MilliporeSigma™ Calbiochem™ Nur77 LBD Antagonist, TMPA

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

Manufacturer:  MilliporeSigma™ 49291010MG

Catalog No. 49-291-010MG

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.

Specifications

• Description: 97% by HPLC
• Storage Requirements: Protect from Light
• Target Proteins: Nur77
• Formula Weight: 380.5g/mol

• Format: Off-white solid
• Quantity: 10mg
• Molecular Formula: C₂₁H₃₂O₆
• Solubility: DMSO