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 (Kd = 0.14 against 5uM LKB1 binding to 5uM full-length Nur77). Shown to induce LKB1 Ser428 phosphorylation (10 & 20uM for 6h) and LKB1 nuclear-to-cytosol translocation in hepatic LO2 cells, resulting in enhanced phosphorylations of LKB1 cytosolic effectors AMPKalpha and MARK1/2/3 without affecting Nur77 transactivation activity. Daily i.p. dosing (50mg/kg) is shown to increase liver LKB1 Ser428/AMPKalpha Thr172 phosphorylations in diabetic db/db mice in vivo, effectively improving animal glucose tolerance. Also reported to lower fasting blood glucose level in STZ-treated, high fat diet-fed type II diabetic mice.
Synonyms:Ethyl-2-(2,3,4-trimethoxy-6-(1-octanoyl)phenyl)acetate, AMPK Signaling Activator XII, Liver Kinase B Activator, LKB1 Activator, MARK Signaling Activator, STK11 Activator, TR3 LBD Antagonist
Solubility (100mg/ml):DMSO. Use only fresh DMSO
Primary Target:Nur77
Molar Mass:380.5
Carbon:As Reported
Hydrogen:As Reported
Water by CHN:As Reported
Storage and Stability:Lyophilized product is stable for 6 months after receipt at 4°C. Reconstitute freshly with DMSO. For maximum recovery of product, centrifuge the original vial prior to removing the cap.
