Design, synthesis, and testing of potent, selective hepsin inhibitors via application of an automated closed-loop optimization platform was written by Pant, Shishir M.;Mukonoweshuro, Amanda;Desai, Bimbisar;Ramjee, Manoj K.;Selway, Christopher N.;Tarver, Gary J.;Wright, Adrian G.;Birchall, Kristian;Chapman, Timothy M.;Tervonen, Topi A.;Klefstrom, Juha. And the article was included in Journal of Medicinal Chemistry in 2018.Related Products of 777-44-6 This article mentions the following:
Hepsin is a membrane-anchored serine protease whose role in hepatocyte growth factor (HGF) signaling and epithelial integrity makes it a target of therapeutic interest in carcinogenesis and metastasis. Using an integrated design, synthesis, and screening platform, we were able to rapidly develop potent and selective inhibitors of hepsin. In progressing from the initial hit (I) to compound (II), the IC50 value against hepsin was improved from â? μM to 22 nM, and the selectivity over urokinase-type plasminogen activator (uPA) was increased from 30-fold to >6000-fold. Subsequent in vitro ADMET profiling and cellular studies confirmed that the leading compounds are useful tools for interrogating the role of hepsin in breast tumorigenesis. In the experiment, the researchers used many compounds, for example, 3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6Related Products of 777-44-6).
3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6) belongs to organic chlorides. Organic chlorides can be used in production of: PVC, pesticides, chloromethane, teflon, insulators. Organochlorine compounds are lipophylic, meaning they are more soluble in fat than in water. This gives them a high tenancy to accumulate in the food chain (biomagnification).Related Products of 777-44-6
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics