Extended knowledge of 1-Chloro-10H-phenothiazine

One of the oldest and most widely used commercial enzyme inhibitors is aspirin, Application of 1910-85-6, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about Application of 1910-85-6

Application of 1910-85-6, Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 1910-85-6, Name is 1-Chloro-10H-phenothiazine, molecular formula is C12H8ClNS. In a Article, authors is Voegerl, Katharina£¬once mentioned of 1910-85-6

Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors

The phenothiazine system was identified as a favorable cap group for potent and selective histone deacetylase 6 (HDAC6) inhibitors. Here, we report the preparation and systematic variation of phenothiazines and their analogues containing a benzhydroxamic acid moiety as the zinc-binding group. We evaluated their ability to selectively inhibit HDAC6 by a recombinant HDAC enzyme assay, by determining the protein acetylation levels in cells by western blotting (tubulin vs histone acetylation), and by assessing their effects on various cancer cell lines. Structure-activity relationship studies revealed that incorporation of a nitrogen atom into the phenothiazine framework results in increased potency and selectivity for HDAC6 (more than 500-fold selectivity relative to the inhibition of HDAC1, HDAC4, and HDAC8), as rationalized by molecular modeling and docking studies. The binding mode was confirmed by co-crystallization of the potent azaphenothiazine inhibitor with catalytic domain 2 from Danio rerio HDAC6.

One of the oldest and most widely used commercial enzyme inhibitors is aspirin, Application of 1910-85-6, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about Application of 1910-85-6

Reference£º
Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem