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

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.

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YKL-5-124 TFA Chemical Structure

YKL-5-124 TFA Chemical Structure

CAS No. : 2748220-93-9

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 353 In-stock
Solution
10 mM * 1 mL in DMSO USD 353 In-stock
Solid
5 mg USD 255 In-stock
10 mg USD 435 In-stock
25 mg USD 870 In-stock
50 mg USD 1390 In-stock
100 mg USD 2220 In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of YKL-5-124 TFA:

YKL-5-124 TFA Related Antibodies

Top Publications Citing Use of Products

    YKL-5-124 TFA purchased from MedChemExpress. Usage Cited in: J Cancer Res Clin Oncol. 2022 Nov 18.  [Abstract]

    OSMI-4 (20 µM; 4 days) and YKL-5-124 (1, 5, 10, 50, 400 nM; 4 days) demonstrate highly signifcant combinatorial toxicity on three CRPC models.

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    YKL-5-124 TFA Related Antibodies

    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
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CC1(C)N(C(N[C@@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

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (158.82 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 50 mg/mL (79.41 mM; Need ultrasonic)

    *"≥" 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 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

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 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

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  PBS

      Solubility: 50 mg/mL (79.41 mM); Clear solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

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    Dosing volume
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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.44%

    COA (254 KB) HNMR (418 KB) LCMS (129 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 1.5882 mL 7.9412 mL 15.8823 mL 39.7059 mL
    5 mM 0.3176 mL 1.5882 mL 3.1765 mL 7.9412 mL
    10 mM 0.1588 mL 0.7941 mL 1.5882 mL 3.9706 mL
    15 mM 0.1059 mL 0.5294 mL 1.0588 mL 2.6471 mL
    20 mM 0.0794 mL 0.3971 mL 0.7941 mL 1.9853 mL
    25 mM 0.0635 mL 0.3176 mL 0.6353 mL 1.5882 mL
    30 mM 0.0529 mL 0.2647 mL 0.5294 mL 1.3235 mL
    40 mM 0.0397 mL 0.1985 mL 0.3971 mL 0.9926 mL
    50 mM 0.0318 mL 0.1588 mL 0.3176 mL 0.7941 mL
    60 mM 0.0265 mL 0.1324 mL 0.2647 mL 0.6618 mL
    DMSO 80 mM 0.0199 mL 0.0993 mL 0.1985 mL 0.4963 mL
    100 mM 0.0159 mL 0.0794 mL 0.1588 mL 0.3971 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    YKL-5-124 TFA Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    YKL-5-1242748220-93-9CDKCyclin dependent kinaseCDK7CDK7/Mat1/CycHtranscriptioncovalentcell-cyclearrestPol-IIphosphorylationT-loopirreversibleInhibitorinhibitorinhibit

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