BI-7190 (BI 7190) is a potent, selective chemical probe targeting the bromodomain of BPTF with binding Kd of 3.5 nM.
BI-7190 shows high binding affinity for bromodomain BPTF with Kd of 131 nM in ITC assays.
BI-7190 shows decreased the affinity for BRD9 (Kd=18.4 nM).
BI-7190 showed only weak cellular target engagement against the off-target bromodomains.
BI-7190 (1 uM) induced minor transcriptional modulation in NCI-H1437 cells over 120 h, including CLCF1, CLMP, and CLSPN.
BI-7190 is a suitable tool compound for in vivo efficacy and mode-of-action studies, as well as for PROTAC design.
