N-Acetyl-S-(N’-phenylhexylthiocarbamoyl)-L-cysteine (PHITC) is a cysteine conjugate of N-acetyl-phenylhexylisothiocyanate. Isothiocyanates are typically found in plants of the Brassicaceae family, including broccoli, cabbage, and radish. Isothiocyanates are best known for their antioxidative, anticancer chemotherapeutic, chemopreventive, anti-angiogenic, and antibiotic properties. In vitro, PHITC increases caspase 3 activity and cleavage of poly(ADP)-ribose polymerase (PARP), inducing caspase-mediated apoptosis in cellular models. This compound decreases oxidation of carcinogen NNK and increases activity of NADPH:quinone oxidoreductase and glutathione-S-transferase in vitro and in vivo. PHITC inhibits histone deacetylase (HDAC) activity, IL-6 receptor production, and VEGF expression; it also induces mitochondrial membrane depolarization and apoptosis in myeloma cells. In leukemia cells, PHITC inhibits expression of cyclin and increases expression of CDK inhibitors, inducing apoptosis and inhibiting growth of xenografts of these cells in animals.
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