YKL-5-124 TFA

YKL-5-124 TFA is a potent, selective, irreversible and covalent CDK7 inhibitor with IC 50 s of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH , respectively. YKL-5-124 TFA is >100-fold greater selective for CDK7 than CDK9 and CDK2 , and inactive against CDK12 and CDK13 . YKL-5-124 TFA induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status In Vitro YKL-5-124 (0-2000 nM; 72 hours; HAP1 cells) treatment causes a dose-dependent increase in G1- and G2/M-phase cells and a corresponding loss of S-phase cells. YKL-5-124 (0-2000 nM; 24 hours; HAP1 WT cells) treatment inhibits CDK1 T-loop phosphorylation, and to a lesser extent CDK2 T-loop phosphorylation in a concentration-dependent fashion. Treatment of cells with YKL-5-124 as a competitor at a concentration of about 30 nM blocks pull-down of CDK7-cyclin H but has no effect on the pull-down of cyclin K-CDK12/13 in HAP1 cells. Treatment with 100 nM YKL-5-124 reduces CDK7-cyclin H binding to bioTHZ1 by >50% at 30 min. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Cycle AnalysisCell Line: HAP1 cells Concentration: 0 nM, 0.2 nM, 0.7 nM, 2 nM, 6.3 nM, 20 nM, 60 nM, 200 nM, 633.3 nM, 2000 nM Incubation Time: 72 hours Result: Caused a dose-dependent increase in G1- and G2/M-phase cells and a corresponding loss of S-phase cells. Western Blot AnalysisCell Line: HAP1 WT cells Concentration: 0 nM, 125 nM, 250 nM, 500 nM, 1000 nM, 2000 nM Incubation Time: 24 hours Result: Inhibited CDK1 T-loop phosphorylation, and to a lesser extent CDK2 T-loop phosphorylation in a concentration-dependent fashion. Form:Solid IC50& Target:CDK7 53.5 nM (IC 50 ) CDK7/Mat1/CycH 9.7 nM (IC 50 ) CDK2 1300 nM (IC 50 ) CDK9 3020 nM (IC 50 )

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