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| Replacement Information |
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| Description | |
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| Overview | 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 5 µM LKB1 binding to 5 µM full-length Nur77). Shown to induce LKB1 Ser428 phosphorylation (10 & 20 µM 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 (50 mg/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. |
| Catalogue Number | 492910 |
| Brand Family | Calbiochem® |
| Synonyms | 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 |
| References | |
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| References | Zhan, Y.Y., et al. 2012. Nat. Chem. Biol. 8, 897. |
| Product Information | |
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| Form | Off-white solid |
| Hill Formula | C₂₁H₃₂O₆ |
| Chemical formula | C₂₁H₃₂O₆ |
| Reversible | Y |
| Structure formula Image | |
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| Biological Information | |
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| Primary Target | Nur77 |
| Purity | ≥97% by HPLC |
| Physicochemical Information | |
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| Cell permeable | Y |
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| Packaging Information | |
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| Packaged under inert gas | Packaged under inert gas |
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