Basic information Safety Supplier Related

YKL-5-124

Basic information Safety Supplier Related

YKL-5-124 Basic information

Product Name:
YKL-5-124
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]-
  • (S)-3-(4-Acrylamidobenzamido)-N-(2-(dimethylamino)-1-phenylethyl)-6,6-dimethyl-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide
  • 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
CAS:
1957203-01-8
MF:
C28H33N7O3
MW:
515.61
Mol File:
1957203-01-8.mol
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YKL-5-124 Chemical Properties

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)
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YKL-5-124 Usage And Synthesis

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-5-124Supplier

ShangHai Biochempartner Co.,Ltd
Tel
17754423994 17754423994
Email
2853530910@QQ.com
TargetMol Chemicals Inc.
Tel
+1-781-999-5354 +1-00000000000
Email
marketing@targetmol.com
HANGZHOU CLAP TECHNOLOGY CO.,LTD
Tel
86-571-88216897,88216896 13588875226
Email
sales@hzclap.com
DC Chemicals
Tel
021-58447131 13564518121
Email
sales@dcchemicals.com
Nantong Hi-Future Biotechnology Co., Ltd
Tel
18051384581
Email
sales@chemhifuture.com
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