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

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. RGFP966 can penetrate the blood brain barrier (BBB).

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

RGFP966 Chemical Structure

RGFP966 Chemical Structure

CAS No. : 1357389-11-7

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO USD 99 In-stock
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5 mg USD 90 In-stock
10 mg USD 140 In-stock
50 mg USD 380 In-stock
100 mg USD 620 In-stock
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Customer Review

Based on 32 publication(s) in Google Scholar

Other Forms of RGFP966:

Top Publications Citing Use of Products

30 Publications Citing Use of MCE RGFP966

WB
IHC

    RGFP966 purchased from MedChemExpress. Usage Cited in: Front Physiol. 2019 Aug 20;10:1060.  [Abstract]

    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.

    RGFP966 purchased from MedChemExpress. Usage Cited in: Pancreatology. 2019 Mar;19(2):383-389.  [Abstract]

    RGFP966 decreases PD-L1 expression in a time- and dose-dependent manner in pancreatic cancer cells.
    • 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. RGFP966 can penetrate the blood brain barrier (BBB).

    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].

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

    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].

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

    Molecular Weight

    362.40

    Formula

    C21H19FN4O

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

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

    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: 

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

    DMSO : 50 mg/mL (137.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 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

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

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

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  50% PEG300    50% Saline

      Solubility: 7.69 mg/mL (21.22 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.81%

    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

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMF / DMSO 1 mM 2.7594 mL 13.7969 mL 27.5938 mL 68.9845 mL
    5 mM 0.5519 mL 2.7594 mL 5.5188 mL 13.7969 mL
    10 mM 0.2759 mL 1.3797 mL 2.7594 mL 6.8985 mL
    15 mM 0.1840 mL 0.9198 mL 1.8396 mL 4.5990 mL
    20 mM 0.1380 mL 0.6898 mL 1.3797 mL 3.4492 mL
    25 mM 0.1104 mL 0.5519 mL 1.1038 mL 2.7594 mL
    30 mM 0.0920 mL 0.4599 mL 0.9198 mL 2.2995 mL
    40 mM 0.0690 mL 0.3449 mL 0.6898 mL 1.7246 mL
    50 mM 0.0552 mL 0.2759 mL 0.5519 mL 1.3797 mL
    60 mM 0.0460 mL 0.2299 mL 0.4599 mL 1.1497 mL
    80 mM 0.0345 mL 0.1725 mL 0.3449 mL 0.8623 mL
    100 mM 0.0276 mL 0.1380 mL 0.2759 mL 0.6898 mL
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    • 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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