1. Apoptosis
  2. DAPK
  3. TC-DAPK 6

TC-DAPK 6 is a potent, ATP-competitive, and highly selective DAPK inhibitor (IC50=69 and 225 nM against DAPK1 and DAPK3, respectively, with 10 μM ATP).

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

TC-DAPK 6 Chemical Structure

TC-DAPK 6 Chemical Structure

CAS No. : 315694-89-4

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 45 In-stock
Solution
10 mM * 1 mL in DMSO USD 45 In-stock
Solid
5 mg USD 40 In-stock
10 mg USD 65 In-stock
25 mg USD 120 In-stock
50 mg USD 170 In-stock
100 mg USD 250 In-stock
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Customer Review

Based on 10 publication(s) in Google Scholar

Top Publications Citing Use of Products

    TC-DAPK 6 purchased from MedChemExpress. Usage Cited in: Sci Rep. 2018 Jul 2;8(1):9930.  [Abstract]

    The effects of DAPK1 inhibitor (10 μM) treatment on the expression of p-MLC, caspase-1, NLRP3, pro-IL-1β and ASC in LPS-primed cells are determined by western blotting analysis.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    TC-DAPK 6 is a potent, ATP-competitive, and highly selective DAPK inhibitor (IC50=69 and 225 nM against DAPK1 and DAPK3, respectively, with 10 μM ATP).

    IC50 & Target

    IC50: 69 nM (DAPK1), 225 nM (DAPK3)[1]

    In Vitro

    TC-DAPK 6 is found to be the most potent Death-associated protein kinase (DAPK) inhibitor with enzyme selectivity. When assayed with 10 μM ATP, the IC50 values for DAPK1 and DAPK3 are 69 and 225 nM, respectively. TC-DAPK 6 also inhibits p70S6K (1 μM < IC50< 10 μM)[1].

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

    Molecular Weight

    276.29

    Formula

    C17H12N2O2

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C(OC(/C=C/C1=CC=CC=C1)=N/2)C2=C/C3=CC=CN=C3

    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 : 18.67 mg/mL (67.57 mM; Need ultrasonic and warming; 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 3.6194 mL 18.0969 mL 36.1939 mL
    5 mM 0.7239 mL 3.6194 mL 7.2388 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)

    Mass
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    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    C2

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    Volume (final)

    V2

    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    90% (20% SBE-β-CD in Saline)

      Solubility: 2 mg/mL (7.24 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2 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 (20.0 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]

    Kinase assay is performed using the Z’-LYTE kinase assay kit Ser/Thr 13 peptide. The standard reaction for compound screening contained 1 mM peptide substrate, 10 mM ATP, 50 mM HEPES (pH 7.4), 10 mM MgCl2, 0.01% Brij-35, and 0.5% DMSO. Human recombinant DAPK1 is used at a final concentration of 2.6 μg/mL, and recombinant DAPK3 is used at a final concentration 1.5 mg/mL. To test the enzyme selectively of the inhibitors (e.g., TC-DAPK 6), ProfilerPro kits are used in the protocol[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, 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 3.6194 mL 18.0969 mL 36.1939 mL 90.4846 mL
    5 mM 0.7239 mL 3.6194 mL 7.2388 mL 18.0969 mL
    10 mM 0.3619 mL 1.8097 mL 3.6194 mL 9.0485 mL
    15 mM 0.2413 mL 1.2065 mL 2.4129 mL 6.0323 mL
    20 mM 0.1810 mL 0.9048 mL 1.8097 mL 4.5242 mL
    25 mM 0.1448 mL 0.7239 mL 1.4478 mL 3.6194 mL
    30 mM 0.1206 mL 0.6032 mL 1.2065 mL 3.0162 mL
    40 mM 0.0905 mL 0.4524 mL 0.9048 mL 2.2621 mL
    50 mM 0.0724 mL 0.3619 mL 0.7239 mL 1.8097 mL
    60 mM 0.0603 mL 0.3016 mL 0.6032 mL 1.5081 mL
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    TC-DAPK 6 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.

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    Product Name:
    TC-DAPK 6
    Cat. No.:
    HY-15513
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