Antibodies
RG2833 (RGFP109)
- 貨號 Cat. No.
- S7292
- 規格 Size
- 10mgã€50mg
- 品牌 Brand
- Selleckchem
Description
RG2833 (RGFP109)
Catalog No.S7292
RG2833 (RGFP109) is a brain-penetrant HDAC inhibitor with IC50 of 60 nM and 50 nM for HDAC1 and HDAC3, respectively.
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | RG2833 (RGFP109) is a brain-penetrant HDAC inhibitor with IC50 of 60 nM and 50 nM for HDAC1 and HDAC3, respectively. | |||||
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| Targets | HDAC1 | HDAC1 | HDAC3 | HDAC3 | ||
| IC50 | 60 nM | 32 nM (Ki) | 50 nM | 5 nM (Ki) [1] | ||
| 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] | |||||
| Features | Orally bioavailable, HDAC inhibitor that penetrates into brain tissue. | |||||
Protocol(Only for Reference)
Kinase Assay: [1]
| Time dependent IC50 value with pre-incubation | Deacetylation assays are based on the homogenous fluorescence release assay. In brief, purified recombinant enzymes are incubated with serial-diluted inhibitors at various concentrations, with pre-incubation times ranging from 0 to 3 hours, in the standard HDAC buffer. Acetyl-Lys(Ac)-AMC substrate (at 10 μM, corresponding to the Km for both HDAC1 and HDAC3) is added after the pre-incubation period. The reaction is allowed to run for 1 hour. The trypsin peptidase developer, at final concentration of 5mg/ml, is added after 1 hour, and the fluorescence emission is then measured using a Tecan M200 96-well plate reader. |
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Animal Study: [1]
| Animal Models | KIKI mice |
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| Dosages | ~150 mg/kg |
| Administration | Subcutaneous injection |
References
Chemical Information
| Molecular Weight (MW) | 339.43 |
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| Formula | C20H25N3O2 |
| CAS No. | 1215493-56-3 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 68 mg/mL (200 mM) |
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| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | 10 mg/mL (29 mM) | ||
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. | |||
| Chemical Name | N-(6-(2-aminophenylamino)-6-oxohexyl)-4-methylbenzamide |
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