Ingenol mebutate (Ingenol 3-Angelate) is a potent activator of PKC subtypes including PKC-α, PKC-β, PKC-γ, PKC-δ, and PKC-ε with Kis of 0.3, 0.105, 0.162, 0.376, and 0.171 nM. Ingenol mebutate exhibits antiinflammatory and antitumor activity.

PKCα:0.3 nM (Ki), PKCδ:0.376 nM (Ki), PKCγ:0.162 nM (Ki), PKCε:0.171 nM (Ki), PKCβ:0.105 nM (Ki)

Ingenol mebutate shows EC50s for PKC-α, PKC-βI, PKC-βII, PKC-γ, PKC-δ, PKC-ε and PKC-μ of 13, 4.37, 10.5, 38.6, 1.08 and 0.9 nM in WEHI-231 cells. The EC50s are 198, 69.1, 4.6, 1 nM in HOP-92 cells for PKC-α, PKC-βI, PKC-ε, PKC-μ and 635, 146, 4.7, 1.1, 30 nM for PKC-α, PKC-βI, PKC-δ, PKC-ε, PKC-μ in Colo-205 cells. Ingenol mebutate sensitizes WEHI-231 cells, HOP-92 and Colo-205 cells with IC50s of 1.41, 3.24, and 11.9 nM, respectively[2]. Ingenol mebutate (20 nM) induces apoptosis in a PKC-δ dependent manner in primary AML marrow blasts but not in normal myeloblasts[3].