YKL-5-124
- Product Name
- 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
- Formula Weight
- 515.61
- MOL File
- 1957203-01-8.mol
YKL-5-124 Property
- 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)
- pka
- 12.78±0.40(Predicted)
N-Bromosuccinimide Price
- Product number
- SML3039
- Product name
- YKL-5-124
- Purity
- ≥98% (HPLC)
- Packaging
- 5MG
- Price
- $113
- Updated
- 2024/03/01
- Product number
- SML3039
- Product name
- YKL-5-124
- Purity
- ≥98% (HPLC)
- Packaging
- 25MG
- Price
- $568
- Updated
- 2024/03/01
YKL-5-124 Chemical Properties,Usage,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
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