2. Epigenetics
  3. Histone Acetyltransferase Epigenetic Reader Domain
  4. GNE-272

GNE-272 est un inhibiteur CBP / EP300 puissant et sélectif avec des valeurs IC50 de 0,02, 0,03 et 13 μM pour CBP, EP300 et BRD4, respectivement. GNE-272 est également une sonde sélective in vivo pour CBP/EP300.

GNE-272 is a potent and selective CBP/EP300 inhibitor with IC50 values of 0.02, 0.03 and 13 μM for CBP, EP300 and BRD4, respectively. GNE-272 is also a selective in vivo probe for CBP/EP300.

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

GNE-272 Chemical Structure

GNE-272 Chemical Structure

CAS No. : 1936428-93-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 213 In-stock
Solution
10 mM * 1 mL in DMSO USD 213 In-stock
Solid
2 mg USD 132 In-stock
5 mg USD 228 In-stock
10 mg USD 360 In-stock
50 mg USD 1140 In-stock
100 mg USD 1800 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 3 publication(s) in Google Scholar

GNE-272 Related Antibodies

Top Publications Citing Use of Products

    GNE-272 purchased from MedChemExpress. Usage Cited in: J Transl Med. 2023 Mar 17;21(1):201.  [Abstract]

    GNE-272 downregulates the expression of SNAI2 both in BxPC-3 and PANC1.

    View All Histone Acetyltransferase Isoform Specific Products:

    View All Isoforms
    CBP/p300 GCN5/PCAF TIP60 MOZ/MORF HBO1

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    GNE-272 is a potent and selective CBP/EP300 inhibitor with IC50 values of 0.02, 0.03 and 13 μM for CBP, EP300 and BRD4, respectively. GNE-272 is also a selective in vivo probe for CBP/EP300[1].

    IC50 & Target

    CBP/p300

     

    In Vitro

    GNE-272 is exquisitely selective for CBP/ EP300 and remarkably selective (650-fold) over BRD4. When tested at 10 μM in 35 kinase panel and 42 receptors off-target screening panel, GNE-272 does not inhibit any target at >30%. In addition, GNE-272 does not inhibit (>10 μM, top concentration) several cytochrome P450s (3A4, 1A2, 2C9, 2C19, 2D6). The compound has good potency in the BRET cellular assay. In an orthogonal measure of the target engagement, GNE-272 is shown to inhibit the expression of MYC10 (MV4?11 cell line) with an EC50 of 0.91 μM and good correlation between the BRET and MYC cellular assays is observed[1].

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

    GNE-272 Related Antibodies
    In Vivo

    GNE-272 demonstrates low clearance following a 1 mg/ kg intravenous dose in a mouse PK experiment and good oral bioavailability when dosed at 100 mg/kg, reaching an unbound Cmax of 26 μM. GNE-272 shows a marked antiproliferative effect in hematologic cancer cell lines and modulates MYC expression in vivo that corresponds with antitumor activity in an AML tumor model[1].

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

    424.47

    Formula

    C22H25FN6O2
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CC(N1CCC2=C(C(NC3=C(F)C=C(C4=CN(C)N=C4)C=C3)=NN2[C@@H]5COCC5)C1)=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 : 100 mg/mL (235.59 mM; Need ultrasonic; 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 2.3559 mL 11.7794 mL 23.5588 mL
    5 mM 0.4712 mL 2.3559 mL 4.7118 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: ≥ 2.5 mg/mL (5.89 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 (5.89 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
    Cell Assay
    [1]

    Human cancer cell lines (MOLM-16, HL-60, LP-1, KMS-34, Pfeiffer, DOHH-2) are treated for 4 h with 5 μM GNE-272 or DMSO control. After 6 days, cell viability is measured by CellTiter-Glo[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Mice: Mice are given 0 (vehicle, 0.5% methylcellulose; 0.2% Tween-80), 12.5, 25, and 50 mg/kg of GNE-272 by gavage, twice daily (BID) for 21 days in a volume of 100 μL. Tumor volumes are measured in two dimensions (length and width) using Ultra CalIV calipers and analyzed using Excel, version 11.2[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 2.3559 mL 11.7794 mL 23.5588 mL 58.8970 mL
    5 mM 0.4712 mL 2.3559 mL 4.7118 mL 11.7794 mL
    10 mM 0.2356 mL 1.1779 mL 2.3559 mL 5.8897 mL
    15 mM 0.1571 mL 0.7853 mL 1.5706 mL 3.9265 mL
    20 mM 0.1178 mL 0.5890 mL 1.1779 mL 2.9448 mL
    25 mM 0.0942 mL 0.4712 mL 0.9424 mL 2.3559 mL
    30 mM 0.0785 mL 0.3926 mL 0.7853 mL 1.9632 mL
    40 mM 0.0589 mL 0.2945 mL 0.5890 mL 1.4724 mL
    50 mM 0.0471 mL 0.2356 mL 0.4712 mL 1.1779 mL
    60 mM 0.0393 mL 0.1963 mL 0.3926 mL 0.9816 mL
    80 mM 0.0294 mL 0.1472 mL 0.2945 mL 0.7362 mL
    100 mM 0.0236 mL 0.1178 mL 0.2356 mL 0.5890 mL
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    GNE-272 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:

    GNE-2721936428-93-1GNE272GNE 272Histone AcetyltransferaseEpigenetic Reader DomainHATsHATInhibitorinhibitorinhibit

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