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

C646 

Cat. No.: HY-13823 Purity: 98.32%
COA Handling Instructions

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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Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 143 In-stock
Solution
10 mM * 1 mL in DMSO USD 143 In-stock
Solid
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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200 mg   Get quote  

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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 wine

    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)

    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
    10 mM 0.2245 mL 1.1225 mL 2.2451 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: 1.67 mg/mL (3.75 mM); Suspended solution; Need ultrasonic

    • 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

    *All of the co-solvents are available by MedChemExpress (MCE).
    Purity & Documentation
    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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    Product Name:
    C646
    Cat. No.:
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