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.
| Storage | Store at -20°C |
| M.Wt | 339.43 |
| Cas No. | 1215493-56-3 |
| Formula | C20H25N3O2 |
| Synonyms | RG 2833;RG-2833;RGFP-109;RGFP109;RGFP 109 |
| Solubility | insoluble in H2O; ≥16.95 mg/mL in DMSO; ≥8.05 mg/mL in EtOH with gentle warming and ultrasonic |
| Chemical Name | N-[6-(2-aminoanilino)-6-oxohexyl]-4-methylbenzamide |
| SDF | Download SDF |
| Canonical SMILES | CC1=CC=C(C=C1)C(=O)NCCCCCC(=O)NC2=CC=CC=C2N |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
Unstimulated peripheral blood mononuclear cells (PBMC) from FRDA Patients. |
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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. |
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Reacting condition |
1, 2.5, 5 or 10 μM for 48 hours |
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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]: | |
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Animal models |
GAA knock-in mice |
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Dosage form |
150 mg/kg, subcutaneous injection |
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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. |
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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. |
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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. | |
| 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 & MSDS
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Chemical structure
