Catalog No.: PC-49537Not For Human Use, Lab Use Only.
TEAD inhibitor TM2 is a potent pan-TEAD auto-palmitoylation inhibitor with IC50 of 156 and 38 nM for TEAD2 palmitoylation and TEAD4 auto-palmitoylation, respectively, disrupts TEAD-YAP association and specifically inhibits YAP transcriptional activities.
TEAD inhibitor TM2 is a potent pan-TEAD auto-palmitoylation inhibitor with IC50 of 156 and 38 nM for TEAD2 palmitoylation and TEAD4 auto-palmitoylation, respectively, disrupts TEAD-YAP association and specifically inhibits YAP transcriptional activities.
TM2 dramatically suppresses Myc-TEAD1 palmitoylation in cells in a dose-dependent manner, also significantly inhibits endogenous TEAD1-4 palmitoylation using an antibody recognizing pan-TEADs at as low as 100 nM.
TM2 adopts a novel binding mode compared to other known TEAD inhibitors (MGH-CP1, VT105 and K975).
TM2 showed striking anti-proliferation efficacy as a single agent in human MPM, a type of tumor that is highly associated with YAP activation, also shows synergy effects in combination with a MEK inhibitor in YAP-dependent cancer cells
