MilliporeSigma™ Calbiochem™ PKCθ/δ Inhibitor

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 = 70nM) with much reduced potency against other novel PKCs (IC 50 = 0.35, 2.33, and 16.35μM against δ, ε, and η isoforms, respectively) and little or no activity against the conventional PKCβ and atypical PKCζ (IC 50 >50μM) as well as a panel of 18 other commonly studied cellular kinases (IC 50 >10μM)
• Shown to preferentially inhibit IL-2 production from anti-CD3- and anti-CD28-activated T cells derived from wild-type over PKCθ-knockout mice (IC 50 = 58 and 231 nM, respectively).