Activator of protein kinase C; attached to cell permeabilization Antennapedia domain vector peptide. Consists of peptide derived from the C2 domain of PKC β linked by a disulfide bridge to the Antennapedia domain vector peptide. The Antennapedia peptide is actively taken up by intact cells, at 4 or 37°C, ensuring rapid and effective uptake of the activator peptide. Once inside the cell, the disulfide bonds are subjected to reduction in the cytoplasm leading to release of the activator peptide.

PEN-221 is a Somatostatin receptor 2 (SSTR2)-targeting cytotoxic conjugate with an IC50 of 10 nM. PEN-221 is a conjugate consisting of microtubule-targeting agent DM1 linked to the C-terminal side chain of Tyr3-octreotate.

Methyl nomilinate from citrus can modulate cell cycle regulators to induce cytotoxicity in human colon cancer (SW480) cells in vitro.