Down, Kenneth et al. published their research in Journal of Medicinal Chemistry in 2021 | CAS: 1073354-14-9

5-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)picolinaldehyde (cas: 1073354-14-9) belongs to pyridine derivatives. Pyridine is diamagnetic and has a diamagnetic susceptibility of âˆ?8.7 × 10âˆ? cm3·molâˆ?.The molecular electric dipole moment is 2.2 debyes. The standard enthalpy of formation is 100.2 kJ·molâˆ? in the liquid phase and 140.4 kJ·molâˆ? in the gas phase. Pyridine derivatives are also useful as small-molecule α-helix mimetics that inhibit protein-protein interactions, as well as functionally selective GABA ligands.Recommanded Product: 5-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)picolinaldehyde

Discovery of GSK251: A Highly Potent, Highly Selective, Orally Bioavailable Inhibitor of PI3Kδ with a Novel Binding Mode was written by Down, Kenneth;Amour, Augustin;Anderson, Niall A.;Barton, Nick;Campos, Sebastien;Cannons, Edward P.;Clissold, Cole;Convery, Maire A.;Coward, John J.;Doyle, Kevin;Duempelfeld, Birgit;Edwards, Christopher D.;Goldsmith, Michael D.;Krause, Jana;Mallett, David N.;McGonagle, Grant A.;Patel, Vipulkumar K.;Rowedder, James;Rowland, Paul;Sharpe, Andrew;Sriskantharajah, Srividya;Thomas, Daniel A.;Thomson, Douglas W.;Uddin, Sorif;Hamblin, J. Nicole;Hessel, Edith M.. And the article was included in Journal of Medicinal Chemistry in 2021.Recommanded Product: 5-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)picolinaldehyde This article mentions the following:

Optimization of a previously reported lead series of PI3Kδ inhibitors with a novel binding mode led to the identification of a clin. candidate compound 31 (GSK251)(I). Removal of an embedded Ames-pos. heteroaromatic amine by reversing a sulfonamide followed by locating an interaction with Trp760 led to a highly selective compound 9 (II). Further optimization to avoid glutathione trapping, to enhance potency and selectivity, and to optimize an oral pharmacokinetic profile led to the discovery of compound 31 (GSK251) that had a low predicted daily dose (45 mg, b.i.d) and a rat toxicity profile suitable for further development. In the experiment, the researchers used many compounds, for example, 5-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)picolinaldehyde (cas: 1073354-14-9Recommanded Product: 5-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)picolinaldehyde).

5-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)picolinaldehyde (cas: 1073354-14-9) belongs to pyridine derivatives. Pyridine is diamagnetic and has a diamagnetic susceptibility of âˆ?8.7 × 10âˆ? cm3·molâˆ?.The molecular electric dipole moment is 2.2 debyes. The standard enthalpy of formation is 100.2 kJ·molâˆ? in the liquid phase and 140.4 kJ·molâˆ? in the gas phase. Pyridine derivatives are also useful as small-molecule α-helix mimetics that inhibit protein-protein interactions, as well as functionally selective GABA ligands.Recommanded Product: 5-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)picolinaldehyde

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem