LAQ824（NVP-LAQ824）是一种新型HDAC抑制剂，IC | 50 |为32 nM。LAQ824以0.30μM的最大启动子激活（AC | 50 |）的50％激活p21启动子，从而激活p21抑制剂基因。LAQ824抑制IC50分别为0.15μM和0.01μM的H1299（非小细胞肺癌细胞系）和HCT116（结肠癌细胞系）的细胞生长。最近的一项研究表明，LAQ824会在IL-10基因启动子水平上诱导染色质变化，从而导致转录阻遏物HDAC11和PU.1的募集增加，并抑制BALB / c鼠巨噬细胞中IL 应用： Dacinostat 是一种有效的 HDAC 抑制剂，IC50 值为 32 nM；Dacinostat 同时可抑制 HDAC1 的活性，IC50 值为 9 nM，主要用于癌症研究。 LAQ824 (NVP-LAQ824) is a novel HDAC inhibitor with IC|50|of 32 nM. LAQ824 activates the p21 promoter with 50% of the maximal promoter activation (AC|50|) 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 IC|50|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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LAQ824
CAS number：404951-53-7 molecular formula：C22H25N3O3
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compound introduction
Specs
| Chinese alias | - | ||
| English alias | (2E)-N-Hydroxy-3-(4-({(2-hydroxyethyl)(2-(1H-indol-3-yl)ethyl)amino}methyl)phenyl)propenamide | 7-Chloro4-quinolinol | Dacinostat (NVP-LAQ824, LAQ824) | 2-Propenamide, N-hydroxy-3-[4-[[(2-hydroxyethyl)[2-(1H-indol-3-yl)ethyl]amino]methyl]phenyl]-, (2E)- | | ||
| CAS number | 404951-53-7 | molecular formula | C22H25N3O3 |
| molecular weight | 379.45 g/mol | Exact mass | - |
| PSA | 88.600 Ų | logp | 2.6 |
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