PROTAC CDK2/9 Degrader-1 (Compound F3) 是 CDK2 (DC50=62 nM) 和 CDK9 (DC50=33 nM) 的有效双降解剂。PROTAC CDK2/9 Degrader-1 通过有效阻断前列腺癌 PC-3 细胞S期和 G2/M 期的细胞周期，抑制前列腺癌 PC-3 细胞增殖 (IC50=0.12 µM)。PROTAC CDK2/9 Degrader-1 是一种 CDK 抑制剂与 CRBN 配体结合的 PROTAC。
PROTAC CDK2/9 Degrader-1 (Compound F3) is a potent dual degrader for CDK2 (DC50=62 nM) and CDK9 (DC50=33 nM). PROTAC CDK2/9 Degrader-1 suppresses prostate cancer PC-3 cell proliferation (IC50=0.12 µM) by effectively blocking the cell cycle in S and G2/M phases. PROTAC CDK2/9 Degrader-1 is a PROTAC by tethering CDK inhibitor with CRBN ligand[1].
PROTAC CDK2/9 Degrader-1 (0.25-3 μM; 48 hours) induces cell cycle blockage at the G2/M phase[1].PROTAC CDK2/9 Degrader-1 (500 nM; 2-24 hours) down-regulates the Mcl-1 protein level in PC-3 cells[1].PROTAC CDK2/9 Degrader-1 effectively degrades CDK2/9 in cell lines MCF-7, HCT-116 and 22Rv1, which all have high CDK2/9 expression[1].PROTAC CDK2/9 Degrader-1 inhibits both CDK2 and CDK9, with IC50 as 7.42 nM and 14.50 nM, respectively[1].
[1]. Zhou F, et al. Development of selective mono or dual PROTAC degrader probe of CDK isoforms. Eur J Med Chem. 2019 Dec 6;187:111952.
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