2. Epigenetics
  3. Epigenetic Reader Domain Histone Acetyltransferase
  4. TPOP146

TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor with Kd values of 134 nM and 5.02 μM for CBP and BRD4.

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

TPOP146 Chemical Structure

TPOP146 Chemical Structure

CAS No. : 2018300-62-2

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Solid + Solvent
10 mM * 1 mL in DMSO
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Customer Review

Based on 4 publication(s) in Google Scholar

TPOP146 Related Antibodies

Top Publications Citing Use of Products

    TPOP146 purchased from MedChemExpress. Usage Cited in: EMBO Rep. 2020 Mar 4;21(3):e48328.  [Abstract]

    Inhibiting acetyltransferases CBP/P300 by TPOP146 (134 nM) or PCAF by L-45 (126 nM) for 24 h did not significantly decrease the K49-acetylated b-cat level in Tau-overexpressing N2a cells (n = 3 biological replicates each group)

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor with Kd values of 134 nM and 5.02 μM for CBP and BRD4.

    IC50 & Target

    CBP/p300

     

    In Vitro

    Exposure to 1 μM TPOP146 results in a significant decrease of recovery half-life that is comparable to the construct that contained the bromodomain inactivating mutation N1168F, demonstrating that TPOP146 targets the CBP bromodomain in the nucleus and is capable of competing with acetyl-lysine mediated interactions of the CBP bromodomain in cellular environments[1].

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

    TPOP146 Related Antibodies
    Molecular Weight

    481.58

    Formula

    C27H35N3O5
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    COC1=CC(OC)=CC(C2=CC(C(N[C@H]3CCCN(C)C3)=O)=C(OCCN(C(CC)=O)C4)C4=C2)=C1
    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 : 21.43 mg/mL (44.50 mM; ultrasonic and warming and heat to 60°C; 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 2.0765 mL 10.3825 mL 20.7650 mL
    5 mM 0.4153 mL 2.0765 mL 4.1530 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
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    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    40% PEG300    5% Tween-80    45% Saline

      Solubility: 2.14 mg/mL (4.44 mM); Clear solution; Need ultrasonic

      This protocol yields a clear solution of 2.14 mg/mL.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.4 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: 2.14 mg/mL (4.44 mM); Clear solution; Need ultrasonic

      This protocol yields a clear solution of 2.14 mg/mL.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.4 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

    Purity: 98.98%

    COA (255 KB) LCMS (268 KB)

    Handling Instructions (2659 KB)
    References
    Kinase Assay
    [1]

    Proteins are buffered in 10 mM HEPES, pH 7.5, 500 mM NaCl and assayed in a 96-well plate at a final concentration of 2 μM in 20 μL volume. Compounds (TPOP146) are added at a final concentration of 10 μM. SYPRO Orange (Molecular Probes) is added as a fluorescence probe at a dilution of 1:1000. Excitation and emission filters for the SYPRO Orange dye are set to 465 and 590 nm, respectively. The temperature is raised with a step of 3°C per minute from 25 to 96°C, and fluorescence readings are taken at each interval[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 2.0765 mL 10.3825 mL 20.7650 mL 51.9125 mL
    5 mM 0.4153 mL 2.0765 mL 4.1530 mL 10.3825 mL
    10 mM 0.2076 mL 1.0382 mL 2.0765 mL 5.1912 mL
    15 mM 0.1384 mL 0.6922 mL 1.3843 mL 3.4608 mL
    20 mM 0.1038 mL 0.5191 mL 1.0382 mL 2.5956 mL
    25 mM 0.0831 mL 0.4153 mL 0.8306 mL 2.0765 mL
    30 mM 0.0692 mL 0.3461 mL 0.6922 mL 1.7304 mL
    40 mM 0.0519 mL 0.2596 mL 0.5191 mL 1.2978 mL
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    TPOP146 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:

    TPOP1462018300-62-2TPOP 146TPOP-146Epigenetic Reader DomainHistone AcetyltransferaseHATsHATInhibitorinhibitorinhibit

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