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. 2024 Aug 29;67(17):15012–15028. doi: 10.1021/acs.jmedchem.4c00577

Figure 4.

Figure 4

Degradation of endogenous MLK3 by CEP1347-VHL-02 PROTAC in MCF-7 and MDA-MB-468 cell lines. (A) Western blot analysis of MLK3 levels in MCF-7 and MDA-MB-468 cell lines treated with 1 μM CEP1347-VHL-02 PROTAC for the indicated times (4–48 h). DMSO was used as a control. The percentage of remaining MLK3 protein during the time of treatment was quantified and plotted in the lower panel, and t1/2 of the PROTAC reaction was determined. (B) Western blot analysis of MLK3 levels in MCF-7 and MDA-MB-468 cell lines after 24 h treatment with CEP1347-VHL-02 PROTAC at a concentration range of 0.1–5 μM. DMSO was used as a control. The percentage of remaining MLK3 protein for the indicated concentration range was quantified and plotted in the lower panel, and DC50 and Dmax were determined. (C) Western blot analysis of MLK3 levels in MCF-7 and MDA-MB-468 cell lines pretreated with 1 μM carfilzomib for 1 h, followed by 1 μM CEP1347-VHL-02 PROTAC treatment for 7 h. DMSO was used as a control.