YKL-5-124 TFA |
Catalog No.GC39462 |
YKL-5-124 TFA es un inhibidor de CDK7 potente, selectivo, irreversible y covalente con IC50 de 53,5 nM y 9,7 nM para CDK7 y CDK7/Mat1/CycH, respectivamente. YKL-5-124 TFA es >100 veces mÁs selectivo para CDK7 que para CDK9 y CDK2, e inactivo contra CDK12 y CDK13. YKL-5-124 TFA induce una fuerte detenciÓn del ciclo celular, inhibe la expresiÓn génica impulsada por E2F y muestra poco efecto sobre el estado de fosforilaciÓn de la ARN polimerasa II.
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Cas No.: 2748220-93-9
Sample solution is provided at 25 µL, 10mM.
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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