MC1568

MC1568，(Aryloxopropenyl)pyrrolyl hydroxyamide的衍生物，是一种新型有效的和特异性的II类组蛋白去乙酰化酶（HDAC）抑制剂，对玉米的II类HDAC具有强烈的抑制效应，IC50值为22 μM。II类HDAC包括两个子类：IIa（HDAC4、HDAC5、HDAC6、HDAC7和HDAC9）和Ⅱb（HDAC6和HDAC10）。据报道，在培养的肌细胞中，MC1568通过三种可能的机制，组织选择性地抑制HDAC和肌肉发生，包括减少肌细胞增强因子2D的表达，稳定HDAC-HDAC3-MEF2D复合体和抑制分化诱导的MEF2D乙酰化。而且，MC1568能够干扰RAR和PPARγ介导的分化诱导的信号通路。

参考文献：
Mai A, Massa S, Pezzi R, Simeoni S, Rotili D, Nebbioso A, Scognamiglio A, Altucci L, Loidl P, Brosch G.  Class II (IIa)-selective histone deacetylase inhibitors. 1. Synthesis and biological evaluation of novel (aryloxopropenyl)pyrrolyl hydroxyamides. J Med Chem. 2005 May 5;48(9):3344-53.
Nebbioso A, Dell'Aversana C, Bugge A, Sarno R, Valente S, Rotili D, Manzo F, Teti D, Mandrup S, Ciana P, Maggi A, Mai A, Gronemeyer H, Altucci L.  HDACs class II-selective inhibition alters nuclear receptor-dependent differentiation. J Mol Endocrinol. 2010 Oct;45(4):219-28. doi: 10.1677/JME-10-0043. Epub 2010 Jul 16.
Nebbioso A, Manzo F, Miceli M, Conte M, Manente L, Baldi A, De Luca A, Rotili D, Valente S, Mai A, Usiello A, Gronemeyer H, Altucci L.  Selective class II HDAC inhibitors impair myogenesis by modulating the stability and activity of HDAC-MEF2 complexes. EMBO Rep. 2009 Jul;10(7):776-82. doi: 10.1038/embor.2009.88. Epub 2009 Jun 5.