Supplemental Figures and Tables from Discovery of Potent and Selective MRCK Inhibitors with Therapeutic Effect on Skin Cancer

Abstract

<p>Supplemental Figure 1. Kinome selectivity profiles for BDP8900 and BDP9066. Supplemental Figure 2. Cancer cell line sensitivity to BDP8900 and BDP9066. Supplemental Figure 3. MRCKα phosphorylations compared with MRCKβ. Supplemental Figure 4. MRCKα, MRCKβ and MRCKα pS1003 antibody validation. Supplemental Figure 5. MRCK and DMPK expression in MDA MB 231 D3H2 LN human breast cancer cells, SCC12 human squamous cell carcinoma cells, and human skeletal muscle. Supplemental Table 1. Crystallographic data and model statistics. Supplemental Table 2: BDP8900 and BDP9066 selectivity in vitro (in-house determinations). Supplemental Table 3. Kinase selectivity screen for BDP8900 and BDP9066. Supplemental Table 4. BDP8900 selectivity in vitro (out-sourced determinations). Supplemental Table 5. BDP9066 selectivity in vitro (out-sourced determinations). Supplemental Table 6. Cancer cell line EC50 values for BDP8900 and BDP9066. Supplemental Table 7. MRCKα phosphorylation sites. Supplemental Table 8. MRCKα phosphorylation on S1003.</p>