Name: BMS-509744
Price: 375.00 USD

- Overview
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    Background
    
    BMS-509744 is a selective inhibitor of ITK with IC50 value of 15 nM [1].ITK (IL-2-inducible T cell kinase) is an enzyme and plays an important role in T cell receptor signaling. It has been reported that ITK involves in the Th2-mediated inflammatory process and thus be regarded as a promising target for Th2-mediated inflammatory/immunosuppressive diseases treatment, such as asthma, rhinitis, allergies and atopic dermatitis [2].BMS-509744 is a potent ITK inhibitor and is different from the reported ITK inhibitor RO5191614. When tested with human and murine cells, administration of BMS-509744 reduced TCR-induced functions by functioning on PLCgamma1 tyrosine phosphorylation, calcium mobilization, IL-2 secretion and T-cell proliferation [2]. In wild-typr HIV1 infected cells, BMS-509744 treatment blocked its infectivity and replication by inhibiting ITK, while has no effect on Nef-defective HIV1 infected cells [3].In mouse model of ovalbuim-induced allergy/asthma, administration of BMS-509744 suppressed the production of IL-2 and significantly diminished lung inflammation by inhibiting ITK activity [2].
    
    [1].Kutach, A.K., et al., Crystal structures of IL-2-inducible T cell kinase complexed with inhibitors: insights into rational drug design and activity regulation. Chem Biol Drug Des, 2010. 76(2): p. 154-63.
    [2].Lin, T.A., et al., Selective Itk inhibitors block T-cell activation and murine lung inflammation. Biochemistry, 2004. 43(34): p. 11056-62.
    [3].Tarafdar, S., J.A. Poe, and T.E. Smithgall, The accessory factor Nef links HIV-1 to Tec/Btk kinases in an Src homology 3 domain-dependent manner. J Biol Chem, 2014. 289(22): p. 15718-28.
- Properties
  - Alternative Name
    
    BMS 509744;BMS509744; N-(5-((5-(4-acetylpiperazine-1-carbonyl)-4-methoxy-2-methylphenyl)thio)thiazol-2-yl)-4-(((3,3-dimethylbutan-2-yl)amino)methyl)benzamide
    
    CAS Number
    
    439575-02-7
    
    Molecular Formula
    
    C32H41N5O4S2
    
    Molecular Weight
    
    623.83
    
    Appearance
    
    White solid
    
    Purity
    
    98.00%
    
    Solubility
    
    Soluble in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

BMS-509744

BMS-509744

Background

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