5.38241

Nur77-p38 Interaction Inhibitor, PDNPA

• Synonym(s): Nur77-p38 Interaction Inhibitor, PDNPA, Pentyl 2-(3,5-dihydroxy-2-nonanoylphenyl)acetate, NR4A1 Inhibitor, PDNPA, TR3-p38 Interaction Inhibitor, PDNPA
• Empirical Formula (Hill Notation): C₂₂H₃₄O₅
• Molecular Weight: 378.50
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• assay: ≥97% (HPLC)
• Quality Level: 100
• form: solid
• potency: 1.6 μM IC₅₀
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: white
• solubility: DMSO: 100 mg/mL
• storage temp.: −20°C

Description

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.

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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable