MS 154 is a potent and selective cereblon-recruiting Degrader (PROTAC®) of mutant epidermal growth factor receptor (EGFR), comprising a cereblon-binding moiety joined by a linker to gefitinib(Iressa). MS 154 decreases EGFR protein levels, inhibits downstream signaling in and inhibits proliferation of mutant EGFR-bearing lung cancer cells (DC50values are 11 and 25 nM in HCC-827 and H3255 cells, respectively; Dmax> 95% at 50 nM), but not in WT-EGFR-bearing ovarian and lung cancer cells lines. Bioavailable in mice following ip administration.
NSC-670224 is an inhibitor of histone deacetylases-6 (HDAC6) and nuclear factor-κB (NF-κB) activation blocker. It has been shown to be toxic to Saccharomyces cerevisiae at low micromolar concentrations, potentially acts via a mechanism of action related t
CCT036477 is a selective inhibitor of wingless-type MMTV integration site family dependent transcription. CCT036477reduces the transcriptional activity of the T-cell factor and lymphoid enhancer factor transcription factor family at the ß-catenin level.