Molecular Weight(MW): 362.4
RGFP966 is an HDAC3 inhibitor with IC50 of 0.08 μM in cell-free assay, exhibits > 200-fold selectivity over other HDAC.
Cited by 17 Publications
5 Customer Reviews
THP-1 cells were treated with indicated concentrations of Ara-C and/or RGFP966 for 24 h, and lysates were immunoblotted for p-AKT473, AKT and γH2AX.
Leukemia, 2017, 31(12):2761-2770. RGFP966 purchased from Selleck.
(c) Primary mouse keratinocytes were treated for 24 hours with the HDAC3 inhibitor RGFP966 or the control vehicle (DMSO) and analyzed by Western blotting for levels of AQP3 compared with the loading control, GAPDH. Results shown are representative of three separate experiments. Primary mouse keratinocytes grown on cover slips were treated as above. At the end of 24 hours of treatment, cells were fixed and immunostained using an antibody-recognizing AQP3 (red), with nuclei counterstained with DAPI (blue). Scale bar = 20 μm. AQP, aquaporin.
J Invest Dermatol, 2017, 137(9):1935-1944. RGFP966 purchased from Selleck.
Representative images of Fluoro-Jade C staining in each group. The histogram shows the numbers of degenerating neurons in the cortex 24 h (C) or 7 days (D) after MCAO (over 30 slices from five rats per group). ∗∗p < 0.01, ∗∗∗p < 0.001 versus MCAO group, ANOVA. Functional outcomes were assessed using the neurological deficits score (day 1, 4, and 7 after MCAO)
Front Mol Neurosci, 2016, 9:131. RGFP966 purchased from Selleck.
BMDC were stimulated for 7 h with LPS plus SAHA (4 μM), M344 (0.5 μM), TSA (100 nM), PCI-34051 (10 μM), valproate (Val; 5 mM), PD106 (10 μM), MS-275 (5 μM), sirtuin inhibitor (10 μM), RGFP966 (10 μM), MC1568 (10 μM), droxinostat (drox; 10 μM), CAY10603 (500 nM), or sodium butyrate (butyrate) (5 mM). (D) IL-1β concentrations were determined in the supernatants by ELISA.
J Immunol, 2015, 195(11):5421-31. RGFP966 purchased from Selleck.
A, 5×106 HeLa, A549, 293T, and H1299 cells were seeded in 10-cm cell culture dishes on day 0 and treated with dimethyl sulfoxide, 10 μM CI994, or 1 μM RGFP966 for 12 h. Cell lysates were collected for Western blotting analysis of Apaf-1 and β-actin.
J Biol Chem, 2016, 291(14):7386-95.. RGFP966 purchased from Selleck.
Purity & Quality Control
Choose Selective HDAC Inhibitors
|Description||RGFP966 is an HDAC3 inhibitor with IC50 of 0.08 μM in cell-free assay, exhibits > 200-fold selectivity over other HDAC.|
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. 
|In vivo||RGFP966 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. |
Deacetylation assays: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.
|In vitro||DMSO||72 mg/mL (198.67 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.
Frequently Asked Questions
Does this product S7229 specifically inhibit HDAC3? Or does it target other HDACs as well?
In the paper, it is indicated that "RGFP966 is specific for HDAC3, with an IC50 of 0.08 μM and no effective inhibition of any other HDAC at concentrations up to 15 μM. ". However, we did not preform experiment to confirm this data. Please refer to the following link for detailed information: http://www.pnas.org/content/110/7/2647.long