H122
Product Specifications
Target
YAP|||PROTACs|||c-Myc
Related Pathways
Cell Cycle/Checkpoint|||PROTAC|||Stem Cells
Bioactivity
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)
Smiles
COCCOC1=C(C(=C(C=C1)C(=O)N)C2=C(C=CC3=C2C[C@@](O3)(CNCCC4CCN(CC4)C5=CC6=C(C=C5)C(=O)N(C6=O)C7CCC(=O)NC7=O)C8=CC=CC=C8)Cl)F
Molecular Formula
C45H45ClFN5O8
Molecular Weight
838.319
Shipping Conditions
Cool pack
Storage Temperature
-20°C
Available Sizes
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