PKCTheta-IN-2 (compound 14) is a potent and selective PKCθ inhibitor with an IC50 of 0.25 nM. PKCTheta-IN-2 shows good selectivity over a wide range of kinases, including the PKC subfamily (30 kinases ). PKCTheta-IN-2 inhibits the IL-2 production in a mouse ( IC50 of 682 nM) [1].
References:
[1]. Taisuke Katoh, et al. Discovery and optimization of 1,7-disubstituted-2,2-dimethyl-2,3-dihydroquinazolin-4(1H)-ones as potent and selective PKCθ inhibitors. Bioorg Med Chem. 2016 Jun 1;24(11):2466-2475.
References:
[1]. Taisuke Katoh, et al. Discovery and optimization of 1,7-disubstituted-2,2-dimethyl-2,3-dihydroquinazolin-4(1H)-ones as potent and selective PKCθ inhibitors. Bioorg Med Chem. 2016 Jun 1;24(11):2466-2475.