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KD5170 is a small molecule, alpha-mercaptoketone-based histone deacetylase (HDAC) inhibitor originally developed by Kalypsys. It functions as a broad-spectrum inhibitor of Class I and Class II HDACs, demonstrating high potency against HDAC6 (IC50 = 14 nM), HDAC1 (IC50 = 20 nM), HDAC4 (IC50 = 26 nM), and HDAC3 (IC50 = 75 nM). Preclinical studies have shown that KD5170 possesses significant antiproliferative activity against various human tumor cell lines and inhibits tumor growth in xenograft models of colorectal cancer (HCT-116), non-small cell lung carcinoma (NCI-H460), and prostate cancer (PC-3). In multiple myeloma, its activity is mediated through the induction of DNA damage and mitochondrial signaling, ultimately leading to apoptosis. Currently, its highest R&D status is preclinical.
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