JNK-IN-8

- Overview
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    Background
    
    JNK-IN-8 is a specific JNK1/2/3 inhibitor with IC50 value of 4.67, 18.7, 0.98 nM respectively [1].
    C-Jun N-terminal kinase (JNK) 1, 2 and 3 belong to the mitogen-activated protein kinase (MAPK) family, which are able to phosphorylate c-Jun on the Ser63 and Ser73 residue.They are responsive for stress stimuli, including cytokines and heat shock, and get involved in T cell differentiation and cell apoptosis process. JNK 1 and 2 are ubiquitous in all cell types but JNK 3 is only found in cells of brain, heart and testes tissues.
    JNK-IN-8 is a JNK1/2/3 inhibitor with high specificity. When JNK-IN-8 was profiled with a panel of 400 kinases, it exhibited specific binding to JNK 1/2/3 but not to other kinases. Crystallization study also found that JNK-IN-8 forms covalent bonds with conserved cysteine residue of JNK 1/2/3, resulting in a conformational change of the activation loop that blocks the substrate binding, thereby inhibiting the activity of JNK 1/2/3 [1].
    In Hela cells and A375 cells, pretreatment of cells with JNK-IN-8 resulted in the inhibition of c-Jun which is a direct phosphorylation substrate of JNK 1/2/3, confirming the inhibitory action of JNK-IN-8 on JNK 1/2/3. In HEK293-ILR1 cells following stimulation by anisomycin, the JNK-IN-8 was observed to inhibit c-Jun but not MSK1 and p38, and the inhibition was not reversible by removing JNK-IN-8 from culture medium. Additionally, JNK-IN-8 only exhibited on-pathway inhibition of JNK signaling pathway, which can be monitored by the phosphorylation of c-Jun [1].
- Properties
  - Alternative Name
    
    3-[[(E)-4-(dimethylamino)but-2-enoyl]amino]-N-[3-methyl-4-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide
    
    CAS Number
    
    1410880-22-6
    
    Molecular Formula
    
    C29H29N7O2
    
    Molecular Weight
    
    507.59
    
    Appearance
    
    A solid
    
    Purity
    
    99.45%
    
    Solubility
    
    ≥25.4 mg/mL in DMSO; insoluble in H2O; ≥9.24 mg/mL in EtOH with gentle warming and ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

JNK-IN-8

Background

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