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Description

A cell-permeable pyridinecarbonitrile compound that acts as a potent, ATP-competitive (Ki = 79 nM, using PKCtheta KD in coupled PK/LDH assays), and isozyme-selective PKCtheta inhibitor (IC50 = 70 nM) with much reduced potency against other novel PKCs (IC50 = 0.35, 2.33, and 16.35 µ,M against delta, epsilon, and eta isoforms, respectively) and little or no activity against the conventional PKCbeta and atypical PKCzeta (IC50 >50 µ,M) as well as a panel of 18 other commonly studied cellular kinases (IC50 >10 µ,M). Shown to preferentially inhibit IL-2 production from anti-CD3- and anti-CD28-activated T cells derived from wild-type over PKCtheta-knockout mice (IC50 = 58 and 231 nM, respectively).