Givinostat (ITF-2357) is a non-selective, orally active HDAC inhibitor capable of inhibiting STAT5 phosphorylation. It exhibits antitumour activity against crlf2-rearranged BCP-ALL and induces apoptosis. Givinostat exhibits anti-inflammatory activity by inhibiting TNF-α and IL-1β in endotoxin-stimulated PBMCs, while also promoting β-cell survival. It holds potential applications in diabetes, acute lymphoblastic leukaemia, and arthritis.

HDAC7 (human):524 nM, HDAC9 (human):541 nM, HDAC3 (human):157 nM, HD2:10 nM, HDAC6 (human):315 nM, HD1-B:7.5 nM, HD1-A:16 nM, HDAC1 (human):198 nM, HDAC11 (human):292 nM, HDAC10 (human):340 nM

After the JS-1 cell line is cultured in DMEM with 10% fetal bovine serum for 24 h, 30 wells of JS-1 cells are divided into two groups. In the first group, the culture medium is replaced by complete medium with final Givinostat (ITF-2357) concentrations of 0 nM, 125 nM, 250 nM, 500 nM, and 1000 nM. In the second group, Givinostat of relevant concentrations is added concomitantly with 100 nM of LPS solution. Three replicates are performed for each group. After inoculation at 37°C and 5% CO2 for 24 h, each well (100 μL) is incubated with 10 μL of CCK-8 solution. The plates are incubated at 37°C for 1 h and the absorbance is measured at 450 nm using a microplate reader[2].