YKL-5-124 TFA |
| Catalog No.GC39462 |
YKL-5-124 TFA는 CDK7 및 CDK7/Mat1/CycH에 대해 IC50이 각각 53.5nM 및 9.7nM인 강력하고 선택적이며 비가역적이며 공유적인 CDK7 억제제입니다. YKL-5-124 TFA는 CDK9 및 CDK2보다 CDK7에 대해 >100배 더 선택적이고 CDK12 및 CDK13에 대해 비활성입니다. YKL-5-124 TFA는 강력한 세포 주기 정지를 유도하고 E2F 유도 유전자 발현을 억제하며 RNA 중합효소 II 인산화 상태에 거의 영향을 미치지 않습니다.
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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.
Average Rating: 5 (Based on Reviews and 6 reference(s) in Google Scholar.)
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