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    C646
    C646

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V2519
    CAS #: 328968-36-1Purity ≥98%

    Description: C646 is a potent, selective and competitive inhibitor for histone acetyltransferase p300. It inhibits p300 with a Ki of 400 nM in a cell-free assay. It is less potent for other acetyltransferases and preferentially selective for p300. C646 induces cell cycle arrest and apoptosis selectively in AML1-ETO-positive AML cells. C646 reverses epithelial to mesenchymal transition of human peritoneal mesothelial cells via blocking TGF-β1/Smad3 signaling pathway in vitro. 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. 

    References: Mol Cancer Ther. 2011 Sep;10(9):1644-55; J Neurosci. 2011 May 18;31(20):7486-91.

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    Molecular Weight (MW)445.42
    FormulaC24H19N3O6
    CAS No.328968-36-1
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 13 mg/mL (29.2 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)5% DMSO+30% PEG 300+ddH2O: 1 mg/mL
    SynonymsC646; C-646; C 646


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    In Vitro

    In vitro activity: C646 is an inhibitor for histone acetyltransferase, inhibits p300 with a Ki of 400 nM and is selective versus other acetyltransferases. C646 produces 86% inhibition of p300 in vitro at 10 μM. C646 is a classical reversible p300 inhibitor. C646 treatment (25μM) reduces histone H3 and H4 acetylation levels and abrogates TSA-induced acetylation in cells. C646 (20μM) induces apoptosis in androgen-sensitive and castration-resistant prostate cancer cell lines by interfering with AR and NF-kB pathways. C646 blocks dynamic acetylation of H3K4me3 globally in mouse and fly cells, and locally across the promoter and start-site of inducible genes in the mouse, thereby disrupting RNA polymerase II association and the activation of these genes


    Kinase Assay: IC50 values for the putative p300 HAT inhibitors are determined using the direct radioactive assay described above. Reactions are performed in 20 mM HEPES (pH 7.9), and contained 5 mM DTT, 80μM EDTA, 40μg/ml BSA, 100μM H4-15, and 5 nM p300. Putative inhibitors are added over a range of concentrations, with DMSO concentration kept constant (<5%). Reactions are incubated at 30°C for 10 min, then initiated with addition of a 1:1 mixture of 12C-acetyl-CoA and 14C-acetyl-CoA to 20 mM. After 10 min at 30°C, reactions are quenched with 14% SDS (w/v). All concentrations are screened in duplicate. Gels are run, washed, dried, and exposed to a PhosphorImager plate, and production of Ac-H4-15 quantified to obtain IC50s.


    Cell Assay: Histone acetylation assays in mouse cells. C3H10T1/2 mouse fibroblasts are grown in DMEM with 10% FCS at 37°C with 6% CO2. Confluent cultures are rendered quiescent in DMEM with 0.5% FCS for 18-20 hr prior to treatment. Cells are treated with the following compounds: TSA (10 ng/ml [33 nM]), C646 (25 μM), C37 (25 μM). Antibodies are used at the following concentrations: total H3 (1:10000; ab7834; Abcam); H4K12ac (1:2500; 06-761; Upstate). Rabbit anti-H3K9ac (1:10000) antibodies are generated in-house. Histones are isolated from cells by acid extraction, separated by SDS and acid-urea polyacrylamide gel electrophoresis and analyzed by western blotting.

    In VivoC646 infused into the ILPFC immediately after weak extinction training enhances the consolidation of fear extinction memory. C646 attenuates mechanical allodynia and thermal hyperalgesia, accompanied by a suppressed COX-2 expression, in the spinal cord.
    Animal modelMouse model
    Formulation & DosageDissolved in 10% DMSO; 2×0.75 μl injection volume in each case, 1.5 μg, administered over 2 min;  infusion into ILPFC
    References

    Mol Cancer Ther. 2011 Sep;10(9):1644-55; J Neurosci. 2011 May 18;31(20):7486-91.  


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    C646

    Inhibition of p300 enhances LTP in the infralimbic PFC. J Neurosci. 2011 May 18; 31(20): 7486–7491.

    C646

    Inhibition of p300 in the ILPFC enhances fear extinction memory. J Neurosci. 2011 May 18; 31(20): 7486–7491.


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