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CAS No. 1215493-56-3
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.
Selleck's RG2833 (RGFP109) has been cited by 14 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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|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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|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
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|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
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