MilliporeSigma™ Calbiochem™ O-GlcNAcase Inhibitor, TMG

A cell-permeable, blood-brain barrier-permeant, orally active aminothiazoline that effectively increases O -GlcNAc level of cellular proteins both in cultures (EC_{50 = 30 nM, ECmax = 200nM in PC3) in vitro and in rats}

Manufacturer:  MilliporeSigma™ 110165CBC25MG

Catalog No. 11-016-5CBC25

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 (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

• CAS: 1009816-48-1
• Format: Off-white solid
• Molecular Formula: C₉H₁₆N₂O₄S
• Solubility: DMSO or H₂O

• Description: ≥98% by HPLC
• Formula Weight: 248.3g/mol
• Quantity: 25mg
• Storage Requirements: 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.