E3 ligase Ligand-Linker Conjugates 50|安捷凯

E3 ligase Ligand-Linker Conjugates 50

E3 ligase Ligand-Linker Conjugates 50 包含用于 E3 泛素连接酶的 cereblon (CRBN) 配体和 linker。E3 ligase Ligand-Linker Conjugates 50 可通过 PROTAC 技术合成选择性的 CDK6 降解剂 CP-10。CP-10 诱导 CDK6 降解，DC50 为 2.1 nM。

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Background

E3 ligase Ligand-Linker Conjugates 50 incorporates a cereblon (CRBN) ligand for the E3 ubiquitin ligase, and a PROTAC linker. E3 ligase Ligand-Linker Conjugates 50 can be used to design a selective CDK6 PROTAC degrader CP-10. CP-10 induces the degradation of CDK6 with an DC50 of 2.1 nM[1]. Cereblon

[1]. Su S, et al. Potent and Preferential Degradation of CDK6 via Proteolysis Targeting Chimera Degraders. J Med Chem. 2019 Aug 2.