HC278

HC278 (50-500 nM; 2-18 h) is a bona fide, proteasome- and CRBN-dependent PROTAC that potently and selectively degrades TEAD1 and TEAD3 in HEK293 stable cells expressing epitope-tagged TEAD1-4, with significant degradation observed at 50 nM, while having minimal effect on TEAD2 and weak activity against TEAD4 at 500 nM^[1].
HC278 (100-200 nM; two weeks) specifically inhibits the colony-forming ability of YAP-dependent NCI-H226 mesothelioma cells at 200 nM, while having no effect on NCI-H28 control mesothelioma cells^[1].
HC278 (500 nM; 24 h) inhibits TEAD/YAP transcriptional activity in NCI-H226 mesothelioma cells, significantly downregulating YAP signature genes and specific target genes including CTGF, CYR61, and ANKRD1 at 500 nM for 24 h^[1].
HC278 (500 nM-1 μM; 24 h) downregulates YAP target gene expression (CTGF, CYR61, ANKRD1) in MDA-MB-231 cells at 500 nM and 1 μM for 24 h^[1].

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