LAQ824 (NVP-LAQ824) is a novel HDAC inhibitor with IC50 of 32 nM. LAQ824 activates the p21 promoter with 50% of the maximal promoter activation (AC50) of 0.30 μM, which in turn, activates the p21 inhibitor gene. LAQ824 inhibits the cell growth of H1299, a non-small cell lung carcinoma line, and HCT116, a colon cancer cell line with IC50 of 0.15 μM and 0.01 μM, respectively. A recent study shows that LAQ824 induces chromatin changes at the level of the IL-10 gene promoter that lead to enhanced recruitment of the transcriptional repressors HDAC11 and PU.1 and inhibits IL-10 production in BALB/c murine macrophages.
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