ITF5924

ITF5924 (compound 1) is a potent and highly selective HDAC6 inhibitor with an IC50 of 7.7 nM. ITF5924 shows greater than 104-fold selectivity for HDAC6 over all other HDAC subtypes. ITF5924 containing a difluoromethyl-1,3,4-oxadiazole (DFMO) moiety is slow-binding substrate analog of HDAC6 that undergo an enzyme-catalyzed ring opening reaction, forming a tight and long-lived enzyme-inhibitor complex[1].

HDAC6: 7.7 nM (IC₅₀)

[1] Edoardo Cellupica, et al. Difluoromethyl-1,3,4-oxadiazoles are slow-binding substrate analog inhibitors of histone deacetylase 6 with unprecedented isotype selectivity. J Biol Chem. 2023 Jan;299(1):102800. DOI:10.1016/j.jbc.2022.102800