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

YKL-5-124 TFA 

Cat. No.: HY-101257B Purity: 99.44%
COA 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

CAS No. : 2748220-93-9

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 353 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 353 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 255 In-stock
Estimated Time of Arrival: December 31
10 mg USD 435 In-stock
Estimated Time of Arrival: December 31
25 mg USD 870 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1390 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2220 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of YKL-5-124 TFA:

Top Publications Citing Use of Products

    YKL-5-124 TFA purchased from MCE. 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

    • 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].

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

    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

    Appearance

    Solid

    Formula

    C30H34F3N7O5
    CAS No.
    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

    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)

    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
    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:  PBS

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

    • 2.

      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

    • 3.

      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

    • 4.

      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 available by MCE.
    Purity & Documentation

    Purity: 99.44%

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

    Handling Instructions (2659 KB)
    References
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.
    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.

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Keywords:

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

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Salutation

    Applicant Name *

    		 

    Email address *

    Phone number *

    		 

    Organization name *

    Department *

    		 

    Requested quantity *

    Country or Region *

    		      

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    YKL-5-124 TFA
    Cat. No.:
    HY-101257B
    Quantity:
    MCE Japan Authorized Agent:

    Customer Review

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Lot #

    Applicant Name *

    		 

    Email address *

    Phone number

    		 

    Department *

    Organization name *

    		 

    Country or Region *

    Remarks

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.