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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


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Description

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

Specifications

97% by HPLC
Protect from Light
Nur77
380.5g/mol
Off-white solid
10mg
C21H32O6
DMSO
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