YKL-5-124
- CAS No.
- 1957203-01-8
- Chemical Name:
- YKL-5-124
- Synonyms
- YKL-5-124;(S)-3-(4-Acrylamidobenzamido)-N-(2-(dimethylamino)-1-phenylethyl)-6,6-dimethyl-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide;Pyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-[(1S)-2-(dimethylamino)-1-phenylethyl]-4,6-dihydro-6,6-dimethyl-3-[[4-[(1-oxo-2-propen-1-yl)amino]benzoyl]amino]-;T-loop,phosphorylation,inhibit,arrest,CDK7,Inhibitor,CDK,YKL5124,YKL 5 124,CDK7/Mat1/CycH,Cyclin dependent kinase,cell-cycle,transcription,Pol-II,irreversible,covalent
- CBNumber:
- CB85867444
- Molecular Formula:
- C28H33N7O3
- Molecular Weight:
- 515.61
- MDL Number:
- MFCD34469131
- MOL File:
- 1957203-01-8.mol
YKL-5-124 Chemical Properties,Uses,Production
Biological Activity
YKL-5-124 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 is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status[1]. YKL-5-124 (0-2000 nM; 72 hours; HAP1 cells) treatment causes a dose-dependent increase in G1- and G2/M-phase cells and a corresponding loss of S-phase cells[1].YKL-5-124 (0-2000 nM; 24 hours; HAP1 WT cells) treatment inhibits CDK1 T-loop phosphorylation, and to a lesser extent CDK2 T-loop phosphorylation in a concentration-dependent fashion[1].Treatment of cells with YKL-5-124 as a competitor at a concentration of about 30 nM blocks pull-down of CDK7-cyclin H but has no effect on the pull-down of cyclin K-CDK12/13 in HAP1 cells. Treatment with 100 nM YKL-5-124 reduces CDK7-cyclin H binding to bioTHZ1 by >50% at 30 min[1].
storage
Store at -20°C
References
[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.
YKL-5-124 Preparation Products And Raw materials
Raw materials
Preparation Products
YKL-5-124 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6313 | 58 |
| Nantong HI-FUTURE Biology Co., Ltd. | +undefined18051384581 | sales@chemhifuture.com | China | 3136 | 58 |
| Wuhan Topule Biopharmaceutical Co., Ltd | +8618327326525 | masar@topule.com | China | 8474 | 58 |
| Aladdin Scientific | +1-833-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
| ShangHai Biochempartner Co.,Ltd | 17754423994 17754423994 | 2853530910@QQ.com | China | 8011 | 62 |
| DC Chemicals | 021-58447131 13564518121 | sales@dcchemicals.com | China | 9414 | 58 |
| Nantong Hi-Future Biotechnology Co., Ltd | 18051384581 | sales@chemhifuture.com | China | 2996 | 58 |
| SINO High Goal Chemical Technology Co., Ltd. | 021-57646680 18306277365 | guoxin@chembiobanksh.com | China | 2319 | 58 |
| Wuhan Augda Biotechnology Co., Ltd | 15071299552 | 262933239@qq.com | China | 6637 | 58 |