SM1-71 is a cell penetrant and potent multi-targeted kinase inhibitor that engages kinases through both reversible and irreversible binding. SM1-71 covalently inhibits 23 kinases including 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. It binds to the cysteine located in vicinity of active site. In some cases, SM1-71 might bind to Cys located at allosteric places. SM1-71 potently inhibits growth of multiple cancer cell lines.
cell penetrant and potent multi-targeted kinase inhibitor that engages kinases through both reversible and irreversible binding
The Journal of biological chemistry, 294(21), 8664-8673 (2019-03-13)
Most cancer cells are dependent on a network of deregulated signaling pathways for survival and are insensitive, or rapidly evolve resistance, to selective inhibitors aimed at a single target. For these reasons, drugs that target more than one protein (polypharmacology)
TAK1 (transforming growth factor-β-activated kinase 1) is an essential intracellular mediator of cytokine and growth factor signaling and a potential therapeutic target for the treatment of immune diseases and cancer. Herein we report development of a series of 2,4-disubstituted pyrimidine
Cell chemical biology, 26(6), 818-829 (2019-04-16)
Covalent kinase inhibitors, which typically target cysteine residues, represent an important class of clinically relevant compounds. Approximately 215 kinases are known to have potentially targetable cysteines distributed across 18 spatially distinct locations proximal to the ATP-binding pocket. However, only 40
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