| Description |
A cell-permeable pyridinecarbonitrile compound that acts as a potent, ATP-competitive (K i = 79 nM, using PKCθ KD in coupled PK/LDH assays), and isozyme-selective PKCθ inhibitor (IC 50 = 70 nM) with much reduced potency against other novel PKCs (IC 50 = 0.35, 2.33, and 16.35 µM against δ, ε, and η isoforms, respectively) and little or no activity against the conventional PKCβ and atypical PKCζ (IC 50 >50 µM) as well as a panel of 18 other commonly studied cellular kinases (IC 50 >10 µM)
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