《Structure-Based Design of Tricyclic NF-κB Inducing Kinase (NIK) Inhibitors That Have High Selectivity over Phosphoinositide-3-kinase (PI3K)》 was written by Castanedo, Georgette M.; Blaquiere, Nicole; Beresini, Maureen; Bravo, Brandon; Brightbill, Hans; Chen, Jacob; Cui, Hai-Feng; Eigenbrot, Charles; Everett, Christine; Feng, Jianwen; Godemann, Robert; Gogol, Emily; Hymowitz, Sarah; Johnson, Adam; Kayagaki, Nobuhiko; Kohli, Pawan Bir; Knuppel, Kathleen; Kraemer, Joachim; Kruger, Susan; Loke, Pui; McEwan, Paul; Montalbetti, Christian; Roberts, David A.; Smith, Myron; Steinbacher, Stefan; Sujatha-Bhaskar, Swathi; Takahashi, Ryan; Wang, Xiaolu; Wu, Lawren C.; Zhang, Yamin; Staben, Steven T.. Product Details of 16982-21-1This research focused ontricyclic benzoxepin preparation NFkappaB inducing kinase inhibitor phosphoinositidekinase PI3K. The article conveys some information:
The authors report a structure-guided optimization of a novel series of NF-κB inducing kinase (NIK) inhibitors. Starting from a modestly potent, low mol. weight lead, activity was improved by designing a type I1/2 binding mode that accessed a back pocket past the methionine-471 gatekeeper. Divergent binding modes in NIK and PI3K were used to dampen PI3K-inhibition while maintaining NIK inhibition within these series. Potent compounds were discovered that selectively inhibit the nuclear translocation of NF-kB2 (p52/REL-B) but not canonical NF-kB1 (REL-A/p50). The results came from multiple reactions, including the reaction of Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1Product Details of 16982-21-1)
Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1) belongs to anime. Large quantities of aliphatic amines are made synthetically. The most widely used industrial method is the reaction of alcohols with ammonia at a high temperature, catalyzed by metals or metal oxide catalysts (e.g., nickel or copper). Mixtures of primary, secondary, and tertiary amines are thereby produced.Product Details of 16982-21-1
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