Aminopyrazine Inhibitors Binding to an Unusual Inactive Conformation of the Mitotic Kinase Nek2: SAR and Structural Characterization was written by Whelligan, Daniel K.;Solanki, Savade;Taylor, Dawn;Thomson, Douglas W.;Cheung, Kwai-Ming J.;Boxall, Kathy;Mas-Droux, Corine;Barillari, Caterina;Burns, Samantha;Grummitt, Charles G.;Collins, Ian;van Montfort, Rob L. M.;Aherne, G. Wynne;Bayliss, Richard;Hoelder, Swen. And the article was included in Journal of Medicinal Chemistry in 2010.Quality Control of Methyl 2-methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoate This article mentions the following:
We report herein the first systematic exploration of inhibitors of the mitotic kinase Nek2. Starting from HTS hit aminopyrazine I, compounds with improved activity were identified using structure-based design. Our structural biol. investigations reveal two notable observations. First, I and related compounds bind to an unusual, inactive conformation of the kinase which to the best of our knowledge has not been reported for other types of kinase inhibitors. Second, a phenylalanine residue at the center of the ATP pocket strongly affects the ability of the inhibitor to bind to the protein. The implications of these observations are discussed, and the work described here defines key features for potent and selective Nek2 inhibition, which will aid the identification of more advanced inhibitors of Nek2. In the experiment, the researchers used many compounds, for example, Methyl 2-methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoate (cas: 525362-07-6Quality Control of Methyl 2-methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoate).
Methyl 2-methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoate (cas: 525362-07-6) belongs to esters. Esters perform as high-grade solvents for a broad array of plastics, plasticizers, resins, and lacquers, and are one of the largest classes of synthetic lubricants on the commercial market. Acyl chlorides and acid anhydrides alcoholysis is another way to produce esters. Acyl chlorides and acid anhydrides react with alcohols to produce esters. Anydrous conditions are recommended since both acyl chlorides and acid anhydrides react with water.Quality Control of Methyl 2-methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoate
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics