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.
Cited by 6 Publications
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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) 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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Choose Selective HDAC Inhibitors
|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.|
RGFP109 dose-dependently upregulates frataxin mRNA and protein levels in cultures of unstimulated peripheral blood mononuclear cells (PBMC) obtained from FRDA patients. 
|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.  RGFP109 ameliorates the disease phenotype of a Friedreich ataxia mouse model.  RGFP109 (30 mg/kg p.o.) also alleviates established l-DOPA-induced dyskinesia. |
|In vitro||DMSO||68 mg/mL (200.33 mM)|
|Ethanol||10 mg/mL (29.46 mM)|
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