IC₅₀ of 2 µM. PST3.1a inhibits TGFβR and FAK signaling pathway activity. PST3.1a alters β1,6-GlcNAc N-glycans and microtubule/microfilament integrity, increases OLIG2 expression, and inhibits proliferation, migration, invasiveness, and clonogenic capacities of glioblastoma initiating cells. PST3.1a reduces invasive and proliferative capacity of glioblastoma initiating cells in orthotopic graft models, increases overall survival of orthotopic graft model mice. PST3.1a blunts MGAT5 overexpression, decreases renal fibrosis via collagen 1, collagen 4, and galectin 3 downregulation in a rat chronic kidney disease model. PST3.1a can be used for the research of glioblastoma multiforme and chronic kidney disease.

β-1,4-GALT1-IN-1 (Compound 6) is a β-1,4-GALT1 inhibitor, with an IC₅₀ value of 6.2 μM. β-1,4-GALT1-IN-1 can be used in many pathology investigations such as cancer, autoimmune diseases and viral infections.

ST-IN-1 (compound (R)-1) is a selective ST inhibitor (K_i=70 nM, rat a-2,6-ST; K_i=19 nM, hST6GAL1) with antitumor activity. ST-IN-1 inhibits tumor growth and metastasis by delipidating the surface of tumor cells.

GYS1-IN-1 (compound 783) is a glycogen synthase 1(GYS1) inhibitor. GYS1-IN-1 can be used for the study of GYS1 -mediated disease, such as Gaucher and Fabry diseases.

ppGalNAc-T2-IN-1 is a polypeptide N-acetylgalactosaminyltransferase 2 (ppGalNAc-T2) inhibitor with an IC₅₀ of 7.11 μM. ppGalNAc-T2-IN-1 is applicable for research on metabolic and neurodevelopmental disorders.

2-Deoxy-2-fluoro-L-fucose (2-Fluorofucose) GMP is a fucosyltransferase inhibitor that inhibits core fucosylation modification in cells. 2-Deoxy-2-fluoro-L-fucose GMP promotes the production of defucosylated IgG1 antibodies in IgG1-expressing cell culture systems; it regulates the levels of inflammatory cytokines such as IL-1β, IL-6 and TGF-β in human induced pluripotent stem cell-derived microglia. 2-Deoxy-2-fluoro-L-fucose GMP can be used in the research of related diseases including dengue fever and Alzheimer's disease.

Glycosyltransferase-IN-1 (compound 5m) is a potent glycosyltransferase inhibitor, with an IC₅₀ of 82.8 μM. Glycosyltransferase-IN-1 shows antibacterial activity, with MIC values of 6 μg/mL for MSSA, MRSA, B. subtilis and 12 μg/mL for E. coli.

Glycosyltransferase-IN-2 (Compound 20) is a Glycosyltransferase inhibitor. Glycosyltransferase-IN-2 has a broad-spectrum anticoronavirus activity with IC₅₀s of 11.3, 5.5 and ~16.2 μM for MHV, HCoV-NL63 and SARS-CoV-2, respectively. Glycosyltransferase-IN-2 interferes with the coronavirus infectivity, alters viral protein glycosylation with inhibition of interaction with the ACE2 receptor or SC-VLP secretion, and inhibits RNA replication. Glycosyltransferase-IN-2 can be used for coronavirus infections research.

SGN-2FF (Standard) is the analytical standard of SGN-2FF (HY-107366). This product is intended for research and analytical applications. SGN-2FF is a potent and orally active inhibitor of fucosylation, directly inhibits fucosyltransferase activity. SGN-2FF possesses antitumor activity.