MilliporeSigma™ Calbiochem™ Nur77 LBD Antagonist, TMPA

Description

• A cell-permeable phenylacetate compound that blocks Nur77 (TR3) LKB1 nuclear-sequestering function by antagonizing against Nur77-LKB1 interaction via direct binding at the LKB1 LBD/ligand binding domain ( K d = 0.14 against 5μM LKB1 binding to 5μM full-length Nur77)
• Shown to induce LKB1 Ser428 phosphorylation (10 and 20μM for 6 h) and LKB1 nuclear-to-cytosol translocation in hepatic LO2 cells, resulting in enhanced phosphorylations of LKB1 cytosolic effectors AMPKα and MARK1/2/3 without affecting Nur77 transactivation activity
• Daily i.p
• dosing (50mg/kg) is shown to increase liver LKB1 Ser428/AMPKα Thr172 phosphorylations in diabetic db/db mice in vivo , effectively improving animal glucose tolerance
• Also reported to lower fasting blood glucose level in STZ- (Cat
• No
• 572201) treated, high fat diet-fed type II diabetic mice.