YKL-5-124 TFA |
| カタログ番号GC39462 |
YKL-5-124 TFA は、CDK7 および CDK7/Mat1/CycH に対してそれぞれ 53.5 nM および 9.7 nM の IC50 を持つ、強力で選択的、不可逆的かつ共有結合的な CDK7 阻害剤です。 YKL-5-124 TFA は、CDK9 および CDK2 よりも CDK7 に対して 100 倍以上選択的であり、CDK12 および CDK13 に対しては不活性です。 YKL-5-124 TFA は強力な細胞周期停止を誘導し、E2F 駆動型遺伝子発現を阻害し、RNA ポリメラーゼ II リン酸化状態にほとんど影響を与えません。
Products are for research use only. Not for human use. We do not sell to patients.
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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