PKCβ inhibitor 1

PKCβ inhibitor is an inhibitor of PKCβ1 and PKCβ2 (IC₅₀s = 21 and 5 nM, respectively).¹ It is selective for PKCβ1 and PKCβ2 over PKCα, PKCε, and PKCγ (IC₅₀s = 331, 2,807, and >1,000 nM, respectively), as well as JAK1, JAK2, and tyrosine kinase 2 (TYK2; IC₅₀s = 770, 3,850, and 2,310 nM, respectively), but also inhibits JAK3 (IC₅₀ = 17 nM).¹,² PKCβ inhibitor (14 ?M) induces apoptosis and inhibits cell cycle progression in 2F7 AIDS-related Burkitt’s lymphoma cells.³

1.Tanaka, M., Sagawa, S., Hoshi, J.-I., et al.Synthesis of anilino-monoindolylmaleimides as potent and selective PKCbeta inhibitorsBioorg. Med. Chem. Lett.14(20)5171-5174(2004) 2.McDonnell, M.E., Bian, H., Wrobel, J., et al.Anilino-monoindolylmaleimides as potent and selective JAK3 inhibitorsBioorg. Med. Chem. Lett.24(4)1116-1121(2014) 3.Saba, N.S., and Levy, L.S.Protein kinase C-beta inhibition induces apoptosis and inhibits cell cycle progression in acquired immunodeficiency syndrome-related non-hodgkin lymphoma cellsJ. Investig. Med.60(1)29-38(2012)