Product Details of 51857-17-1In 2020 ,《Development of selective mono or dual PROTAC degrader probe of CDK isoforms》 appeared in European Journal of Medicinal Chemistry. The author of the article were Zhou, Fei; Chen, Luyu; Cao, Chaoguo; Yu, Jiang; Luo, Xiaojiao; Zhou, Peiting; Zhao, Lifeng; Du, Wu; Cheng, Jijun; Xie, Yongmei; Chen, Yuanwei. The article conveys some information:
Cyclin-dependent kinase (CDK) family members are promising mol. targets in discovering potent inhibitors in disease settings, they function differentially. CDK2, CDK4 and CDK6, directly regulate the cell cycle, while CDK9 primarily modulates the transcription regulation. In discovering inhibitors of these CDKs, toxicity associated with off-target effect on other CDK homologs often posts as a clin. issue and hinders their further therapeutic development. To improve efficacy and reduce toxicity, here, using the Proteolysis Targeted Chimeras (PROTACs) approach, we design and further optimize small mol. degraders targeting multiple CDKs. We showed that heterobifunctional compound A9 selectively degraded CDK2. We also identified a dual-degrader, compound F3, which potently induced degradation of both CDK2 (DC50: 62 nM) and CDK9 (DC50: 33 nM). In human prostate cancer PC-3 cells, compound F3 potently inhibits cell proliferation by effectively blocking the cell cycle in S and G2/M phases. Our preliminary data suggests that PROTAC-oriented CDK2/9 degradation is potentially an effective therapeutic approach. In the experimental materials used by the author, we found N-Boc-1,6-Diaminohexane(cas: 51857-17-1Product Details of 51857-17-1)
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.Product Details of 51857-17-1
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