Jiang, Xueyang; Zhou, Junting; Wang, Yang; Liu, Xin; Xu, Kaiying; Xu, Jian; Feng, Feng; Sun, Haopeng published an article in 2021. The article was titled 《PROTACs suppression of GSK-3β, a crucial kinase in neurodegenerative diseases》, and you may find the article in European Journal of Medicinal Chemistry.HPLC of Formula: 51857-17-1 The information in the text is summarized as follows:
Glycogen synthase kinase 3β (GSK-3β) is involved in a variety of diseases such as neurodegenerative diseases, bipolar disorder, and diabetes. In this study, a series of heterobifunctional small mol. proteolysis targeting chimera (PROTAC) were designed and synthesized based on E3 ubiquitin ligase cereblon (CRBN). Most of PROTACs displayed good inhibitory activity, with the IC50 values at the double-digits nanomolar levels and moderate protein degradation ability against GSK-3β. Western-blot data showed compound PG21(I) can effectively degrade GSK-3β in a dose-dependent manner, which can induce 44.2% protein degradation at 2.8μM. Further pharmacol. experiments revealed that the ability of PG21 to degrade GSK-3β is mediated by the ubiquitin-proteasome system (UPS). In addition, PG21 protects against glutamate-induced cell death in HT-22 cells. As the first PROTAC example to degrade GSK-3β protein, the present study has provided potential candidates for further investigation in the biol. function of GSK-3β protein and its association with diseases. In the part of experimental materials, we found many familiar compounds, such as N-Boc-1,6-Diaminohexane(cas: 51857-17-1HPLC of Formula: 51857-17-1)
N-Boc-1,6-Diaminohexane(cas: 51857-17-1) is a compound useful in organic synthesis used in the preparation of mixed self-assembled monolayers (SAMs) that resist adsorption of proteins using the reaction of amines with a SAM that presents interchain carboxylic anhydride groupsHPLC of Formula: 51857-17-1
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