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产品目录编号 | 库存情况 | 包装 | 数量 / 包装 | 价格 | 数量 | |
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492910-10MGCN |
| 玻璃瓶 | 10 mg |
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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 |
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Cell permeable | Y |
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Packaged under inert gas | Packaged under inert gas |
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