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. 2018 Nov 23;8:17297. doi: 10.1038/s41598-018-35602-1

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© The Author(s) 2018

Open Access This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in a credit line to the material. If material is not included in the article’s Creative Commons license and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this license, visit http://creativecommons.org/licenses/by/4.0/.

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Enzyme selectivity of CKD-506 & Pharmacokinetic profile of CKD-506. The selectivity of CKD-506 was analyzed based on HDAC enzyme inhibition and protein acetylation. (A) After single intraperitoneal injection of CKD-506, blood samples were collected at the indicated time points. The plasma concentration of CKD-506 was analyzed. All the data were presented as mean ± SD. Upper panel: plasma concentration – time plot of CKD-506; Lower table: pharmacokinetic parameters of CKD-506. (B) The enzyme activity of HDAC family members with the indicated concentration of CKD-506 (log of molar concentration; Log M) was analyzed and plotted. The Y-axis represents the percentage of enzymatic activity normalized to the enzyme activity without CKD-506. (C) The HDAC6 enzyme selectivity of CKD-506 in human PBMC was analyzed based on the acetylation of α tubulin, one of the major target proteins of HDAC6, and the acetylation of histone H4 which is not a target protein of other HDAC isozymes. LBH-589 is a pan HDAC inhibitor, a positive control for the induction of histone H4 acetylation (the chemicals were treated for 4 hr.). Samples were derived from the same experiment, and blots were processed in parallel. Full-length blots are presented in Supplementary Fig. 1. T_1/2: elimination half-life; hr: hour; T_max: time to maximum plasma concentration; Cmax: maximum plasma concentration; AUC_0–24hr: area under the curve from time zero to 24 hr; AUC_inf: area under the curve from time zero to infinity (extrapolated data); i.p.: intraperitoneal.