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

TPOP146 

Cat. No.: HY-100697 Purity: 98.98%
COA Handling Instructions

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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Solution
10 mM * 1 mL in DMSO USD 111 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 111 In-stock
Solid
5 mg USD 105 In-stock
10 mg USD 180 In-stock
50 mg USD 480 In-stock
100 mg USD 800 In-stock
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Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products

    TPOP146 purchased from MCE. 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

    IC50: 134 nM (CBP); 5.02 μM (BRD4)[1]
    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].

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

    481.58

    Appearance

    Solid

    Formula

    C27H35N3O5
    CAS No.
    SMILES

    COC1=CC(OC)=CC(C2=CC(C(N[[email protected]]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 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 21.43 mg/mL (44.50 mM; ultrasonic and warming and heat to 60°C)

    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
    10 mM 0.2076 mL 1.0382 mL 2.0765 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 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

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

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

    *All of the co-solvents are available by MCE.
    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
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    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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    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass   Concentration   Volume   Molecular Weight *
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    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:

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

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