SL-IST-002

SL-IST-002 is a preclinical-stage, orally bioavailable small molecule inhibitor of lysine acetyltransferase 6A (KAT6A), an epigenetic regulator belonging to the MYST family of histone acetyltransferases (HATs). Developed by Isosterix in collaboration with Sai Life Sciences, SL-IST-002 belongs to the 'Series 2' class of KAT6A selective inhibitors. It binds to the active site of KAT6A within the acetyl-CoA substrate-binding pocket, inhibiting histone H3 lysine 23 (H3K23) acetylation. SL-IST-002 has demonstrated potent biochemical inhibition of KAT6A (IC50 of 7 nM) and significant anti-proliferative activity in estrogen receptor-positive (ER+) breast cancer cell lines (such as ZR-75-1), as well as robust anti-tumor efficacy in mouse xenograft models.