RG2833
Based on 13 publication(s) in Google Scholar
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.31%
- No. CAS: 1215493-56-3
- Fòrmula: C20H25N3O2
- Peso molecular:339.43
-
Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) RG2833
More- Cancer Res. 2021 Dec 15;81(24):6131-6141. [Abstract]
- J Clin Invest. 2024 Sep 10;134(21):e175310. [Abstract]
- Int J Biol Sci. 2026 May 18;22(10):5385-5398. [Abstract]
- Acta Pharmacol Sin. 2022 Feb;43(2):457-469. [Abstract]
- EMBO J. 2024 Nov;43(21):4954-4983. [Abstract]
- J Mol Med (Berl). 2019 Aug;97(8):1183-1193. [Abstract]
- J Neurochem. 2026 Jun;170(6):e70493. [Abstract]
- ACS Med Chem Lett. 2015 Jun 22;6(8):948-52. [Abstract]
- J Alzheimers Dis. 2025 Mar;104(1):173-190. [Abstract]
- PLoS One. 2016 Apr 14;11(4):e0153574. [Abstract]
- Virology. 2025 Jan:601:110305. [Abstract]
- Patent. US20250161243A1.
- Res Sq. 2024 May 28.
Actividad biológica
|
HDAC3 50 nM (IC50) |
HDAC1 60 nM (IC50) |
HDAC3 5 nM (Ki) |
HDAC1 32 nM (Ki) |
The Ki values of RG2833 for HDAC1 and HDAC3 are 32 nM and 5 nM, respectively. RG2833 is highly active in the whole tested concentration range from 1 to 10 μM. Continuous incubation with RG2833 slows the increase in frataxin protein, and when the compound is removed, frataxin protein levels rapidly increased in the cells from patient P13[1]. RG2833 produces significant increases in brain aconitase enzyme activity, together with reduction of neuronal pathology of the dorsal root ganglia (DRG)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
No. CAS 1215493-56-3
-
Appearance Solid
-
Peso molecular 339.43
-
Fòrmula C20H25N3O2
-
Color White to off-white
-
SMILES
O=C(NCCCCCC(NC1=CC=CC=C1N)=O)C2=CC=C(C)C=C2
-
Synonyms
RGFP109
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (13)
-
Journal Impact Factor
-
Most Recent
-
Cancer Res
2021 Dec 15;81(24):6131-6141. PMID: 34728538 -
J Clin Invest
Epigenetic regulation of cell state by H2AFY governs immunogenicity in high-risk neuroblastoma. [Abstract]2024 Sep 10;134(21):e175310. PMID: 39255035 -
Int J Biol Sci
E3 ligase UHRF2 hijacks nuclear TBK1 to epigenetically repress type I interferons expression. [Abstract]2026 May 18;22(10):5385-5398. PMID: 42212328 -
Acta Pharmacol Sin
2022 Feb;43(2):457-469. PMID: 33850273 -
EMBO J
Acetylation of TIR domains in the TLR4-Mal-MyD88 complex regulates immune responses in sepsis. [Abstract]2024 Nov;43(21):4954-4983. PMID: 39294473 -
J Mol Med (Berl)
2019 Aug;97(8):1183-1193. PMID: 31201471 -
J Neurochem
Effects of Lysine Deacetylation Inhibition Alone or in Combination With Arimoclomol on TDP-43 Proteinopathy. [Abstract]2026 Jun;170(6):e70493. PMID: 42283221 -
ACS Med Chem Lett
High-Throughput Screening of Patient-Derived Cultures Reveals Potential for Precision Medicine in Glioblastoma. [Abstract]2015 Jun 22;6(8):948-52. PMID: 26288699 -
J Alzheimers Dis
Brain-penetrant histone deacetylase inhibitor RG2833 improves spatial memory in females of an Alzheimer's disease rat model. [Abstract]2025 Mar;104(1):173-190. PMID: 39924842 -
PLoS One
Lymphoblast Oxidative Stress Genes as Potential Biomarkers of Disease Severity and Drug Effect in Friedreich's Ataxia. [Abstract]2016 Apr 14;11(4):e0153574. PMID: 27078885 -
Virology
H1N1 swine influenza viruses upregulate NEU1 expression through histone H3 acetylation regulated by HDAC2. [Abstract]2025 Jan:601:110305. PMID: 39566266 -
-
Solvente y solubilidad
DMSO : ≥ 50 mg/mL (147.31 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.37 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.37 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
-
Ficha de datos (277 KB)
-
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
-
Instrucciones de manejo (2659 KB)
Referencias
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9461 mL | 14.7306 mL | 29.4612 mL | 73.6529 mL |
| 5 mM | 0.5892 mL | 2.9461 mL | 5.8922 mL | 14.7306 mL | |
| 10 mM | 0.2946 mL | 1.4731 mL | 2.9461 mL | 7.3653 mL | |
| 15 mM | 0.1964 mL | 0.9820 mL | 1.9641 mL | 4.9102 mL | |
| 20 mM | 0.1473 mL | 0.7365 mL | 1.4731 mL | 3.6826 mL | |
| 25 mM | 0.1178 mL | 0.5892 mL | 1.1784 mL | 2.9461 mL | |
| 30 mM | 0.0982 mL | 0.4910 mL | 0.9820 mL | 2.4551 mL | |
| 40 mM | 0.0737 mL | 0.3683 mL | 0.7365 mL | 1.8413 mL | |
| 50 mM | 0.0589 mL | 0.2946 mL | 0.5892 mL | 1.4731 mL | |
| 60 mM | 0.0491 mL | 0.2455 mL | 0.4910 mL | 1.2275 mL | |
| 80 mM | 0.0368 mL | 0.1841 mL | 0.3683 mL | 0.9207 mL | |
| 100 mM | 0.0295 mL | 0.1473 mL | 0.2946 mL | 0.7365 mL |
RG2833 Related Classifications
HY-16425 Related Classifications
Powered by Bioz