1. Epigenetics Autophagy Apoptosis
  2. Histone Acetyltransferase Autophagy Epigenetic Reader Domain Apoptosis
  3. C646

C646 is a selective and competitive histone acetyltransferase p300 inhibitor with Ki of 400 nM, and is less potent for other acetyltransferases.

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

C646 Chemical Structure

C646 Chemical Structure

CAS No. : 328968-36-1

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Solid + Solvent
10 mM * 1 mL in DMSO
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USD 143 In-stock
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10 mM * 1 mL in DMSO USD 143 In-stock
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5 mg USD 83 In-stock
10 mg USD 130 In-stock
20 mg USD 225 In-stock
50 mg USD 502 In-stock
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Customer Review

Based on 57 publication(s) in Google Scholar

Top Publications Citing Use of Products

52 Publications Citing Use of MCE C646

WB

    C646 purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2023 Mar 11;210:115497.  [Abstract]

    C646 (20 μM) decreases the expression of PLK1 following effective inhibition of H3K27ac, and αSMA and COLI are also repressed, in TGFβ-activated LX2 cells.

    C646 purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2018 Nov;25(11):1980-1995.  [Abstract]

    Western blot analysis of LAMC2 expression after C646 treatment in KYSE150 and KYSE450. C646 treatment: 20μM, 12h.

    C646 purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2018 Aug 20;124:454-465.  [Abstract]

    To explore whether P300 is required for NaB’s activation of Nrf2 expression and function, HG-treated endothelial cells (ECs) are co-treated with NaB, in the presence or absence of C646.

    C646 purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2017 Oct 5;812:206-215.  [Abstract]

    C646 inhibits the proliferation of Cervical cancer cells and induced the accumulation of p53 protein. Protein levels of p53 and p21 are augmented by C646 in a dose-dependent manner. Whole cell lysates are analyzed with western-blot analysis.

    C646 purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2016 Dec 2;481(1-2):90-96.  [Abstract]

    DMKG inhibits autophagy of HSCs via acetyl-coenzyme A and EP300. Western blot analysis of LC3B, Beclin-1, a-SMA, and collagen-I expression from lysates of HSC-T6 incubated with control media, DMKG (4 mM), or Lipoic acid (5 mM) in the presence or absence of C646 (10 mM) for 12 h.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    C646 is a selective and competitive histone acetyltransferase p300 inhibitor with Ki of 400 nM, and is less potent for other acetyltransferases[1].

    IC50 & Target

    CBP/p300

     

    In Vitro

    C646 is a linear competitive inhibitor of p300 versus acetyl-CoA with a Ki?of 400 nM. C646 shows a noncompetitive pattern of p300 inhibition versus the H4-15 peptide substrate. C646 treatment reduces histone H3 and H4 acetylation levels and abrogates TSA-induced acetylation in cells. C646 has a more potent effect on cell growth than Lys-CoA-Tat does[1].
    C646 enhances mitotic catastrophe after IR and suppresses phosphorylation of CHK1 after IRin A549 cells[2]. C646 attenuates the increased acetylation of GATA1 and the increased transcriptional activity of GATA1 induced by EDAG[3].

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

    In Vivo

    Suppression of P300 by c646 (intraperitoneally injected, 30 nmol/g/d for 2 weeks) dramatically reduces the level of blood glucose in db/db mice[4].

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

    Animal Model: Fourteen-week-old male db/db mice and normal m/m mice[4]
    Dosage: 30 nmol/g
    Administration: Intraperitoneally injected; daily; 2 weeks
    Result: The db/db mice showed greater body masses and higher levels of fasting blood glucose than the m/m mice.
    Molecular Weight

    445.42

    Formula

    C24H19N3O6

    CAS No.
    Appearance

    Solid

    Color

    Brown to reddish brown

    SMILES

    O=C(O)C1=CC=C(N2N=C(C)/C(C2=O)=C\C3=CC=C(C4=CC(C)=C(C)C=C4[N+]([O-])=O)O3)C=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 : 13.89 mg/mL (31.18 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 2.2451 mL 11.2254 mL 22.4507 mL
    5 mM 0.4490 mL 2.2451 mL 4.4901 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)

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    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: 1.67 mg/mL (3.75 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 1.67 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 (16.7 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: 1.67 mg/mL (3.75 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 1.67 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 (16.7 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

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    (per animal)

    g

    Dosing volume
    (per animal)

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    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

    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 2.2451 mL 11.2254 mL 22.4507 mL 56.1268 mL
    5 mM 0.4490 mL 2.2451 mL 4.4901 mL 11.2254 mL
    10 mM 0.2245 mL 1.1225 mL 2.2451 mL 5.6127 mL
    15 mM 0.1497 mL 0.7484 mL 1.4967 mL 3.7418 mL
    20 mM 0.1123 mL 0.5613 mL 1.1225 mL 2.8063 mL
    25 mM 0.0898 mL 0.4490 mL 0.8980 mL 2.2451 mL
    30 mM 0.0748 mL 0.3742 mL 0.7484 mL 1.8709 mL
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    • 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:
    C646
    Cat. No.:
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