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    RG2833 (RGFP109)
    RG2833 (RGFP109)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0273
    CAS #: 1215493-56-3Purity ≥98%

    Description: RG-2833 (formerly RGFP-109) is a potent, selective and brain-permeable inhibitor of HDAC (histone deacetylase) with potential neuroprotective effects. It inhibits HDAC1 and HDAC3 with IC50s of 60 nM and 50 nM  in cell-free assays, respectively. RG2833 is an investigational drug candidate being studies for the treatment of Parkinson's disease. It has been granted orphan drug status and is being investigated in phase one clinical trials. In iPSC-derived neuronal cell model, plasma RG2833 (5μM) inhibited maximal deacetylase and upregulated FXN. The result showed a good correlation between increase in FXN (Friedreich Ataxia) transcript and inhibition of deacetylase activity, providing evidence that the mechanism of action of RG2833 is through deacetylation. 

    References: PLoS One. 2010 Jan 21;5(1):e8825; Neurobiol Dis. 2011 Jun;42(3):496-505; Parkinsonism Relat Disord. 2013 Feb;19(2):260-4.

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    Molecular Weight (MW)339.43
    CAS No.1215493-56-3
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 68 mg/mL (200.3 mM)
    Water: <1 mg/mL
    Ethanol: 10 mg/mL (29.6 mM)

    RGFP 109; RGFP-109; RGFP109; RG2833; RG 2833; RG-2833

    Chemical Name: N-(6-(2-Aminophenylamino)-6-oxohexyl)-4-methylbenzamide


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    In Vitro

    In vitro activity: RGFP109 dose-dependently upregulates frataxin mRNA and protein levels in cultures of unstimulated peripheral blood mononuclear cells (PBMC) obtained from FRDA patients.

    Kinase Assay:  Aconitase activities are determined by homogenization of mouse brain tissues on ice at 10% w/v in CellLytic MT Mammalian Tissue Lysis/Extraction buffer, followed by centrifugation at 800×g for 10 min at 4°C. Tissue lysates (50 μL) are then added to 200 μL of substrate mix (50 mM Tris/HCl pH 7.4, 0.4 mM NADP, 5 mM Na citrate, 0.6 mM MgCl2, 0.1% (v/v) Triton X-100 and 1U isocitrate dehydrogenase) and the reactions are incubated at 37°C for 15 min, followed by spectrophotometric absorbance measurements every minute for 15 min at 340 nm 37°C to determine the reaction slope. Aconitase activities of mouse brain tissues are then normalized to citrate synthase activities, which are determined using a citrate synthase assay kit.

    Cell Assay:  The Ki values of RG2833 for HDAC1 and HDAC3 are 5.4 nM and 7.8 nM, respectively. RG2833 is highly active in the whole tested concentration range from 1 to 10 µM. Continuous incubation with RG2833 slows the increase in frataxin protein, and when the compound is removed, frataxin protein levels rapidly increased in the cells from patient P13. RG2833 produces significant increases in brain aconitase enzyme activity, together with reduction of neuronal pathology of the dorsal root ganglia (DRG).

    In VivoRG2833 (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.
    Animal modelMice are housed in conventional open cages with Litaspen Premium 8/20 bedding, paper wool nesting and standard fun tunnel environmental enrichment, with 13 h light, 11 h dark, 20-23°C and 45-60% humidity. The mice are given a diet of SDS RM3 Expanded food pellets and standard drinking water. Mice are given subcutaneous injections of 150 mg/kg RG2833 three times per week for 4.5 months, or 50 mg/kg 136 or 100 mg/kg RG2833 five times per week for 5 months, followed by culling for tissue collection 24 h after the final injection.
    Formulation & DosageFormulated in a vehicle solution of 20% glycerol, 20% PEG400, 20% propylene glycol, 5 mM Na acetate pH 5.2.; s.c. administration.

    PLoS One. 2010 Jan 21;5(1):e8825; Neurobiol Dis. 2011 Jun;42(3):496-505; Parkinsonism Relat Disord. 2013 Feb;19(2):260-4.

    These protocols are for reference only. InvivoChem does not independently validate these methods.

    RG2833 (RGFP109)
    Structure and kinetic properties of histone deacetylase inhibitors. Compound 109 is RG2833). PLoS One. 2010 Jan 21;5(1):e8825. 
    RG2833 (RGFP109)
    Effect of compounds 106, 109 and 136 in unstimulated KIKI splenocytes.
    RG2833 (RGFP109)
    Time course for drug exposure, frataxin mRNA expression, and histone acetylation changes in the brain and heart of KIKI mice.
    RG2833 (RGFP109)
    Effect of compounds 136 and 109 on FRDA patients' primary lymphocytes. PLoS One. 2010 Jan 21;5(1):e8825. 
    RG2833 (RGFP109)
    Frataxin expression changes as function of drug 136 dosage. PLoS One. 2010 Jan 21;5(1):e8825. 


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