492910 Sigma-AldrichNur77 LBD Antagonist, TMPA - 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
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Overview
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Pricing & Availability
Catalog Number | Availability | Packaging | Qty/Pack | Price | Quantity | |
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492910-10MG |
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Glass bottle | 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 | |
Quality Level | MQ100 |
Applications |
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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 |
Dimensions |
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Materials Information |
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Toxicological Information |
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Safety Information according to GHS |
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Safety Information |
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Product Usage Statements |
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Packaging Information | |
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Packaged under inert gas | Packaged under inert gas |
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Supplemental Information |
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Specifications |
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Global Trade Item Number | |
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Catalog Number | GTIN |
492910-10MG | 04055977272819 |
Documentation
Nur77 LBD Antagonist, TMPA - Calbiochem Certificates of Analysis
Title | Lot Number |
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492910 |
References
Reference overview |
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Zhan, Y.Y., et al. 2012. Nat. Chem. Biol. 8, 897. |
Data Sheet | ||||||||||||||||||||||||||||
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Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
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