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RG2833

In stock
Catalog No.
A3761
Brain-penetrant HDAC inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$50.00
In stock
5mg
$50.00
In stock
10mg
$70.00
In stock
25mg
$130.00
In stock
50mg
$190.00
In stock

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Email: [email protected]

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Background

RG2833 is a histone deacetylase (HDAC) inhibitor.
In the neuronal cell, RG2833 increased Friedreich Ataxia (FXN) mRNA and protein levels, with concomitant changes in the epigenetic state of the gene. In PBMCs, RG2833 inhibited HDAC expression and increased H3K9 acetylation, and increased FXN mRNA in blood from patients.
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 transcript and inhibition of deacetylase activity, providing evidence that the mechanism of action of RG2833 is through deacetylation. [1]
Reference:
1.Soragni E, Miao W, Iudicello M et al. Epigenetic therapy for Friedreich ataxia. Ann Neurol. 2014 Oct;76(4):489-508.

Chemical Properties

StorageStore at -20°C
M.Wt339.43
Cas No.1215493-56-3
FormulaC20H25N3O2
SynonymsRG 2833;RG-2833;RGFP-109;RGFP109;RGFP 109
Solubility≥16.95 mg/mL in DMSO, ≥8.05 mg/mL in EtOH with ultrasonic and warming, <2.38 mg/mL in H2O
Chemical NameN-[6-(2-aminoanilino)-6-oxohexyl]-4-methylbenzamide
SDFDownload SDF
Canonical SMILESCC1=CC=C(C=C1)C(=O)NCCCCCC(=O)NC2=CC=CC=C2N
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Protocol

Cell experiment [1]:

Cell lines

Unstimulated peripheral blood mononuclear cells (PBMC) from FRDA Patients.

Preparation method

The solubility of this compound in DMSO is >17mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

1, 2.5, 5 or 10 μM for 48 hours

Applications

RG2833 dose-dependently upregulates frataxin mRNA and protein levels in cultures of unstimulated peripheral blood mononuclear cells (PBMC) from FRDA patients.

Animal experiment [2]:

Animal models

GAA knock-in mice

Dosage form

150 mg/kg, subcutaneous injection

Application

RG2833 corrected frataxin deficiency and increases histone acetylation in the brain and heart of KIKI mice (a GAA repeat based FRDA mouse model) without acute toxicity signs.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Rai M, et al. Two new pimelic diphenylamide HDAC inhibitors induce sustained frataxin upregulation in cells from Friedreich's ataxia patients and in a mouse model. PLoS One. 2010, 5(1), e8825.

Biological Activity

Description RG2833 is a brain-penetrant inhibitor of HDAC with IC50 values of 60 nM and 50 nM for HDAC1 and HDAC3, respectively.
Targets HDAC1 HDAC3        
IC50 60 nM 50 nM        

Quality Control

Chemical structure

RG2833