MC1568 is a selective inhibitor of class IIa histone deacetylases (HDACs). In vivo, MC1568 shows an apparent tissue-selective HDAC inhibition. In skeletal muscle and heart, MC1568 inhibits the activity of HDAC4 and HDAC5 without affecting HDAC3 activity, thereby leaving MEF2-HDAC complexes in a repressed state. In F9 cells, MC1568 specifically blocks endodermal differentiation despite not affecting retinoic acid-induced maturation of promyelocytic NB4 cells. In 3T3-L1 cells, MC1568 attenuates PPARγ-induced adipogenesis. Finally, treatment of pancreatic explants with the selective class IIa HDAC inhibitor MC1568 enhances expression of Pax4, a key factor required for proper β-and δ-cell differentiation and amplifies endocrine β- and δ-cells.
|Source||Toxicol Sci (2016). Figure 1. MC1568|
|Cell Lines||SH-SY5Y cells|
|Results||Interestingly, cell viability was significantly ameliorated when cells were pretreated with MC1568, but not with MS275 compared with cells exposed to thimerosal alone|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Specific control of pancreatic endocrine β- and δ-cell mass by class IIa histone deacetylases HDAC4, HDAC5, and HDAC9.
Lenoir O, et al. Diabetes. 2011 Nov;60(11):2861-71. PMID: 21953612.
HDACs class II-selective inhibition alters nuclear receptor-dependent differentiation.
Nebbioso A, et al. J Mol Endocrinol. 2010 Oct;45(4):219-28. PMID: 20639404.
Selective class II HDAC inhibitors impair myogenesis by modulating the stability and activity of HDAC-MEF2 complexes.
Nebbioso A, et al. EMBO Rep. 2009 Jul;10(7):776-82. PMID: 19498465.
Specific activity of class II histone deacetylases in human breast cancer cells.
Duong V, et al. Mol Cancer Res. 2008 Dec;6(12):1908-19. PMID: 19074835.
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