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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

Product Datasheet

https://www.targetmol.com/attachment/DataSheet/315447026521210976/T204932

Available Sizes

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