KG-FP-003 is a highly potent, selective, and durable TEAD PROTAC degrader (TEAD1 DC 50 = 6 ± 4 nM, TEAD2 DC 50 = 68 ± 15 nM, TEAD3 DC 50 = 12 ± 5 nM, TEAD4 DC 50 = 7 ± 5 nM). KG-FP-003 promotes ubiquitination and degradation of TEAD . KG-FP-003 exhibits anticancer activity against mesothelioma and ovarian cancer . (Pink: TEAD ligand ( HY-186118 ); Blue: Cereblon E3 ligase ligand; Black: linker).
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