4921-82-8

TM-2-51 (4921-82-8) is a highly potent and isozyme selective activator of recombinant HDAC8. Increases the activity of HDAC8 by a factor of 12 at 10 μM. No activation of other HDACs is observed. TM-2-51 rescues the activity of catalytically compromised HDAC8 mutants?in vitro.2

1) Singh?et al. (2011), Histone deacetylase activators: N-acetylthioureas as highly potent and isozyme selective activators for human histone deacetylase-8 on a fluorescent substrate; Bioorg. Med. Chem. Lett.,?21?5920 2) Decross?et al. (2014), Compromised Structure and Function of HDAC8 Mutants Identified in Cornelia de Lange Syndrome Spectrum Disorders; ACS Chem. Biol.,?9?2157 3) Singh?et al. (2015),?Mechanism of N-acylthiourea Mediated Activation of Human Histone Deacetylase 8 (HDAC8) at Molecular and Cellular Levels; J. Biol. Chem.,?290?6607