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

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

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 289 In-stock
Solution
10 mM * 1 mL in DMSO USD 289 In-stock
Solid
1 mg USD 121 In-stock
5 mg USD 255 In-stock
10 mg USD 435 In-stock
25 mg USD 696 In-stock
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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of YKL-5-124:

YKL-5-124 Related Antibodies

Top Publications Citing Use of Products

    YKL-5-124 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.

    View All CDK Isoform Specific Products:

    View All Isoforms
    CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    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].

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

    YKL-5-124 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 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.
    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
    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 (193.95 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9395 mL 9.6973 mL 19.3945 mL
    5 mM 0.3879 mL 1.9395 mL 3.8789 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • 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

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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: ≥ 2.08 mg/mL (4.03 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: 2.08 mg/mL (4.03 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
    In Vivo Dissolution Calculator
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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    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).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 98.79%

    SDS (393 KB)

    COA (251 KB) HNMR (479 KB) LCMS (99 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. 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
    DMSO 1 mM 1.9395 mL 9.6973 mL 19.3945 mL 48.4863 mL
    5 mM 0.3879 mL 1.9395 mL 3.8789 mL 9.6973 mL
    10 mM 0.1939 mL 0.9697 mL 1.9395 mL 4.8486 mL
    15 mM 0.1293 mL 0.6465 mL 1.2930 mL 3.2324 mL
    20 mM 0.0970 mL 0.4849 mL 0.9697 mL 2.4243 mL
    25 mM 0.0776 mL 0.3879 mL 0.7758 mL 1.9395 mL
    30 mM 0.0646 mL 0.3232 mL 0.6465 mL 1.6162 mL
    40 mM 0.0485 mL 0.2424 mL 0.4849 mL 1.2122 mL
    50 mM 0.0388 mL 0.1939 mL 0.3879 mL 0.9697 mL
    60 mM 0.0323 mL 0.1616 mL 0.3232 mL 0.8081 mL
    80 mM 0.0242 mL 0.1212 mL 0.2424 mL 0.6061 mL
    100 mM 0.0194 mL 0.0970 mL 0.1939 mL 0.4849 mL
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    YKL-5-124 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-5-1241957203-01-8CDKCyclin dependent kinaseCDK7CDK7/Mat1/CycHtranscriptioncovalentcell-cyclearrestPol-IIphosphorylationT-loopirreversibleInhibitorinhibitorinhibit

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