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

YKL-5-124 TFA 

Cat. No.: HY-101257B
Handling Instructions

YKL-5-124 TFA 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 TFA is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 TFA induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status.

For research use only. We do not sell to patients.

YKL-5-124 TFA Chemical Structure

YKL-5-124 TFA Chemical Structure

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 353 In-stock
Estimated Time of Arrival: December 31
5 mg USD 255 In-stock
Estimated Time of Arrival: December 31
10 mg USD 435 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

YKL-5-124 TFA 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 TFA is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 TFA 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 WT 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

629.63

Formula

C₃₀H₃₄F₃N₇O₅

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.FC(F)(C(O)=O)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (158.82 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5882 mL 7.9412 mL 15.8823 mL
5 mM 0.3176 mL 1.5882 mL 3.1765 mL
10 mM 0.1588 mL 0.7941 mL 1.5882 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (3.97 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (3.97 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (3.97 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

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

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YKL-5-124 TFA
Cat. No.:
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