Table 3.

The available inhibitors targeting OGT

Categories	Compound	IC50 (μM)	Advantages	Disadvantages	References
Substrate and product analogs	Alloxan	18 ± 1	Cell-permeable	Potential off-target effects and general cellular toxicity	Konrad et al. (2002)
	UDP- S -GlcNAc	93 ± 15	Sub-millimolar inhibitors	Lack of cell permeability	UniProt: a worldwide hub of protein knowledge (2019)
	UDP- C-GlcNAc	41 ± 7	Sub-millimolar inhibitors	Lack of cell permeability, a weak hOGT inhibitor	Dorfmueller et al. (2011)
	C-UDP	9.0 ± 1.0	Sub-millimolar inhibitors	Lack of cell permeability	Dorfmueller et al. (2011)
	UDP-5SGlcNAc	5	Cell-permeable	Affect N-glycosylation in cells and glycan synthesis outside the cells	Gloster et al. (2011)
HTS-derived inhibitors	ST045849	53 ± 7	Highly selective and cell-permeable	Potential off-target effects and cellular toxicity	Kamigaito et al. (2014)
	OSMI-1	2.7	Cell-permeable, not alter cell surface N- or O-linked glycans, on-target activity		Ortiz-Meoz et al. (2015)
Bisubstrate inhibitor	goblin1	18	Can synergize with goblin2 to enhance inhibition	Lack of cell permeability	Borodkin et al. (2014)
	goblin2	40	Can synergize with goblin1 to enhance inhibition	Lack of cell permeability	Borodkin et al. (2014)