The protein kinase C (PKC) isoforms PKCβ1 and PKCβ2 have central roles in cell signaling in diabetes, diffuse large B-cell lymphoma, and cardiovascular diseases. LY333531 is a selective and potent inhibitor of PKCβ1 and PKCβ2 (IC50 = 4.7 and 5.9 nM, respectively). For comparison, its IC50 values for PKC isoforms α, γ, δ, ε, ζ, and η are 360, 300, 250, 600, >100,000, and 52 nM, respectively. LY333531 is effective in vivo.