Getlik, Matthaus et al. published their research in Journal of Medicinal Chemistry in 2016 | CAS: 113893-08-6

Benzo[b]thiophen-3-ylboronic acid (cas: 113893-08-6) belongs to benzothiophene derivatives. Benzothiophene is relatively a stable molecule. 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: Benzo[b]thiophen-3-ylboronic acid

Structure-Based Optimization of a Small Molecule Antagonist of the Interaction Between WD Repeat-Containing Protein 5 (WDR5) and Mixed-Lineage Leukemia 1 (MLL1) was written by Getlik, Matthaus;Smil, David;Zepeda-Velazquez, Carlos;Bolshan, Yuri;Poda, Gennady;Wu, Hong;Dong, Aiping;Kuznetsova, Ekaterina;Marcellus, Richard;Senisterra, Guillermo;Dombrovski, Ludmila;Hajian, Taraneh;Kiyota, Taira;Schapira, Matthieu;Arrowsmith, Cheryl H.;Brown, Peter J.;Vedadi, Masoud;Al-awar, Rima. And the article was included in Journal of Medicinal Chemistry in 2016.Recommanded Product: Benzo[b]thiophen-3-ylboronic acid This article mentions the following:

WD repeat-containing protein 5 (WDR5) is an important component of the multiprotein complex essential for activating mixed-lineage leukemia 1 (MLL1). Rearrangement of the MLL1 gene is associated with onset and progression of acute myeloid and lymphoblastic leukemias, and targeting the WDR5-MLL1 interaction may result in new cancer therapeutics. Our previous work showed that binding of small mol. ligands to WDR5 can modulate its interaction with MLL1, suppressing MLL1 methyltransferase activity. Initial structure-activity relationship studies identified N-(2-(4-methylpiperazin-1-yl)-5-substituted-phenyl) benzamides as potent and selective antagonists of this protein-protein interaction. Guided by crystal structure data and supported by in silico library design, we optimized the scaffold by varying the C-1 benzamide and C-5 substituents. This allowed us to develop the first highly potent (Kdisp < 100 nM) small mol. antagonists of the WDR5-MLL1 interaction and demonstrate that N-(4-(4-methylpiperazin-1-yl)-3′-(morpholinomethyl)-[1,1′-biphenyl]-3-yl)-6-oxo-4-(trifluoromethyl)-1,6-dihydropyridine-3-carboxamide 16d (OICR-9429) is a potent and selective chem. probe suitable to help dissect the biol. role of WDR5. In the experiment, the researchers used many compounds, for example, Benzo[b]thiophen-3-ylboronic acid (cas: 113893-08-6Recommanded Product: Benzo[b]thiophen-3-ylboronic acid).

Benzo[b]thiophen-3-ylboronic acid (cas: 113893-08-6) belongs to benzothiophene derivatives. Benzothiophene is relatively a stable molecule. 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: Benzo[b]thiophen-3-ylboronic acid

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem