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. Primary Target: Nur77 AMPK, Nuclear Hormone Receptor 4A/NR4A 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 CAS No: 1258275-73-8 Molecular Formula: C21H32O6 Molecular Weight: 380.48 Purity: 97% (LCMS) Appearance: Light yellow to yellow solid Solubility: DMSO: 100mg/ml Method for Determining Identity: Liquid Chromatography-Mass Spectrometry Storage and Stability: Lyophilized product is stable for 6 months after receipt at 4C. Reconstitute with DMSO. For maximum recovery of product, centrifuge the original vial prior to removing the cap.
Molecular Weight:
380.48
CAS Number:
[1258275-73-8]
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