SM1-71

SM1-71 (compound 5) is a potent TAK1 inhibitor, with a K i of 160 nM, it also can covalently inhibit MKNK2 , MAP2K1/2/3/4/6/7 , GAK , AAK1 , BMP2K , MAP3K7 , MAPKAPK5 , GSK3A/B , MAPK1/3 , SRC , YES1 , FGFR1 , ZAK (MLTK) , MAP3K1 , LIMK1 and RSK2 . SM1-71 can inhibit proliferation of multiple cancer cell lines In Vitro SM1-71 (0.001-100 μM; 72 h) potently inhibits the proliferation of H23 and Calu-6 non-small cell lung cancer cell lines with a concentration-dependent manner. SM1-71 (72 h) induces potent cytotoxicity with nanomolar values for GR 50 and negative GR max values in eight of 11 cancer cell lines. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: H23-KRAS G12C and Calu-6-KRAS Q61K cells Concentration: 0.001, 0.01, 0.1, 1, 10, 100 μM Incubation Time: 72 hours Result: Inhibited proliferation of H23-KRAS G12C and Calu-6-KRAS Q61K cells with IC 50 s of 0.4 and 0.3 μM, respectively. IC50& Target:IC50: 0.8 nM (GAK), 0.8 nM (YES1), 2 nM (SRC), 4.4 nM (AAK1), 5.4 nM (LIMK1), 7.1 nM (BMP2K), 9.3 nM (MAP2K2), 10.4 nM (MAP2K1), 28.7 nM (MAP3K1), 48.3 nM (MAPK1), 107 nM (MAPK3)

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