CDK9-Cyclin T1 PPI-IN-1 is a selective inhibitor of the CDK9-Cyclin T1 protein-protein interaction. This compound effectively inhibits cell proliferation in triple-negative breast cancer (TNBC) MDA-MB-231 cells with an IC50 of 0.044 μM and promotes apoptosis. Additionally, CDK9-Cyclin T1 PPI-IN-1 suppresses CDK9 transcriptional activity and diminishes the phosphorylation of RNA Polymerase II at the CTD serine 2 residue. In vivo studies further demonstrate its capability to inhibit tumor growth in a TNBC 4T1 mouse model.
CDK9-Cyclin T1 PPI-IN-1 is a selective inhibitor of the CDK9-Cyclin T1 protein-protein interaction. This compound effectively inhibits cell proliferation in triple-negative breast cancer (TNBC) MDA-MB-231 cells with an IC50 of 0.044 μM and promotes apoptosis. Additionally, CDK9-Cyclin T1 PPI-IN-1 suppresses CDK9 transcriptional activity and diminishes the phosphorylation of RNA Polymerase II at the CTD serine 2 residue. In vivo studies further demonstrate its capability to inhibit tumor growth in a TNBC 4T1 mouse model.
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