GAS41 YEATS inhibitor 19 (GAS41 YEATS-IN-19) is potent, selective, cell-permeable dimeric inhibitor of GAS41 YEATS domain with IC50 of 18 nM (AlphaScreen competition assay).
GAS41 YEATS inhibitor 19 bind to GAS41 YEATS domain in a channel constituting a recognition site for acylated lysine on histone proteins, facilitate specific dimerization of the GAS41 YEATS domain.
GAS41 YEATS inhibitor 19 disrupted GAS41 interactions with acetylated histone H3 in cells with IC50 of 6 uM in the NanoBiT assay.
GAS41 YEATS inhibitor 19 induced dose-dependent cell growth inhibition with GI50 of 3 uM in treated H1299 cells.
GAS41 YEATS inhibitor 19 represents a valuable chemical tool and may further serve to explore the inhibition of GAS41 in cancer models.GAS41 YEATS inhibitor 19 (GAS41 YEATS-IN-19) is potent, selective, cell-permeable dimeric inhibitor of GAS41 YEATS domain with IC50 of 18 nM (AlphaScreen competition assay).
GAS41 YEATS inhibitor 19 bind to GAS41 YEATS domain in a channel constituting a recognition site for acylated lysine on histone proteins, facilitate specific dimerization of the GAS41 YEATS domain.
GAS41 YEATS inhibitor 19 disrupted GAS41 interactions with acetylated histone H3 in cells with IC50 of 6 uM in the NanoBiT assay.
GAS41 YEATS inhibitor 19 induced dose-dependent cell growth inhibition with GI50 of 3 uM in treated H1299 cells.
GAS41 YEATS inhibitor 19 represents a valuable chemical tool and may further serve to explore the inhibition of GAS41 in cancer models.
GAS41 is an emerging oncogene overexpressed and implicated in multiple cancers, including NSCLC. GAS41 is a dimeric protein that contains the YEATS domain, which is involved in the recognition of lysine-acylated histones.