eCF309: a potent, selective and cell-permeable mTOR inhibitor was written by Fraser, Craig;Carragher, Neil O.;Unciti-Broceta, Asier. And the article was included in MedChemComm in 2016.Recommanded Product: 7-Azaindole-5-boronic Acid Pinacol Ester This article mentions the following:
Kinase inhibitors capable of blocking the phosphorylation of protein substrates with high selectivity are essential to probe and elucidate the etiol. role of such mols. and their signalling pathways. By addressing these biochem. questions in disease relevant cell-based and in vivo models, strong pharmacol. evidence can be generated towards validating or disproving a target hypothesis. Pharmacol. studies can also provide fundamental information to identify appropriate biomarkers and rational drug combination strategies and thereby facilitate clin. translation. However, due to the high number of kinases encoded by the human genome (>500) and their highly conserved catalytic domains, the development of such an elite class of inhibitors-a.k.a. high-quality chem. probes-represents a major challenge. Through a ligand-based inhibitor design, focused library synthesis and phenotypic screening to prioritize compounds with potent cell activity, we recently identified a cell cycle inhibitor with micromolar potency that inhibits mTOR kinase activity. Following a rapid lead optimization campaign, we report the development of eCF309, an mTOR inhibitor displaying low nanomolar potency both in vitro and in cells and an excellent selectivity profile (S-score (35%) = 0.01 at 10 μM). In the experiment, the researchers used many compounds, for example, 7-Azaindole-5-boronic Acid Pinacol Ester (cas: 754214-56-7Recommanded Product: 7-Azaindole-5-boronic Acid Pinacol Ester).
7-Azaindole-5-boronic Acid Pinacol Ester (cas: 754214-56-7) belongs to indole derivatives. Indole is an important structural motif of various drugs, therapeutic leads besides its prevalence in numerous natural products, agrochemicals, perfumery, and dyes. They are capable of binding to a variety of receptors with high affinity and thus have applications in a wide range of therapeutic areas.Recommanded Product: 7-Azaindole-5-boronic Acid Pinacol Ester
Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles