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PRN694

Chemical Structure : PRN694

CAS No.: 1575818-46-0

PRN694 (PRN-694)

Catalog No.: PC-35183Not For Human Use, Lab Use Only.

PRN694 (PRN-694) is a highly selective, potent, covalent inhibitor of interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) with IC50 of 0.3 and 1.4 nM, respectively.

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    Biological Activity

    PRN694 (PRN-694) is a highly selective, potent, covalent inhibitor of interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) with IC50 of 0.3 and 1.4 nM, respectively.
    PRN694 also potently inhibits family member TEC (IC50=3.3 nM), weakly inhibits BTK (IC50=17 nM), has no activity against EGFR, ERBB2 and ERBB4 in a panel of 250 kinases.
    PRN694 prevents T-cell receptor- and Fc receptor-induced cellular and molecular activation, inhibits T-cell receptor-induced T-cell proliferation, and blocks proinflammatory cytokine release as well as activation of Th17 cells.
    PRN694 demonstrates inhibitory activity against T-cell prolymphocytic leukemia cells in ex vivo assays.
    PRN694 is a potent inhibitor of Th1 and Th17 differentiation and cytokine production, markedly reduces disease progression in models of colitis.

    Physicochemical Properties

    M.Wt 543.67
    Formula C28H35F2N5O2S
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20 °C 12 Months; 4°C 6 Months
    In Solvent
    -80 °C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    5-(Difluoromethyl)-N-[1-[[(2R)-1-(1-oxo-2-propen-1-yl)-2-pyrrolidinyl]methyl]-5-[[[(1S)-1,2,2-trimethylpropyl]amino]methyl]-1H-benzimidazol-2-yl]-2-thiophenecarboxamide

    References

    1. Zhong Y, et al. J Biol Chem. 2015 Mar 6;290(10):5960-78.

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