IEM930 is a small molecule inhibitor targeting the GAS41 YEATS domain (YEATS4) with ITC binding Kd of 32.6 uM, inhibits GAS41/ITGA4-mediated PI3K/Akt/mTOR signaling pathway in glioma cells.
IEM930 inhibits proliferative activities in glioma cell lines with IC50 of 50 uM for U87 cells.
IEM930 inhibits colony formation of U87 and U251 cells in a dose-dependent manner, induces less antiproliferative effect in GAS41-depleted U87 cells than that in U87 cells.
IEM930 treatment significantly reduced ITGA4 mRNA and protein levels in U87 cells but not U87-shGAS41-1# cells.
IEM930 primarily targets the GAS41/ITGA4-mediated PI3K/Akt/mTOR signaling pathway in glioma cells.
Glioma Amplified Sequence 41 (GAS41, also known as YEATS4) was previously isolated from glioblastomas and is frequently amplified in various human gliomas.
GAS41 belongs to the YEATS domain-containing protein family, including ENL, Taf14, Yaf9 and AF9.