PROTAC CDK2/9 Degrader-1

PROTAC CDK2/9 Degrader-1 (Compound F3) is a potent dual degrader for CDK2 ( DC 50 =62 nM) and CDK9 ( DC 50 =33 nM). PROTAC CDK2/9 Degrader-1 suppresses prostate cancer PC-3 cell proliferation (IC 50 =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 Cereblon ligand In Vitro PROTAC CDK2/9 Degrader-1 (0.25-3 μM; 48 hours) induces cell cycle blockage at the G2/M phase. ? PROTAC CDK2/9 Degrader-1 (500 nM; 2-24 hours) down-regulates the Mcl-1 protein level in PC-3 cells. ? 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. ? PROTAC CDK2/9 Degrader-1 inhibits both CDK2 and CDK9, with IC 50 as 7.42 nM and 14.50 nM, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Cycle AnalysisCell Line: PC-3 cells Concentration: 500 nM Incubation Time: 2, 4, 8, 16, 24 hours Result: Down-regulated the Mcl-1 protein level in PC-3 cells. Western Blot AnalysisCell Line: PC-3 cells Concentration: 0.25, 1, 3 μM Incubation Time: 48 hours Result: Induced cell cycle blockage at the G2/M phase. Form:Solid IC50& Target:CDK2 62 nM (DC 50 ) CDK9 33 nM (DC 50 ) Cereblon

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