Investigations on small molecule inhibitors targeting the histone H3K4 tri-methyllysine binding PHD-finger of JmjC histone demethylases was written by Bhushan, Bhaskar;Erdmann, Alexandre;Zhang, Yijia;Belle, Roman;Johannson, Catrine;Oppermann, Udo;Hopkinson, Richard J.;Schofield, Christopher J.;Kawamura, Akane. And the article was included in Bioorganic & Medicinal Chemistry in 2018.Recommanded Product: 1195-14-8 This article mentions the following:
Plant homeodomain (PHD) finger containing proteins are important epigenetic regulators and are of interest as potential drug targets. Inspired by the amiodarone derivatives reported to inhibit the PHD finger 3 of KDM5A (KDM5A(PHD3)), a set of compounds were synthesized. Amiodarone and its derivatives were observed to weakly disrupt the interactions of a histone H3K4me3 peptide with KDM5A(PHD3). Selected amiodarone derivatives inhibited catalysis of KDM5A, but in a PHD-finger independent manner. Amiodarone derivatives also bind to H3K4me3-binding PHD-fingers from the KDM7 subfamily. Further work is required to develop potent and selective PHD finger inhibitors. In the experiment, the researchers used many compounds, for example, 2-Methylbenzo[b]thiophene (cas: 1195-14-8Recommanded Product: 1195-14-8).
2-Methylbenzo[b]thiophene (cas: 1195-14-8) belongs to benzothiophene derivatives. Benzothiophene is used as starting material for the synthesis of bioactive molecules. The core structure is a part of various pharmaceutical substances and natural products. Due to its aromaticity, thiophenes do not exhibit the same properties as conventional thioethers.Recommanded Product: 1195-14-8
Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem