RG2833

Brain-penetrant HDAC inhibitor CAS# 1215493-56-3

RG2833

Catalog No. BCC1893----Order now to get a substantial discount!

Product Name & Size Price Stock
RG2833:5mg $49.00 In stock
RG2833:10mg $83.00 In stock
RG2833:25mg $196.00 In stock
RG2833:50mg $343.00 In stock
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Quality Control of RG2833

Quality Control & MSDS

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Chemical structure

RG2833

3D structure

Chemical Properties of RG2833

Cas No. 1215493-56-3 SDF Download SDF
PubChem ID 56654642 Appearance Powder
Formula C20H25N3O2 M.Wt 339.43
Type of Compound N/A Storage Desiccate at -20°C
Synonyms RGFP109
Solubility DMSO : ≥ 50 mg/mL (147.31 mM)
H2O : < 0.1 mg/mL (insoluble)
*"≥" means soluble, but saturation unknown.
Chemical Name N-[6-(2-aminoanilino)-6-oxohexyl]-4-methylbenzamide
SMILES CC1=CC=C(C=C1)C(=O)NCCCCCC(=O)NC2=CC=CC=C2N
Standard InChIKey VOPDXHFYDJAYNS-UHFFFAOYSA-N
Standard InChI InChI=1S/C20H25N3O2/c1-15-10-12-16(13-11-15)20(25)22-14-6-2-3-9-19(24)23-18-8-5-4-7-17(18)21/h4-5,7-8,10-13H,2-3,6,9,14,21H2,1H3,(H,22,25)(H,23,24)
General tips For 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.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of RG2833

DescriptionRG2833 is a brain-penetrant inhibitor of HDAC with IC50 values of 60 nM and 50 nM for HDAC1 and HDAC3, respectively.
TargetsHDAC1HDAC3    
IC5060 nM50 nM    

Protocol

Kinase Assay [2]
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.

Animal Administration [2]
Mice 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.

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. [2]. Sandi C, et al. Prolonged treatment with pimelic o-aminobenzamide HDAC inhibitors ameliorates the disease phenotype of a Friedreich ataxia mouse model. Neurobiol Dis. 2011, 42(3), 496-505. [3]. Johnston TH, et al. RGFP109, a histone deacetylase inhibitor attenuates L-DOPA-induced dyskinesia in the MPTP-lesioned marmoset: a proof-of-concept study. Parkinsonism Relat Disord. 2013, 19(2), 260-264.

RG2833 Dilution Calculator

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Preparing Stock Solutions of RG2833

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.9461 mL 14.7306 mL 29.4612 mL 58.9223 mL 73.6529 mL
5 mM 0.5892 mL 2.9461 mL 5.8922 mL 11.7845 mL 14.7306 mL
10 mM 0.2946 mL 1.4731 mL 2.9461 mL 5.8922 mL 7.3653 mL
50 mM 0.0589 mL 0.2946 mL 0.5892 mL 1.1784 mL 1.4731 mL
100 mM 0.0295 mL 0.1473 mL 0.2946 mL 0.5892 mL 0.7365 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on RG2833

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.

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References on RG2833

Epigenetic therapy for Friedreich ataxia.[Pubmed:25159818]

Ann Neurol. 2014 Oct;76(4):489-508.

OBJECTIVE: To investigate whether a histone deacetylase inhibitor (HDACi) would be effective in an in vitro model for the neurodegenerative disease Friedreich ataxia (FRDA) and to evaluate safety and surrogate markers of efficacy in a phase I clinical trial in patients. METHODS: We used a human FRDA neuronal cell model, derived from patient induced pluripotent stem cells, to determine the efficacy of a 2-aminobenzamide HDACi (109) as a modulator of FXN gene expression and chromatin histone modifications. FRDA patients were dosed in 4 cohorts, ranging from 30mg/day to 240mg/day of the formulated drug product of HDACi 109, RG2833. Patients were monitored for adverse effects as well as for increases in FXN mRNA, frataxin protein, and chromatin modification in blood cells. RESULTS: In the neuronal cell model, HDACi 109/RG2833 increases FXN mRNA levels and frataxin protein, with concomitant changes in the epigenetic state of the gene. Chromatin signatures indicate that histone H3 lysine 9 is a key residue for gene silencing through methylation and reactivation through acetylation, mediated by the HDACi. Drug treatment in FRDA patients demonstrated increased FXN mRNA and H3 lysine 9 acetylation in peripheral blood mononuclear cells. No safety issues were encountered. INTERPRETATION: Drug exposure inducing epigenetic changes in neurons in vitro is comparable to the exposure required in patients to see epigenetic changes in circulating lymphoid cells and increases in gene expression. These findings provide a proof of concept for the development of an epigenetic therapy for this fatal neurological disease.

Description

RG2833 is a brain-penetrant HDAC inhibitor with IC50s of 60 nM and 50 nM for HDAC1 and HDAC3, respectively. The Ki values for HDAC1 and HDAC3 are 32 and 5 nM, respectively.

Keywords:

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