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Background: MC1568, a derivative of (Aryloxopropenyl)pyrrolyl hydroxyamide, is a novel, potent and specific inhibitor of class II histone deacetylase (HDAC), including two subclasses IIa (HDAC4, HDAC5, HDAC6, HDAC7 and HDAC9) and IIb (HDAC6 and HDAC 10), that exhibits strong inhibition against maize class II HDAC with 50% inhibition concentration IC50 value of 22 µM. MC1568 has been found to tissue-selectively inhibits HDAC and arrest myogenesis in cultured muscle cells through three possible mechanisms, including decreasing the expression of myocyte enhancer factor 2D, stabilizing the HDAC3/4 -MEF2D complex and inhibiting the acetylation of differentiation-induced MEF2D. Moreover, MC1568 is able to interfere with RAR- and PPARγ-mediated differentiation-inducing signaling pathways.
CAS Number: 852475-26-4
Description: Selective inhibitor of class IIa histone deacetylases (HDACs). Exhibits tissue-selective inhibition between members of class II deacetylases in vivo; inhibits HDAC4 and HDAC5 in skeletal muscle and the heart without affecting HDAC3 activity. Displays no inhibition of class I HDAC activity (HDAC1, 2, 3) or expression.
Solubility: Soluble in DMSO
Storage Stability: Store at or below -20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.
Target: HDAC
Biosafety Level: Not applicable (BSL-1)
References: 1. Mai A, et al. J Med Chem. 2005 May 5;48(9):3344-53.
2. Nebbioso A, et al. J Mol Endocrinol. 2010 Oct;45(4):219-28.
3. Nebbioso A, et al. EMBO Rep. 2009 Jul;10(7):776-82.
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