MK2 Inhibitor IV

- Overview
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    Background
    
    MK2 Inhibitor IV is a highly selective and non-ATP competitive MK2 inhibitor with IC50 value of 0.11 μM [1]. MAP kinase-activated protein kinase 2 (MAPKAPK2 or MK2) is a member of the Ser/Thr protein kinase family and regulated through direct phosphorylation by p38 MAP kinase. Activation of the p38/MK2 pathway involved in promoting pro-inflammatory cytokine production and related inflammatory diseases [1]. MK2 Inhibitor IV is a highly selective and non-ATP competitive MK2 inhibitor. In a broad panel of 150 protein kinases, MK2 Inhibitor IV only significantly inhibited CK1γ3 at greater than 50%. MK2 Inhibitor IV also demonstrated no inhibition against a panel of cytochrome P450 (CYP) enzymes up to 30 μM. In the human THP1 acute monocytic leukemia cell line, MK2 Inhibitor IV inhibited pro-inflammatory cytokine secretion. MK2 Inhibitor IV also dose-dependently inhibited LPS-stimulated TNFα and IL6 secretion with IC50 values of 4.4 μM and 5.2 μM, respectively. In the SW1353 chondrosarcoma cell line and human primary chondrocyte cultures, MK2 Inhibitor IV dose dependently inhibited IL1β-stimulated matrixmetalloprotease (MMP)13 secretion with IC50 values of 5.7 μM and 2.2 μM, respectively.
- Properties
  - Alternative Name
    
    MK 25; 5-(4-chlorophenyl)-N-[4-(1-piperazinyl)phenyl]-N-(2-pyridinylmethyl)-2-furancarboxamide, monohydrochloride
    
    CAS Number
    
    1314118-94-9
    
    Molecular Formula
    
    C27H25ClN4O2·HCl
    
    Molecular Weight
    
    509.4
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in DMSO; ≥16.5 mg/mL in EtOH with ultrasonic; ≥37.4 mg/mL in H2O
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

MK2 Inhibitor IV

Background

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