RG2833 (RGFP109)

Catalog No.S7292

RG2833 (RGFP109) Chemical Structure

Molecular Weight(MW): 339.43

RG2833 (RGFP109) is a brain-penetrant HDAC inhibitor with IC50 of 60 nM and 50 nM for HDAC1 and HDAC3 in cell-free assays, respectively.

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3 Customer Reviews

  • The cells were treated with 1 μM RG2833 (HDAC1/3 inhibitor), 2 μM RGFP966 (HDAC3 inhibitor), 1 μM TSA (pan-HDAC inhibitor), or vehicle for 16 h in serum-free medium. Cell lysates were analysed by Western blotting for expression of SREBP-2 activated fragment, HMG-CoA reductase and APP. Shown are representative blots and quantifications with means ± SEM of the indicated number of independent experiments performed in duplicate. *p < 0.05; **p < 0.01; n.s., not significant in one-sample t-test.

    Sci Rep, 2017, 7:43575. RG2833 (RGFP109) purchased from Selleck.

    a. Cell apoptosis was determined by Annexin V-PI double staining kits and flow cytometry. B. Quantification of the apoptosis, TUNEL staining

    Neurochem Res, 2016, 41(12):3192-3205. RG2833 (RGFP109) purchased from Selleck.

  • (A) refers to the HDAC activity in SK-MEL-5 cells. (B) refers to the HDAC activity in SK-MEL-28 cells. All HDAC activity is relative to a control of 0nM. Numbers above bars indicate statistically independent groups.

    The Winthrop McNair Research Bulletin, 2015, 1:17-22.. RG2833 (RGFP109) purchased from Selleck.

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Biological Activity

Description RG2833 (RGFP109) is a brain-penetrant HDAC inhibitor with IC50 of 60 nM and 50 nM for HDAC1 and HDAC3 in cell-free assays, respectively.
Features Orally bioavailable, HDAC inhibitor that penetrates into brain tissue.
Targets
HDAC3 [1]
(Cell-free assay)
HDAC1 [1]
(Cell-free assay)
5 nM(Ki) 32 nM(Ki)
In vitro

RGFP109 dose-dependently upregulates frataxin mRNA and protein levels in cultures of unstimulated peripheral blood mononuclear cells (PBMC) obtained from FRDA patients. [1]

In vivo RG2833 (150 mg/kg) corrects frataxin deficiency and increases histone acetylation in the brain and heart of KIKI mice without acute toxicity signs. [1] RGFP109 ameliorates the disease phenotype of a Friedreich ataxia mouse model. [2] RGFP109 (30 mg/kg p.o.) also alleviates established l-DOPA-induced dyskinesia. [3]

Protocol

Animal Research:

[1]

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  • Animal Models: KIKI mice
  • Formulation: --
  • Dosages: ~150 mg/kg
  • Administration: Subcutaneous injection
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 68 mg/mL (200.33 mM)
Ethanol 10 mg/mL (29.46 mM)
Water 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.

Chemical Information

Molecular Weight 339.43
Formula

C20H25N3O2

CAS No. 1215493-56-3
Storage powder
Synonyms N/A

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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.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID