BRD73954 is a potent and selective inhibitor of HDAC with IC50 values of 36 and 120 nM for HDAC6 and HDAC8, respectively [1].
Histone deacetylases (HADCs) are a series of enzymes that remove acetyl groups from an ε-N-acetyl lysine amino acid on a histone and make the histones to wrap the DNA more tightly, which prevent transcription [1].
BRD73954 is a potent and selective HDAC inhibitor with IC50 values of 36 and 120 nM for HDAC6 and HDAC8, respectively. Also, BRD73954 inhibited HDAC1, HDAC2, HDAC3, HDAC4, HDAC5, HDAC7 and HDAC9 with IC50 values of 12, 9.0, 23, >33, >33, 13 and >33 μM, respectively. In HeLa cells, BRD73954 significantly increased α-tubulin acetylation, which was a substrate for HDAC6, while there was no change in the acetylation state of histone H3, which was a substrate for HDACs 1, 2 and 3 [1].
Reference:
[1]. Olson DE, Wagner FF, Kaya T, et al. Discovery of the first histone deacetylase 6/8 dual inhibitors. J Med Chem, 2013, 56(11): 4816-4820.