Name: PF-4708671
Price: 220.00 USD

- Overview
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    Background
    
    PF-4708671 is a cell-permeable and highly specific inhibitor of p70 ribosomal S6 kinase 1 with IC50 value of 160nM [1].
    S6K1 is a regulator of various biology processes. The inhibition of S6K1 is regard as a therapeutic for the treatment of cancer and insulin resistance. PF-4708671 is the first reported inhibitor of S6K1. It inhibits the activity of S6K1 in the in vitro assay with Ki value of 20nM. For the isolated S6K1 from HEK293 cell, PF-4708671 shows inhibition with IC50 value of 160nM. The inhibition of S6K1caused by PF-4708671 is much more potent than of other related kinases such as RSK2 and MSK1. Besides that, PF-4708671 prevents S6K1 from phosphorylating its substrates including the ribosomal S6 protein, mTOR and Rictor. In addition, PF-4708671 is found to enhance the phosphorylation of S6K1 at Thr229 and Thr389, results in a subsequent increase of S6K1 activity. Whereas this increased activity is much less than that stimulated by IGF1 [1].
    
    [1] Pearce L, Alton G, Richter D, et al. Characterization of PF-4708671, a novel and highly specific inhibitor of p70 ribosomal S6 kinase (S6K1). Biochem. J, 2010, 431: 245-255.
- Properties
  - Alternative Name
    
    2-[[4-(5-ethylpyrimidin-4-yl)piperazin-1-yl]methyl]-6-(trifluoromethyl)-1H-benzimidazole
    
    CAS Number
    
    1255517-76-0
    
    Molecular Formula
    
    C19H21F3N6
    
    Molecular Weight
    
    390.41
    
    Appearance
    
    A solid
    
    Purity
    
    99.77%
    
    Solubility
    
    ≥37.8 mg/mL in DMSO; ≥17.13 mg/mL in EtOH; insoluble in H2O
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Jafari N, Zheng Q, et al. "p70S6K1 (S6K1)-mediated Phosphorylation Regulates Phosphatidylinositol 4-Phosphate 5-Kinase Type I γ Degradation and Cell Invasion." J Biol Chem. 2016 Dec 2;291(49):25729-25741. PMID:27780861

PF-4708671

PF-4708671

Background

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