Fig. 3. (A) Head-to-head comparison of vemurafenib-based PROTACs (cmpd 12, SJF-0628), the negative control SJF-0661 with paradox-breaker PROTACs 25 and 26. SK-MEL-28 cells were treated with 10 μM compounds for 24 h; (B) in the NRAS mutant cell line SK-N-AS, SJF-0628 but not 25 (CST905) induced paradoxical ERK-signalling. Cells were treated for 4 h at the dose indicated. Quantified values for BRAFV600E, pERK1/2, and pMEK1/2 refer to mean of duplicates.
