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

C646 

Cat. No.: HY-13823 Purity: >98.0%
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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10 mM * 1 mL in DMSO USD 130 In-stock
Estimated Time of Arrival: December 31
10 mg USD 118 In-stock
Estimated Time of Arrival: December 31
50 mg USD 456 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 16 publication(s) in Google Scholar

Top Publications Citing Use of Products

    C646 purchased from MCE. Usage Cited in: Eur J Pharmacol. 2017 Oct 5;812:206-215.

    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 MCE. Usage Cited in: Biochem Biophys Res Commun. 2016 Dec 2;481(1-2):90-96.

    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.

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

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

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

    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.
    • Biological Activity

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    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

    Ki: 400 nM (histone acetyltransferase 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 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].

    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].

    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.

    328968-36-1

    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 : 16.67 mg/mL (37.43 mM; Need ultrasonic)

    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.
    References
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    Keywords:

    C646C 646C-646Histone AcetyltransferaseAutophagyEpigenetic Reader DomainApoptosisHATsHATInhibitorinhibitorinhibit

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    Product Name:
    C646
    Cat. No.:
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