1. Cell Cycle/DNA Damage
    Epigenetics
  2. HDAC
  3. RGFP966

RGFP966 

Cat. No.: HY-13909 Purity: 98.99%
Handling Instructions

RGFP966 is a highly selective HDAC3 inhibitor with an IC50 of 80 nM and shows no inhibition to other HDACs at concentrations up to 15 μM.

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

RGFP966 Chemical Structure

RGFP966 Chemical Structure

CAS No. : 1357389-11-7

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 119 In-stock
Estimated Time of Arrival: December 31
5 mg USD 108 In-stock
Estimated Time of Arrival: December 31
10 mg USD 168 In-stock
Estimated Time of Arrival: December 31
50 mg USD 420 In-stock
Estimated Time of Arrival: December 31
100 mg USD 734 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 9 publication(s) in Google Scholar

Top Publications Citing Use of Products

    RGFP966 purchased from MCE. Usage Cited in: Pancreatology. 2019 Mar;19(2):383-389.

    RGFP966 decreases PD-L1 expression in a time- and dose-dependent manner in pancreatic cancer cells.

    RGFP966 purchased from MCE. Usage Cited in: Front Physiol. 2019; 10: 1060.

    Osteoarthritis rats are treated with RGFP966. Immunohistochemistry (IHC) was performed to measure relative inflammatory proteins in OA. Expression of collagen II in CG and OAG + RGFP966 group is higher than OAG by IHC.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    RGFP966 is a highly selective HDAC3 inhibitor with an IC50 of 80 nM and shows no inhibition to other HDACs at concentrations up to 15 μM.

    IC50 & Target[1]

    HDAC3

    80 nM (IC50)

    In Vitro

    RGFP966 potently and selectively inhibits HDAC 3 with IC50 of 0.21 μM in RAW 264.7 macrophages, while HDACs 1 (IC50=5.6 μM), 2 (9.7 μM) and 8 (>100 μM), indicating a good level of selectivity for HDAC 3. The mRNA levels of HDACs 1, 2 and 3 are not significantly affected by RGFP966 in RAW 264.7 macrophages, whereas the HDAC 1 and HDAC 2 protein levels are slightly, though significantly, reduced upon RGFP966 treatment. Moreover, RGFP966 significantly reduced the transcriptional activity of NF-κB p65, whereas NF-κB p65 acetylation and localization remain unaltered[2].

    In Vivo

    RGFP966 (10 and 25 mg/kg) treatment significantly improves body weight, rotarod performance and several measures of motor function in the open field locomoter test[3]. RGFP966 at a 10 mg/kg dose penetrates the blood-brain barrier into rat auditory cortex with typical pharmacokinetics, which together establish feasibility for the modulation of A1 plasticity due to action in the auditory cortex[4].

    Molecular Weight

    362.40

    Formula

    C₂₁H₁₉FN₄O

    CAS No.

    1357389-11-7

    SMILES

    O=C(NC1=CC=C(F)C=C1N)/C=C/C2=CN(C/C=C/C3=CC=CC=C3)N=C2.[E]

    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 : 50 mg/mL (137.97 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.7594 mL 13.7969 mL 27.5938 mL
    5 mM 0.5519 mL 2.7594 mL 5.5188 mL
    10 mM 0.2759 mL 1.3797 mL 2.7594 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: ≥ 2.5 mg/mL (6.90 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (6.90 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Kinase Assay
    [2]

    The respective human recombinant HDAC enzymes are incubated in absence and/or in presence of various concentrations RGFP966 and a pro-fluorogenic substrate at room temperature for 60 min. Next, the deacetylation reaction is stopped by the addition of the HDAC Stop Solution (6 mg/mL trypsin, 0.3 mM SAHA) in all wells and the plate is incubated at 37°C for 20 min. The release of the fluorescent 7-amino-4-methylcoumarin is monitored by measuring the fluorescence at λem=460 nm and λex=390 nm using a Synergy H1 plate reader. The fluorescence value of the background wells is subtracted from the fluorescence of the positive control, blank and inhibitor wells. Nonlinear regression is used to fit the data to the log(inhibitor) vs. response curve using GraphPad Prism[2].

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

    Cell Assay
    [2]

    To investigate the influence of the HDAC 3-selective inhibitor RGFP966 on cell viability, RAW 264.7 macrophages, HBE cells and hASM cells are seeded in 96-well plates. To obtain identical cell density at the start of the experiments, RAW 264.7 macrophages are seeded at 25,000 cells/cm2, HBE cells and hASM cells are seeded at 70% confluency (based on surface area) and are serum-starved for 24 h prior incubation with RGFP966. Shortly before incubation with RGFP966, the medium is replaced by 100 μL fresh (if appropriate serum free) culture medium. Incubations with LPS and IFNγ are performed as described for HDAC 1-3 downregulation by siRNA. After 20 h of incubation with RGFP966, 20 μL of CellTiter 96 AQueous One Solution reagent is added to each well and incubated at 37°C for 1 h in the dark. The absorbance at 490 nm is measured using a Synergy H1 plate reader. LPS/IFNγ-stimulated cells without addition of RGFP966 are considered 100%[2].

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

    Animal Administration
    [3][4]

    Mice[3]
    N171-82Q transgenic mice are housed and maintained on a normal 12-h light/dark cycle with lights on at 6:00 a.m and free access to food and water. Mice are administered RGFP966 (10 or 25 mg/kg) for 10 weeks by S.C. injection (3 injections/week) beginning at 8 weeks of age. RGFP966 is dissolved with 75% polyethylene glycol 200/25% sodium acetate (6.25 mM); control mice received an equal volume of drug vehicle. Body weights are recorded twice per week. Mice are sacrificed at 18 weeks of age, 6 h after the final injection by overdose with isofluorane anesthesia. Brains are removed, and striata and cortex dissected out for gene expression assays or intracardially perfused with 4% paraformaldehyde.
    Rats[4]
    A total of thirty-three adult male Sprague Dawley rats (275-350 g) are used. Immediately following the daily training session, a posttraining systemic injection of either RGPF966 (10 mg/kg, s.c.) or vehicle (at a comparable volume to drug treatment) is delivered to each subject.

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

    References
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.
    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product name

     

    Salutation

    Applicant name *

     

    Email address *

    Phone number *

     

    Organization name *

    Country or Region *

     

    Requested quantity *

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    RGFP966
    Cat. No.:
    HY-13909
    Quantity: