MilliporeSigma™ Calbiochem™ O-GlcNAcase Inhibitor, TMG

Description

A cell-permeable, blood-brain barrier-permeant, orally active aminothiazoline that effectively increases O -GlcNAc level of cellular proteins both in cultures (EC₅₀ = 30 nM, EC_max = 200nM in PC3) in vitro and in rats

A cell-permeable, blood-brain barrier-permeant, orally active aminothiazoline that effectively increases O -GlcNAc level of cellular proteins both in cultures (EC₅₀ = 30 nM, EC_max = 200nM in PC3) in vitro and in rats (50mg/kg i.v.; 200mg/kg via drinking water ad libitum ) and mice (500mg/kg via drinking water ad libitum ) in vivo by inhibiting O-GlcNAcase/OGA-mediated O -GlcNAc cleavage in a substrate-competitive ( K _i = 21nM), time- and dose-dependent, and highly selective manner. TMG long-term treatment in murine AD model effectively prevents loss of motor neurons and reduces NFTs in brain without apparent effect on Tau hyperphosphorylation. O -GlcNAcylation is also reported to slow down heat-induced sTAB1 (TAK1-binding protein) aggregation and modulate CK2α kinase activity and substrate selectivity in vitro .

Specifications

• Color: Off-white
• Description: ≥98% by HPLC
• CAS: 1009816-48-1
• Molecular Formula: C₉H₁₆N₂O₄S
• Formula Weight: 248.3g/mol
• Solubility: DMSO or H₂O
• Content And Storage: Toxicity: Harmful, Store at -20°C, Protect from light, Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
• Form: Solid
• Quantity: 25 mg