Reference of N-Boc-1,6-DiaminohexaneIn 2021 ,《Selective degradation-inducing probes for studying cereblon (CRBN) biology》 was published in RSC Medicinal Chemistry. The article was written by Powell, Chelsea E.; Du, Guangyan; Bushman, Jonathan W.; He, Zhixiang; Zhang, Tinghu; Fischer, Eric S.; Gray, Nathanael S.. The article contains the following contents:
Targeted protein degradation represents a rapidly growing area in drug discovery and development. Moreover, small mols. that induce the targeted degradation of a given protein also represent an important addition to the chem. probes toolbox as these compounds can achieve selective protein knockdown, thus providing an approach that is orthogonal to genetic knockdowns. In order to develop degradation-inducing chem. probes for studying cereblon (CRBN) biol., we generated six CRBN-CRBN (homo-PROTAC) degraders and six CRBN-VHL (hetero-PROTAC) degraders. From these compounds we identified two potent and selective CRBN degraders (ZXH-4-130 and ZXH-4-137), both of which are CRBN-VHL compounds We characterized these lead degraders by quant. proteomics in five cell lines (MM1.S, Kelly, SK-N-DZ, HEK293T, and MOLT-4) and observed high selectivity for CRBN in all cell lines. Furthermore, we directly compared our compounds to current lead CRBN degraders and demonstrated how these probes can be used as chem. knockdown reagents for studying CRBN-dependent processes. Overall, our work provides a roadmap for thorough degrader characterization by combination western and proteomic anal., as illustrated by the identification of ZXH-4-130 and ZXH-4-137 as CRBN-knockdown tool compounds suitable for cell-based studies. In addition to this study using N-Boc-1,6-Diaminohexane, there are many other studies that have used N-Boc-1,6-Diaminohexane(cas: 51857-17-1Reference of N-Boc-1,6-Diaminohexane) was used in this study.
N-Boc-1,6-Diaminohexane(cas: 51857-17-1) is used to prepare 1,3-Bis[6-(Boc-amino)hexyl]urea by reacting with carbonyl dichloride in the presence of triethylamine. Further, it is used as a reagent for the introduction of a C6-spacer.Reference of N-Boc-1,6-Diaminohexane
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