Nur77-p38 Interaction Inhibi 1PC X 10MG

Biochem/physiol Actions

Reversible: yes

Primary TargetNur77

Cell permeable: yes

General description

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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Li, L., et al. 2015. Nat. Chem. Biol.11, 339.

Packaging

Packaged under inert gas

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)