PKC-theta inhibitor 1 is an orally active and selective ATP-competitive inhibitor of Protein Kinase Ctheta (PKCtheta), 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 µM in anti-CD3/CD28-stimulated PBMCs, IL-17 IC50 = 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[1].
Molecular Weight:
348.32
Purity:
99.73
CAS Number:
[1160501-81-4]
Formula:
C17H15F3N4O
Target:
Interleukin Related,PKC
Application Notes:
Reference compound
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