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Product Name | Nur77 LBD Antagonist, TMPA |
Description | Purity ~97% (HPLC). 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. Solubility: DMSO Primary Target: Nur77 Molar Mass: 380.5 |
Size | 10mg |
Concentration | n/a |
Applications | n/a |
Other Names | Nur77 LBD Antagonist, TMPA (AMPK Signaling Activator XII, Liver Kinase B Activator, LKB1 Activator, MARK Signaling Activator, STK11 Activator, TR3 LBD Antagonist, Ethyl-2-(2,3,4-trimethoxy-6-(1-octanoyl)phenyl)acetate) |
Gene, Accession, CAS # | n/a |
Catalog # | 217604 |
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Order / More Info | Nur77 LBD Antagonist, TMPA from UNITED STATES BIOLOGICAL |
Product Specific References | n/a |
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