TEAD degrader-1 

TEAD degrader-1 is a potent FBXO22-mediated molecular glue degrader of TEAD, with a 24 h DC₅₀ of 1.0 nM. TEAD degrader-1 binds reversibly and covalently to FBXO22 C326, assembles a functional ternary complex, and mediates proteasomal degradation of TEAD. TEAD degrader-1 exhibits high selectivity for the Hippo pathway and specifically downregulates only TEAD and its downstream target proteins. TEAD degrader-1 is applicable to research related to malignant pleural mesothelioma and non-small cell lung cancer^[1].

TEAD degrader-1 (compound 15) potently inhibits the TEAD1-YAP1 protein-protein interaction with an IC₅₀ of 3.1 nM in a cell-free biochemical assay^[1].
TEAD degrader-1 potently and rapidly degrades TEAD in NCI-H226 mesothelioma cells, with a DC₅₀ of 1.9 nM (6 h, 97% D_max) and 1.0 nM (24 h, 98% D_max), and sustained deep degradation for up to 72 hours^[1].
TEAD degrader-1 (24 h) potently degrades TEAD in MSTO-211H mesothelioma cells, achieving > 72% maximal degradation with a DC₅₀ < 80 nM after 24 hours^[1].
TEAD degrader-1 (24 h) potently inhibits TEAD target gene (CCN1, CCN2) expression in MSTO-211H mesothelioma cells, with > 90% maximal inhibition and an IC₅₀ < 2 nM after 24 hours^[1].
TEAD degrader-1 (120 h) potently inhibits the viability of Hippo pathway-dysregulated MSTO-211H mesothelioma cells, achieving >95% maximal growth inhibition after 120 hours^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

682.15

C₃₆H₃₈ClF₂N₃O₆

O=C(N)C1=[C@]([C@]2=C(Cl)C(F)=CC3=C2[C@H](C)[C@](C4=CC=CC=C4)(CN[C@@H]5CC[C@@H](C(N6CC(C=O)OCC6)=O)CC5)O3)C(F)=C(OC)C=C1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Fisher M, et al. Identification and SAR optimization of FBXO22-mediated TEAD Targeted Glue™ degraders. bioRxiv. 2026.