H122 is a TEADPROTAC degrader effective in degrading TEAD1 with a DC50 of 3 nM, and it shows strong affinity for TEAD2, TEAD3, and TEAD4 with Ki values of 2.0, 3.6, and 1.6 nM, respectively. H122 also downregulates Myc expression and inhibits the growth of MSTO-211H and NCI-H226 cells, with IC50 values of 21.3 nM and 0.6 nM, respectively, demonstrating antitumor activity in mouse models. (Pink: ligand for target protein, Black: linker, Blue: ligand for E3 ligaseCereblon)
Molecular Weight:
838.319
Formula:
C45H45ClFN5O8
Target:
YAP|||PROTACs|||c-Myc
T204932
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