Zapf, Christoph W. published the artcileCovalent Inhibitors of Interleukin-2 Inducible T Cell Kinase (Itk) with Nanomolar Potency in a Whole-Blood Assay, HPLC of Formula: 774170-15-9, the publication is Journal of Medicinal Chemistry (2012), 55(22), 10047-10063, database is CAplus and MEDLINE.
We wish to report a strategy that targets interleukin-2 inducible T cell kinase (Itk) with covalent inhibitors. Thus far, covalent inhibition of Itk has not been disclosed in the literature. Structure-based drug design was utilized to achieve low nanomolar potency of the disclosed series even at high ATP concentrations Kinetic measurements confirmed an irreversible binding mode with off-rate half-lives exceeding 24 h and moderate on-rates. The analogs are highly potent in a cellular IP1 assay as well as in a human whole-blood (hWB) assay. Despite a half-life of approx. 2 h in resting primary T cells, the covalent inhibition of Itk resulted in functional silencing of the TCR pathway for more than 24 h. This prolonged effect indicates that covalent inhibition is a viable strategy to target the inactivation of Itk.
Journal of Medicinal Chemistry published new progress about 774170-15-9. 774170-15-9 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester,Amine,Boronic Acids, name is (6-(Methylamino)pyridin-3-yl)boronic acid, and the molecular formula is C15H21BO2, HPLC of Formula: 774170-15-9.
Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem