RG2833 (RGFP109)

Catalog No.S7292

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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RG2833 (RGFP109) Chemical Structure

RG2833 (RGFP109) Chemical Structure
Molecular Weight: 339.43

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Quality Control & MSDS

Product Information

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Product Description

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.
Targets HDAC3 [1]
(Cell-free assay)
HDAC1 [1]
(Cell-free assay)
HDAC3 [1]
(Cell-free assay)
HDAC1 [1]
(Cell-free assay)
IC50 5 nM(Ki) 32 nM(Ki) 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]
Features Orally bioavailable, HDAC inhibitor that penetrates into brain tissue.

Protocol(Only for Reference)

Kinase Assay: [1]

Time dependent IC50 value with pre-incubation Deacetylation assays are based on the homogenous fluorescence release assay. In brief, purified recombinant enzymes are incubated with serial-diluted inhibitors at various concentrations, with pre-incubation times ranging from 0 to 3 hours, in the standard HDAC buffer. Acetyl-Lys(Ac)-AMC substrate (at 10 μM, corresponding to the Km for both HDAC1 and HDAC3) is added after the pre-incubation period. The reaction is allowed to run for 1 hour. The trypsin peptidase developer, at final concentration of 5mg/ml, is added after 1 hour, and the fluorescence emission is then measured using a Tecan M200 96-well plate reader.

Animal Study: [1]

Animal Models KIKI mice
Dosages ~150 mg/kg
Administration Subcutaneous injection

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[1] Rai M, et al. PLoS One. 2010, 5(1), e8825.

[2] Sandi C, et al. Neurobiol Dis. 2011, 42(3), 496-505.

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Chemical Information

Download RG2833 (RGFP109) SDF
Molecular Weight (MW) 339.43


CAS No. 1215493-56-3
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 68 mg/mL (200.33 mM)
Ethanol 10 mg/mL (29.46 mM)
Water <1 mg/mL (<1 mM)
* <1 mg/ml means slightly soluble or 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 Name N-(6-(2-aminophenylamino)-6-oxohexyl)-4-methylbenzamide

Tech Support

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.

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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