RGFP966

Catalog No.S7229 Batch:S722901

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Technical Data

Formula

C21H19FN4O
Molecular Weight 362.4 CAS No. 1396841-57-8
Solubility (25°C)* In vitro DMSO 72 mg/mL (198.67 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description RGFP966 is an HDAC3 inhibitor with IC50 of 0.08 μM in cell-free assay, exhibits > 200-fold selectivity over other HDAC.
Targets
HDAC3 [1]
(Cell-free assay)
80 nM
In vitro 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. [1] 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. [2]
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. [1]

Protocol (from reference)

Kinase Assay:[1]
  • 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.
Cell Assay:[2]
  • Cell lines

    HH and Hut78 CTCL cell lines

  • Concentrations

    ~10μM

  • Incubation Time

    24 to 72 h

  • Method

    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.
Animal Study:[1]
  • Animal Models

    Mouse

  • Dosages

    10 mg/kg, 10.0 mL/kg

  • Administration

    s.c.

Customer Product Validation

Data from [Data independently produced by , , Leukemia, 2017, 31(12):2761-2770]

Data from [Data independently produced by , , J Invest Dermatol, 2017, 137(9):1935-1944]

Data from [Data independently produced by , , Front Mol Neurosci, 2016, 9:131]

Data from [Data independently produced by , , J Immunol, 2015, 195(11):5421-31]

Selleck's RGFP966 has been cited by 117 publications

HDAC3 integrates TGF-β and microbial cues to program tuft cell biogenesis and diurnal rhythms in mucosal immune surveillance [ Sci Immunol, 2024, 9(99):eadk7387] PubMed: 39331726
Unbiased screening identifies regulators of cell-cell adhesion and treatment options in pemphigus [ Nat Commun, 2024, 15(1):8044] PubMed: 39271654
The lysine methyltransferase SMYD2 facilitates neointimal hyperplasia by regulating the HDAC3-SRF axis [ Acta Pharm Sin B, 2024, 14(2):712-728] PubMed: 38322347
Kaempferol alleviates myocardial ischemia injury by reducing oxidative stress via the HDAC3-mediated Nrf2 signaling pathway [ J Adv Res, 2024, S2090-1232(24)00491-0] PubMed: 39505146
Extracellular CIRP induces abnormal activation of fibroblast-like synoviocytes from patients with RA via the TLR4-mediated HDAC3 pathways [ Int Immunopharmacol, 2024, 128:111525] PubMed: 38218010
LINC01021 Attenuates Expression and Affects Alternative Splicing of a Subset of p53-Regulated Genes [ Cancers (Basel), 2024, 16(9)1639] PubMed: 38730591
Deficiency of histone deacetylases 3 in macrophage alleviates monosodium urate crystals-induced gouty inflammation in mice [ Arthritis Res Ther, 2024, 26(1):96] PubMed: 38711064
LncRNA CHROMR/miR-27b-3p/MET axis promotes the proliferation, invasion, and contributes to rituximab resistance in diffuse large B-cell lymphoma [ J Biol Chem, 2024, 300(3):105762] PubMed: 38367665
Afatinib or Bevacizumab in combination with Osimertinib efficiently control tumor development in orthotopic murine models of non-small lung cancer [ PLoS One, 2024, 19(6):e0304914] PubMed: 38935790
Macrophagic HDAC3 inhibition ameliorates Dextran Sulfate Sodium induced inflammatory bowel disease through GBP5-NLRP3 pathway [ Int J Med Sci, 2024, 21(8):1385-1398] PubMed: 38903915

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.