Sangivamycin is an effective inhibitor of protein kinase C (PKC, Ki = 10 μM). Sangivamycin exhibits antiproliferative activity against a variety of human cancers.
Sangivamycin (0.3 μM; 0-72 hours) exhibits almost maximal cytocidal for MCF7/ADR or cytostatic for MCF7/WT effects. Sangivamycin activates caspases in MCF7/ADR cells. Upon exposure of MCF7/ADR cells to Sangivamycin (0.3 μM), a vast amount of cleavage of lamin A to a 28-kDa fragment is detected within 48 hours. Sangivamycin has differential antitumor effects in drug-sensitive MCF7/wild type (WT) cells, causing growth arrest, and in multidrug-resistant MCF7/adriamycin-resistant (ADR) human breast carcinoma cells, causing massive apoptotic cell death[2].