A cell-permeable phenylacetate based compound that specifically blocks the Nur77-p38α interaction by directly targeting the ligand-binding domain of Nur77 (~1 to 10 µM) and impedes Nur77 phosphorylation by p38α. Does neither modulate p38α kinase activity nor affects the stability of the p38α-Nur77 complex. Inhibits p65 binding to DNA and blocks LPS-induced (100 ng/ml) NF-κB activity in RAW264.7 cells (IC50 = 1.6 µM), but does not affect the interaction between Nur77 and p65. Shown to reduce IL-6 concentration and prolong the lifespan of wild type mice treated with LPS. Also increases the survival rate of wild-type mice subjected to cecal ligation and puncture (CLP)-induced sepsis.
A cell-permeable phenylacetate based compound that specifically blocks the Nur77-p38α interaction by directly targeting the ligand-binding domain of Nur77 (~1 to 10 µM) and impedes Nur77 phosphorylation by p38α. Does neither modulate p38α kinase activity nor affects the stability of the p38α-Nur77 complex. Inhibits p65 binding to DNA and blocks LPS-induced (100 ng/ml) NF-κB activity in RAW264.7 cells (IC50 = 1.6 µM), but does not affect the interaction between Nur77 and p65. Shown to reduce IL-6 concentration and prolong the lifespan of wild type mice treated with LPS. Also increases the survival rate of wild-type mice subjected to cecal ligation and puncture (CLP)-induced sepsis.
Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
Biochem/physiol Actions
Cell permeable: yes
Primary Target Nur77
Reversible: yes
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Li, L., et al. 2015. Nat. Chem. Biol.11, 339.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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