CDK9 Antagonist-1|安捷凯

CDK9 Antagonist-1

CDK9 Antagonist-1 是一种基于 PROTAC 技术，高效选择性的 CDK9 降解剂，在 MCF-7 细胞系中抑制 CDK9 的 IC50 值为 17 μM。PROTAC 由天然产物汉黄芩素 (Wogonin) 与泛素 E3 连接酶 (CRBN) 通过 linker 连接而成。

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Background

CDK9 Antagonist-1 (compounds 11c) is a potent and selective CDK9 degrader based on PROTAC, with an IC50 of 17 μM in MCF-7 cell lines. Natural product Wogonin binds ubiquitin E3 ligase cereblon (CRBN) via a linker to form PROTAC[1]. CDK9|17 μM (IC50, MCF-7 cells)

[1]. Bian J , et al. Discovery of Wogonin-based PROTACs against CDK9 and capable of achieving antitumor activity. Bioorg Chem. 2018 Dec;81:373-381.