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    RGFP966
    RGFP966

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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 #: V0272
    CAS #: 1357389-11-7Purity ≥98%

    Description: RGFP966 (RGF-P966) is a novel, potent and highly selective inhibitor of HDAC3 (histone deacetylase 3) with potential anticancer activity. It inhibits HDAC3 with an IC50 of 80 nM in cell-free assay, exhibits > 200-fold selectivity for HDAC3 over other HDACs.

    References: Proc Natl Acad Sci U S A. 2013 Feb 12;110(7):2647-52; PLoS One. 2013 Jul 22;8(7):e68915.

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    Molecular Weight (MW)362.4
    FormulaC21H19FN4O
    CAS No.1357389-11-7
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 72 mg/mL (198.7 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)1% DMSO+30% polyethylene glycol+1% Tween 80: 30 mg/mL
    Other info

    Synonym: RGFP966; RGFP-966; RGFP 966

    Chemical Name: (E)-N-(2-amino-4-fluorophenyl)-3-(1-cinnamyl-1H-pyrazol-4-yl)acrylamide

    InChi Key: BLVQHYHDYFTPDV-VCABWLAWSA-N

    InChi Code: InChI=1S/C21H19FN4O/c22-18-9-10-20(19(23)13-18)25-21(27)11-8-17-14-24-26(15-17)12-4-7-16-5-2-1-3-6-16/h1-11,13-15H,12,23H2,(H,25,27)/b7-4+,11-8+

    SMILES Code: O=C(NC1=CC=C(F)C=C1N)/C=C/C2=CN(C/C=C/C3=CC=CC=C3)N=C2


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    In Vitro

    In vitro activity: RGFP966 is a slow-on/slow-off, competitive tight-binding HDAC inhibitor, with an IC50 of 0.08μM for HDAC3 and no effective inhibition of any other HDAC at concentrations up to 15μM. RGFP966 treatment on two CTCL cell lines for 24 hours prior to western blot analysis resulted in increased acetylation at H3K9/K14, H3K27, and H4K5, but not H3K56ac. RGFP966 decreases cell growth in CTCL (cutaneous T cell lymphoma) cell lines due to increased apoptosis that is associated with DNA damage and impaired S phase progression. RGFP966 causes a significant reduction in DNA replication fork velocity within the first hour of drug treatment.


    Kinase Assay: Deacetylation assays are based on the homogenous fluorescence release assay. Purified recombinant enzymes are incubated with serial-diluted inhibitors at the concentrations indicated in the figures, with pre-incubation times ranging from 0 to 3 hours, in the standard HDAC buffer. Acetyl-Lys(Ac)-AMC substrate (at 10 μM, corresponding to the Km for both HDAC1 and HDAC3) is added after the pre-incubation period. The reaction is allowed to run for 1 hour. The trypsin peptidase developer, at final concentration of 5mg/ml, is added after 1 hour, and the fluorescence emission is then measured using a Tecan M200 96-well plate reader.


    Cell Assay: Cells are counted and split into T25 (Corning) flasks at 26105 cells/mL. Cells are then treated with DMSO, or HDIs once at hour 0. 100 ml aliquots are taken in triplicate from each flask at 0 hr, 24 hrs, 48 hrs, and 72 hrs after treatment, distributed into a flat bottom 96-well plate, and 10 ml of alamar blue added to each well. After a 4 hr incubation, fluorescence is measured using the Biotek Synergy MX Microplate Reader.

    In VivoRGFP966 treatment (10 mg/kg) enhances long-term memory for object memory. RGFP966 (3 or 10 mg/kg, s.c.) facilitates extinction and prevents reinstatement of cocaine- conditioned place preference.
    Animal modelMouse
    Formulation & DosageFormulated in in DMSO and diluted in a vehicle of 30% (wt/vol) hydroxypropyl-β-cyclodextrin and 100mM sodium acetate (pH 5.4); 10 mg/kg; s.c. administration.
    References

    Proc Natl Acad Sci U S A. 2013 Feb 12;110(7):2647-52; PLoS One. 2013 Jul 22;8(7):e68915.


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

     

    RGFP966

    HDAC3 inhibition enhances the rate and persistence of extinction of cocaine-CPP. Proc Natl Acad Sci U S A. 2013 Feb 12;110(7):2647-52.
     

    RGFP966

    HDAC3 inhibition simultaneously reduces drug-seeking behavior and enhances memory. Proc Natl Acad Sci U S A. 2013 Feb 12;110(7):2647-52. 
     
    RGFP966
    HDAC3 inhibition promotes histone acetylation and gene expression during extinction consolidation. Proc Natl Acad Sci U S A. 2013 Feb 12;110(7):2647-52. 


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