1. Cell Cycle/DNA Damage
  2. CDK
  3. YKL-5-124

YKL-5-124 

Cat. No.: HY-101257
Handling Instructions

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.

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YKL-5-124 Chemical Structure

YKL-5-124 Chemical Structure

CAS No. : 1957203-01-8

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Description

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].

IC50 & Target[1]

CDK7

53.5 nM (IC50)

CDK7/Mat1/CycH

9.7 nM (IC50)

CDK2

1300 nM (IC50)

CDK9

3020 nM (IC50)

In Vitro

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].

Cell Cycle Analysis[1]

Cell Line: HAP1 cells
Concentration: 0 nM, 0.2 nM, 0.7 nM, 2 nM, 6.3 nM, 20 nM, 60 nM, 200 nM, 633.3 nM, 2000 nM
Incubation Time: 72 hours
Result: Caused a dose-dependent increase in G1- and G2/M-phase cells and a corresponding loss of S-phase cells.

Western Blot Analysis[1]

Cell Line: HAP1 cells
Concentration: 0 nM, 125 nM, 250 nM, 500 nM, 1000 nM, 2000 nM
Incubation Time: 24 hours
Result: Inhibited CDK1 T-loop phosphorylation, and to a lesser extent CDK2 T-loop phosphorylation in a concentration-dependent fashion.
Molecular Weight

515.61

Formula

C₂₈H₃₃N₇O₃

CAS No.

1957203-01-8

SMILES

CC1(C)N(C(N[[email protected]@H](C2=CC=CC=C2)CN(C)C)=O)CC3=C1NN=C3NC(C4=CC=C(NC(C=C)=O)C=C4)=O

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

YKL-5-124CDKCyclin dependent kinaseCDK7CDK7/Mat1/CycHtranscriptioncovalentcell-cyclearrestPol-IIphosphorylationT-loopirreversibleInhibitorinhibitorinhibit

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YKL-5-124
Cat. No.:
HY-101257
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