– (-)-Indolactam V, a potent PKC activator, exhibits binding affinities (Kis) of 3.36 nM and 1.03 μM for η-CRD2 and γ-CRD2, respectively, and dissociation constants (Kds) of 5.5 nM (η-C1B), 7.7 nM (ε-C1B), 8.3 nM (δ-C1B), 18.9 nM (β-C1A-long), 20.8 nM (α-C1A-long), 137 nM (β-C1B), 138 nM (γ-C1A), and 213 nM (γ-C1B), also demonstrating antitumor activity.