| Identification | Back Directory | [Name]
YKL-5-124 | [CAS]
1957203-01-8 | [Synonyms]
YKL-5-124
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]- | [Molecular Formula]
C28H33N7O3 | [MDL Number]
MFCD34469131 | [MOL File]
1957203-01-8.mol | [Molecular Weight]
515.61 |
| Chemical Properties | Back Directory | [Boiling point ]
706.1±60.0 °C(Predicted) | [density ]
1.284±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 250 mg/mL (484.86 mM; Need ultrasonic) | [form ]
Solid | [pka]
12.78±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [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. |
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| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
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