YKL-5-124 TFA |
| Katalog-Nr.GC39462 |
YKL-5-124 TFA ist ein potenter, selektiver, irreversibler und kovalenter CDK7-Inhibitor mit IC50-Werten von 53,5 nM und 9,7 nM fÜr CDK7 bzw. CDK7/Mat1/CycH. YKL-5-124 TFA ist >100-mal selektiver fÜr CDK7 als CDK9 und CDK2 und inaktiv gegen CDK12 und CDK13. YKL-5-124 TFA induziert einen starken Zellzyklusarrest, hemmt die E2F-gesteuerte Genexpression und zeigt nur geringe Wirkung auf den Phosphorylierungsstatus der RNA-Polymerase II.
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Cas No.: 2748220-93-9
Sample solution is provided at 25 µL, 10mM.
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YKL-5-124 TFA is a potent, selective, irreversible and covalent CDK7 inhibitor with IC50s of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH, respectively. YKL-5-124 TFA is >100-fold greater selectivity for CDK7 than CDK9 and CDK2 and inactive against CDK12 and CDK13. YKL-5-124 TFA induces a strong cell-cycle arrest, and inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status[1].
[1]. Olson CM, et al. Development of a Selective CDK7 Covalent Inhibitor Reveals Predominant Cell-Cycle Phenotype. Cell Chem Biol. 2019 Jun 20;26(6):792-803.e10.
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