Discovery of a Potent Dual SLK/STK10 Inhibitor Based on a Maleimide Scaffold was written by Serafim, Ricardo A. M.;Sorrell, Fiona J.;Berger, Benedict-Tilman;Collins, Ross J.;Vasconcelos, Stanley N. S.;Massirer, Katlin B.;Knapp, Stefan;Bennett, James;Fedorov, Oleg;Patel, Hitesh;Zuercher, William J.;Elkins, Jonathan M.. And the article was included in Journal of Medicinal Chemistry in 2021.Recommanded Product: 2-(2-Chlorophenyl)acetamide This article mentions the following:
SLK (STE20-like kinase) and STK10 (serine/threonine kinase 10) are closely related kinases whose enzymic activity is linked to the regulation of ezrin, radixin, and moesin function and to the regulation of lymphocyte migration and the cell cycle. We identified a series of 3-anilino-4-arylmaleimides as dual inhibitors of SLK and STK10 with good kinome-wide selectivity. Optimization of this series led to multiple SLK/STK10 inhibitors with nanomolar potency. Crystal structures of exemplar inhibitors bound to SLK and STK10 demonstrated the binding mode of the inhibitors and rationalized their selectivity. Cellular target engagement assays demonstrated the binding of the inhibitors to SLK and STK10 in cells. Further selectivity analyses, including anal. of activity of the reported inhibitors against off-targets in cells, identified compound 31 as the most potent and selective inhibitor of SLK and STK10 yet reported. In the experiment, the researchers used many compounds, for example, 2-(2-Chlorophenyl)acetamide (cas: 10268-06-1Recommanded Product: 2-(2-Chlorophenyl)acetamide).
2-(2-Chlorophenyl)acetamide (cas: 10268-06-1) belongs to amides. Amides include many other important biological compounds, as well as many drugs like paracetamol, penicillin and LSD. Low-molecular-weight amides, such as dimethylformamide, are common solvents. Amides can be recrystallised from large quantities of water, ethanol, ethanol/ether, aqueous ethanol, chloroform/toluene, chloroform or acetic acid. The likely impurities are the parent acids or the alkyl esters from which they have been made. The former can be removed by thorough washing with aqueous ammonia followed by recrystallisation, whereas elimination of the latter is by trituration or recrystallisation from an organic solvent.Recommanded Product: 2-(2-Chlorophenyl)acetamide
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics