SML2738
SM1-71
≥98% (HPLC)
Sinônimo(s):
N-[2-[[5-Chloro-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]amino]phenyl]-2-propenamide
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About This Item
Produtos recomendados
Nível de qualidade
Ensaio
≥98% (HPLC)
forma
powder
cor
white to beige
solubilidade
DMSO: 2 mg/mL, clear
temperatura de armazenamento
2-8°C
Ações bioquímicas/fisiológicas
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.
Código de classe de armazenamento
11 - Combustible Solids
Classe de risco de água (WGK)
WGK 3
Ponto de fulgor (°F)
Not applicable
Ponto de fulgor (°C)
Not applicable
Certificados de análise (COA)
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Bioorganic & medicinal chemistry, 25(3), 838-846 (2016-12-25)
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
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)
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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