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492910 Nur77 LBD Antagonist, TMPA - Calbiochem

Nur77 LBD Antagonist, TMPA - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

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

492910
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492910-10MGCN
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      Description
      OverviewA 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 Number492910
      Brand Family Calbiochem®
      SynonymsEthyl-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
      References
      ReferencesZhan, Y.Y., et al. 2012. Nat. Chem. Biol. 8, 897.
      Product Information
      FormOff-white solid
      Hill FormulaC₂₁H₃₂O₆
      Chemical formulaC₂₁H₃₂O₆
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetNur77
      Purity≥97% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Catalogue Number GTIN
      492910-10MGCN 04055977272819

      Documentation

      Nur77 LBD Antagonist, TMPA - Calbiochem Certificates of Analysis

      TitleLot Number
      492910

      References

      Reference overview
      Zhan, Y.Y., et al. 2012. Nat. Chem. Biol. 8, 897.
      Data Sheet

      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.

      Revision17-May-2013 JSW
      SynonymsEthyl-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
      DescriptionA cell-permeable phenylacetate compound that blocks Nur77 (TR3) LKB1 nuclear-sequestering function by antagonizing Nur77-LKB1 interaction via direct binding at the LKB1 LBD/ligand binding domain (Kd = 0.14 and 0.25 µM, respectively, against 5 µM LKB1 binding to 5 µM full-length Nur77 or Nur77 LBD). Shown to induce LKB1 Ser428 phosphorylation (10 & 20 µM for 6 hr) and LKB1 nuclear-to-cytosol translocation in hepatic LO2 cells, resulting in enhanced phosphorylations of LKB1 cytosolic effectors AMPKα (Thr172) and MARK (Thr215, Thr208, and Thr234 of MARK1, MARK2, and MARK3, respectively), without affecting Nur77 transactivation activity. Likewise, daily i.p. dosing (50 mg/kg for 19 d) results in greatly enhanced liver LKB1 Ser428/AMPKα Thr172 phosphorylations only in Nr4a1+/+, but not Nur77-null Nr4a1-/-, diabetic db/db mice in vivo, effectively lowering fasting blood glucose and insulin level, and enhancing glucose tolerance in db/db mice. Also reported to lower fasting blood glucose level in high fat diet-fed Nr4a1+/+ mice treated with STZ (Cat. No. 572201) to induce type II diabetes.
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₁H₃₂O₆
      Structure formulaStructure formula
      Purity≥97% by HPLC
      SolubilityDMSO (100 mg/ml). Use only fresh DMSO for reconstitution.
      Storage Protect from light
      +2°C to +8°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesZhan, Y.Y., et al. 2012. Nat. Chem. Biol. 8, 897.