RG2833Brain-penetrant HDAC inhibitor CAS# 1215493-56-3 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| 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. |
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| 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. |
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| 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. | ||
| 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 | ||||
RG2833 Dilution Calculator
RG2833 Molarity Calculator
| 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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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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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.
