PKC-theta inhibitor 1

Description

PKC-theta inhibitor 1 is an orally active and selective ATP-competitive inhibitor of Protein Kinase C? PKC? , with a Ki value of 6 nM. PKC-theta inhibitor 1 inhibits T-cell-mediated inflammatory responses by suppressing the release of proinflammatory cytokines IL-2 IC50 = 0.21 ?M in anti-CD3/CD28-stimulated PBMCs; IL-17 IC50 = 1 ?M 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.