IK-930 (IK930) is a selective, oral TEAD inhibitor that selectively inhibits TEAD-dependent transcription by directly blocking autopalmitoylation.
IK-930 is inactive in a broad panel of kinases, receptors, and transporters, furthering evidence of selectivity.
IK-930 inhibits in vitro proliferation of Hippo pathway-deficient cancer cell lines, but not Hippo pathway wild type cells.
IK-930 demonstrates antitumor activity in mouse xenograft models with Hippo pathway genetic alterations.
IK-930 enhances apoptosis and in vivo antitumor activity in combination with EGFR and MEK inhibitors, respectively, in EGFR or KRAS mutated tumors.
