| Bioactivity | H122 is a PROTAC degrader for TEAD that degrades TEAD1 with a DC50 of 3 nM, and exhibits good affinity to TEAD2, TEAD3, and TEAD4 with Ki of 2.0, 3.6 and 1.6 nM. H122 downregulates the expression of Myc. H122 inhibits the cell growth of MSTO-211H and NCI-H226 with IC50 of 21.3 nM and 0.6 nM, and exhibits antitumor efficacy in mouse models[1]. (Pink: ligand for target protein (HY-151525); Black: linker (HY-W573128); Blue: ligand for E3 ligase Cereblon (HY-W087383)) |
| Formula | C45H45ClFN5O8 |
| Molar Mass | 838.32 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Lu Y, et al., Selective Degradation of TEADs by a PROTAC Molecule Exhibited Robust Anticancer Efficacy In Vitro and In Vivo. J Med Chem. 2025 Jan 13. |