JG-2016 is a small molecule inhibitor of histone acetyltransferase 1 (HAT1) with IC50 of 14.8 uM in the HAT1 acetylation assays.
JG-2016 binds HAT1 at the cofactor-binding site and does not compete with the histone substrate.
JG-2016 robustly inhibited cell growth (EC50=10.4 uM) in triple-negative breast cancer cell line HCC1806, inhibits A549 (lung cancer) with EC50 of 1.9 uM.
JG-2016 (50-100 mg/kg, i.p.) impairs HAT1 dependent acetylation and suppresses tumor growth with minimal toxicity in vivo.
