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Histone deacetylase 6 (HDAC6) is a class II HDAC that represses transcription by removing acetyl groups from histones. In addition, HDAC6 deacetylases tubulin, which is important in regulating microtubule stability and function. CAY10603 is a potent and selective inhibitor of HDAC6 (IC50 = 0.002 nM, as compared with 271, 252, 0.42, 6851, and 90.7 nM for HDAC1, 2, 3, 8, and 10, respectively).1 Also, CAY10603 prevents the growth of several pancreatic cancer cell lines (IC50 = 0.1-
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1. Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: A new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6. J. Med. Chem. 51, 4370-4373 (2008).