Henning, Nathaniel J. published the artcileDiscovery of a Covalent FEM1B Recruiter for Targeted Protein Degradation Applications, SDS of cas: 79-07-2, the publication is Journal of the American Chemical Society (2022), 144(2), 701-708, database is CAplus and MEDLINE.
A cysteine-reactive covalent ligand, EN106, that targets FEM1B, an E3 ligase recently discovered as the critical component of the cellular response to reductive stress was disclosed. By targeting C186 in FEM1B, EN106 disrupted recognition of the key reductive stress substrate of FEM1B, FNIP1. Further established that EN106 was used as a covalent recruiter for FEM1B in TPD applications by demonstrating that a PROTAC linking EN106 to the BET Bromodomain inhibitor JQ1 or the kinase inhibitor dasatinib led to the degradation of BRD4 and BCR-ABL, resp. Study showcased a covalent ligand that targets a natural E3 ligase-substrate binding site and highlights the utility of covalent ligand screening in expanding the arsenal of E3 ligase recruiters suitable for TPD applications.
Journal of the American Chemical Society published new progress about 79-07-2. 79-07-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Aliphatic hydrocarbon chain,Amide,Inhibitor, name is 2-Chloroacetamide, and the molecular formula is C2H4ClNO, SDS of cas: 79-07-2.
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