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492910 Nur77 LBD Antagonist, TMPA - Calbiochem

492910
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Overview

Replacement Information

Products

Catalog NumberPackaging Qty/Pack
492910-10MG Glass bottle 10 mg
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®
SynonymsAMPK 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
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
Catalog Number GTIN
492910-10MG 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
SynonymsAMPK 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
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.