2. Cell Cycle/DNA Damage Apoptosis
  3. CDK Apoptosis
  4. LDC000067

LDC000067 is a highly specific CDK9 inhibitor with an IC50 value of 44±10 nM in vitro.

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

LDC000067 Chemical Structure

LDC000067 Chemical Structure

CAS No. : 1073485-20-7

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10 mM * 1 mL in DMSO
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Customer Review

Based on 10 publication(s) in Google Scholar

LDC000067 Related Antibodies

Top Publications Citing Use of Products

    LDC000067 purchased from MedChemExpress. Usage Cited in: Biochim Biophys Acta. 2017 Nov 20;1865(2):354-363.  [Abstract]

    LAPC-4 cells are grown in charcoal-stripped serum medium (CSS) for 24 hours and then stimulated by R1881 alone or with different doses of LDC000067. LDC000067 is added 30 min before androgen treatment. Cellular expression of all proteins was detected by immunoblotting analysis. β-actin was included as a control for protein loading.

    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

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    LDC000067 is a highly specific CDK9 inhibitor with an IC50 value of 44±10 nM in vitro.

    IC50 & Target[1]

    CDK9- Cyclin T1

    44 nM (IC50)

    cdk2-cyclin A

    2441 nM (IC50)

    cdk1-cyclin B1

    5513 nM (IC50)

    cdk4-cyclin D1

    9242 nM (IC50)

    GSK3A

    1460 nM (IC50)

    HGK/MAP4K4

    820 nM (IC50)

    ABL2/ARG

    3640 nM (IC50)

    In Vitro

    The selectivity of LDC000067 for CDK9 over other CDKs exceeds that of the known inhibitors flavopiridol and DRB. LDC000067 displayed 55/125/210/ >227/ >227-fold selectivity for CDK9 versus CDK2/1/4/6/7. LDC000067 inhibits in vitro transcription in an ATP-competitive and dose-dependent manner. Gene expression profiling of cells treated with LDC000067 demonstrates a selective reduction of short-lived mRNAs, including important regulators of proliferation and apoptosis[1].

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

    LDC000067 Related Antibodies
    Molecular Weight

    370.43

    Formula

    C18H18N4O3S
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=S(CC1=CC=CC(NC2=NC=NC(C3=CC=CC=C3OC)=C2)=C1)(N)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 47 mg/mL (126.88 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.6996 mL 13.4978 mL 26.9957 mL
    5 mM 0.5399 mL 2.6996 mL 5.3991 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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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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    Volume (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 (6.75 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 (6.75 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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    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
    References
    Kinase Assay
    [1]

    The fluorescence resonance energy transfer (FRET)-based LANCE Ultra KinaSelect Ser/Thr kit is used to determine IC50 values for various CDK inhibitors. Briefly, a specific ULight MBP peptide substrate (50 nM final concentration) is phosphorylated by a CDK-cyclin pair in buffer (50 mM HEPES-KOH pH 7.5, 10 mM MgCl2, 1 mM EGTA, 2 mM dithiothreitol) containing ATP at the concentration of the Km values of the individual kinases for 1 h at room temperature. Subsequently, phosphorylation is detected by addition of specific Eu-labelled anti-phospho-antibodies (2 nM), which upon binding to the phosphopeptide give rise to a FRET signal. FRET signals are then recorded[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.6996 mL 13.4978 mL 26.9957 mL 67.4891 mL
    5 mM 0.5399 mL 2.6996 mL 5.3991 mL 13.4978 mL
    10 mM 0.2700 mL 1.3498 mL 2.6996 mL 6.7489 mL
    15 mM 0.1800 mL 0.8999 mL 1.7997 mL 4.4993 mL
    20 mM 0.1350 mL 0.6749 mL 1.3498 mL 3.3745 mL
    25 mM 0.1080 mL 0.5399 mL 1.0798 mL 2.6996 mL
    30 mM 0.0900 mL 0.4499 mL 0.8999 mL 2.2496 mL
    40 mM 0.0675 mL 0.3374 mL 0.6749 mL 1.6872 mL
    50 mM 0.0540 mL 0.2700 mL 0.5399 mL 1.3498 mL
    60 mM 0.0450 mL 0.2250 mL 0.4499 mL 1.1248 mL
    80 mM 0.0337 mL 0.1687 mL 0.3374 mL 0.8436 mL
    100 mM 0.0270 mL 0.1350 mL 0.2700 mL 0.6749 mL
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    LDC000067 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:

    LDC0000671073485-20-7LDC067LDC 000067LDC-000067LDC 067LDC-067CDKApoptosisCyclin dependent kinaseInhibitorinhibitorinhibit

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