1-BENZOYL-3-PHENYL-2-THIOUREA

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 mutantsin vitro.2

[1] RAUSHAN K. SINGH . Histone deacetylase activators: N-acetylthioureas serve as highly potent and isozyme selective activators for human histone deacetylase-8 on a fluorescent substrate[J]. Bioorganic & Medicinal Chemistry Letters, 2011, 21 19: Pages 5920-5923. DOI:10.1016/j.bmcl.2011.07.080
[2] CHRISTOPHE DECROOS. Compromised Structure and Function of HDAC8 Mutants Identified in Cornelia de Lange Syndrome Spectrum Disorders[J]. ACS Chemical Biology, 2014, 9 9: 2157-2164. DOI:10.1021/cb5003762
[3] RAUSHAN K SINGH. Mechanism of N-Acylthiourea-mediated activation of human histone deacetylase 8 (HDAC8) at molecular and cellular levels.[J]. The Journal of Biological Chemistry, 2015, 290 10: 6607-6619. DOI:10.1074/jbc.m114.600627