compound introduction
SGC-iMLLT is a first-in-class chemical probe and a potent, selective inhibitor of MLLT1/3-histone interactions with an IC 50 of 0.26 μM. SGC-iMLLT shows high binding activity towards MLLT1 YEATS domain (YD) and MLLT3 YD (AF9/YEATS3) with K d s of 0.129 and 0.077 μM, respectively In Vivo SGC-iMLLT shows moderate metabolic resistance with t 1/2 of 53 min and 48 % remaining after 60 min, and the primary process for metabolism is N demethylation . MCE has not independently confirmed the accuracy of these methods. They are for reference only. IC50& Target:IC50: 0.26 μM (MLLT1 YD), Kd: 0.077 μM (MLLT3 YD), 0.129 μM (MLLT1 YD)
