A PKCθ inhibitor
VTX-27 is a PKCθ inhibitor (Ki = 0.08 nM).1 It is selective for PKCθ over PKCα, -βI, -βII, -γ, -δ, -ε, -η, -?, and -ζ with Ki values ranging from 1 to >5,000 nM as well as a panel of seven kinases from the Src, spleen tyrosine kinase (Syk), Tec, and MAP kinase families (Kis = >1,000 nM for all). VTX-27 inhibits CD28-induced IL-2 release in isolated human peripheral blood mononuclear cells (PBMCs; IC50 = 11 nM). Oral administration of VTX-27 (12.5, 25, and 50 mg/kg) prevents staphylococcal enterotoxin B-induced increases in IL-2 plasma levels in mice.
1.Jimenez, J.-M., Boyall, D., Brenchley, G., et al.Design and optimization of selective protein kinase C θ (PKCθ) inhibitors for the treatment of autoimmune diseasesJ. Med. Chem.56(5)1799-1810(2013)
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