YKL-5-124 is a selective and irreversible inhibitor of cyclin-dependent kinase 7 (CDK7), demonstrating IC50 values of 53.5 nM and 9.7 nM for CDK7 and the CDK7/Mat1/CycH complex, respectively. This compound exhibits over 100-fold selectivity for CDK7 compared to CDK9 and CDK2 and has negligible activity against CDK12 and CDK13. YKL-5-124 effectively induces cell-cycle arrest, inhibits E2F-driven transcription, and has a limited impact on the phosphorylation status of RNA polymerase II, making it a valuable tool for research in cell cycle regulation and transcriptional control.
YKL-5-124 is a selective and irreversible inhibitor of cyclin-dependent kinase 7 (CDK7), demonstrating IC50 values of 53.5 nM and 9.7 nM for CDK7 and the CDK7/Mat1/CycH complex, respectively. This compound exhibits over 100-fold selectivity for CDK7 compared to CDK9 and CDK2 and has negligible activity against CDK12 and CDK13. YKL-5-124 effectively induces cell-cycle arrest, inhibits E2F-driven transcription, and has a limited impact on the phosphorylation status of RNA polymerase II, making it a valuable tool for research in cell cycle regulation and transcriptional control.
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