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

TPOP146 

Cat. No.: HY-100697 Purity: 99.66%
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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10 mM * 1 mL in DMSO USD 111 In-stock
Estimated Time of Arrival: December 31
5 mg USD 105 In-stock
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10 mg USD 180 In-stock
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50 mg USD 480 In-stock
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100 mg USD 800 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products

Publications Citing Use of MCE TPOP146

    TPOP146 purchased from MCE. Usage Cited in: EMBO Rep. 2020 Mar 4;21(3):e48328.

    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)
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    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

    Formula

    C₂₇H₃₅N₃O₅

    CAS No.

    2018300-62-2

    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 : ≥ 100 mg/mL (207.65 mM)

    *"≥" means soluble, but saturation unknown.

    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: ≥ 2.5 mg/mL (5.19 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (5.19 mM); Clear solution

    • 3.

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

      Solubility: ≥ 2.5 mg/mL (5.19 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    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

    Purity: 99.66%

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    Keywords:

    TPOP146TPOP 146TPOP-146Epigenetic Reader DomainHistone AcetyltransferaseHATsHATInhibitorinhibitorinhibit

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    Product Name:
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    Cat. No.:
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