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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.
Product Catalog 2023
Guide to Product Handling
RGFP 109; RGFP-109; RGFP109; RG2833; RG 2833; RG-2833
Chemical Name: N-(6-(2-Aminophenylamino)-6-oxohexyl)-4-methylbenzamide
SMILES Code: O=C(NCCCCCC(NC1=CC=CC=C1N)=O)C2=CC=C(C)C=C2
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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).
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.
Lot#: V027301,Purity ≥98%
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MSDS
NMR
Lot#: V027302,Purity ≥98%
Lot#: V027303,Purity ≥98%