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Name:RG2833
Chemical structure | Code NO. |
MT1053 |
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Name |
RG2833 |
Synonym |
RG 2833; RG-2833; RGFP-109; RGFP109; RGFP 109 | |
CAS NO. |
1215493-56-3 | |
Chemical Formula |
C20H25N3O2 | |
MW |
339.43 | |
Purity |
>98% | |
Solubility(R.T.: 25℃) |
DMSO 68 mg/ml; Water <1 mg/ml | |
Stability |
- 20℃, 2 years |
Availability and price
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Description
RG2833 (RGFP109) is a brain-penetrant HDAC inhibitor with IC50 of 60 nM and 50 nM for HDAC1 and HDAC3, respectively.
IC50 Value: 60 nM (HDAC1); 50 nM (HDAC3) [1]
Target: HDAC1/3
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].
Clinical trial: Phase 1
IC50 Value: 60 nM (HDAC1); 50 nM (HDAC3) [1]
Target: HDAC1/3
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].
Clinical trial: Phase 1
References
Attention
Sold for research purposes only; not for human use of any kind.