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492910 | Nur77 LBD Antagonist, TMPA - Calbiochem

492910
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      Overview

      Replacement Information

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      492910-10MG
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          Glass bottle 10 mg
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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 Image
          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

          Documentation

          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 formula
          Purity≥97% by HPLC
          SolubilityDMSO (100 mg/ml). Use only fresh DMSO for reconstitution.
          Storage +2°C to +8°C
          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.
          Toxicity Standard Handling
          ReferencesZhan, Y.Y., et al. 2012. Nat. Chem. Biol. 8, 897.