β-Hydroxymethyl chalcone

β-Hydroxymethyl chalcone is a time-dependent selective HDAC2 inhibitor, with IC₅₀ values of 0.17 μM (24 h) and 9.19 μM (1 h). After binding to the catalytic zinc ion in the active pocket of HDAC2, β-Hydroxymethyl chalcone undergoes an intramolecular nucleophilic attack to form a cyclic product, resulting in time-dependent tight binding. β-Hydroxymethyl chalcone can be used for the study of HDAC2 selective inhibition and related epigenetic targets^[1]. In Vitro:β-Hydroxymethyl chalcone (1-24 h) exhibits time-dependent selective inhibition of HDAC2 in in vitro recombinant enzymatic assays. The IC₅₀ values after 1 h and 24 h of incubation are 9.19 μM and 0.17 μM, respectively, with an approximately 20-fold selectivity for HDAC2 over HDAC1 (3.68 μM at 1 h; 2.74 μM at 24 h), and shows weak activity against HDAC3 (approximately 50 μM)^[1].