YKL-5-124 TFA |
رقم الكتالوجGC39462 |
YKL-5-124 TFA هو مثبط CDK7 قوي وانتقائي ولا رجوع فيه وتساهمي مع IC50s من 53.5 نانومتر و 9.7 نانومتر لـ CDK7 و CDK7 / Mat1 / CycH ، على التواليYKL-5-124 TFA هو أكثر من 100 ضعف انتقائي لـ CDK7 من CDK9 و CDK2 ، وغير نشط ضد CDK12 و CDK13يحث YKL-5-124 TFA على توقيف قوي لدورة الخلية ، ويمنع التعبير الجيني الذي يحركه E2F ، ويظهر تأثيرًا ضئيلًا على حالة فسفرة RNA polymerase 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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