PKC-theta inhibitor 1 is an orally active and selective ATP-competitive inhibitor of Protein Kinase Cθ ( PKCθ ), with a K i value of 6 nM. PKC-theta inhibitor 1 inhibits T-cell-mediated inflammatory responses by suppressing the release of proinflammatory cytokines ( IL-2 IC 50 = 0.21 μM in anti-CD3/CD28-stimulated PBMCs; IL-17 IC 50 = 1 μM in CD3/CD28-stimulated Th17 cells) PKC-theta inhibitor 1 significantly reduces symptoms in mice with ongoing experimental autoimmune encephalomyelitis (EAE). PKC-theta inhibitor 1 can be used for the study of T-cell-mediated inflammatory diseases such as multiple sclerosis.
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