Catalog No.: PC-26967Not For Human Use, Lab Use Only.
TMPA is a specific, high-affinity Nur77 antagonist that binds directly to Nur77ligand-binding domain (LBD) with KD of 0.25 uM, antagonizes the Nur77-LKB1 interaction, induces LKB1 nuclear export to activate AMPKα.
TMPA is a specific, high-affinity Nur77 antagonist that binds directly to Nur77ligand-binding domain (LBD) with KD of 0.25 uM, antagonizes the Nur77-LKB1 interaction, induces LKB1 nuclear export to activate AMPKα. TMPA enhances rather than downregulates the phosphorylation of AMPKα in hepatic LO2 cells in both dose- and time-dependent manners. TMPA has a strong affinity for both Nur77 and LBD in the quenching experiments but not for monomeric or heterotrimeric AMPKα, AMPKβ, AMPKγ or LKB1. TMPA does not show any effect on Nur77 transactivation activity. TMPA affects subcellular localization of LKB1 through phosphorylation at Ser428 in LO2 cells. TMPA is capable of lowering blood glucose in HFD- and STZ-induced diabetic mice.
