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Submit ReviewRGFP 966
Description: Potent and selective HDAC3 inhibitor
Chemical Name: (2E)-N-(2-Amino-4-fluorophenyl)-3-[1-(3-phenyl-2-propen-1-yl)-1H-pyrazol-4-yl]-2-propenamide
Purity: ≥98% (HPLC)
Biological Activity for RGFP 966
RGFP 966 is a potent and selective HDAC3 inhibitor (IC50 = 80 nM); exhibits no effect on other HDAC (up to 15 μM). RGFP 966 reduces the frequency of striatal CAG repeat expansions in mouse models of Huntington's disease and reduces mHTT accumulation. RGFP 966 blocks the formation of reactive astrocytes and, in vivo, it is neuroprotective and enhances long-term object-location memory.
Compound Libraries for RGFP 966
RGFP 966 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.
Technical Data for RGFP 966
| M. Wt | 362.4 |
| Formula | C21H19FN4O |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1357389-11-7 |
| PubChem ID | 56650312 |
| InChI Key | BLVQHYHDYFTPDV-VCABWLAWSA-N |
| Smiles | NC1=C(C=CC(F)=C1)NC(/C=C/C2=CN(N=C2)C/C=C/C3=CC=CC=C3)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for RGFP 966
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 36.24 | 100 |
Preparing Stock Solutions for RGFP 966
The following data is based on the product molecular weight 362.4. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.76 mL | 13.8 mL | 27.59 mL |
| 5 mM | 0.55 mL | 2.76 mL | 5.52 mL |
| 10 mM | 0.28 mL | 1.38 mL | 2.76 mL |
| 50 mM | 0.06 mL | 0.28 mL | 0.55 mL |
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Product Datasheets for RGFP 966
References for RGFP 966
References are publications that support the biological activity of the product.
Malvaez et al (2013) HDAC3-selective inhibitor enhances extinction of cocaine-seeking behavior in a persistent manner. Proc.Natl.Acad.Sci.USA. 110 2647 PMID: 23297220
Suelvez et al (2017) A selective inhibitor of histone deacetylase 3 prevents cognitive deficits and suppresses striatal CAG repeat expansions in Huntington's disease mice. Sci.Rep. 7 PMID: 28729730
Clayton et al (2024) A phenotypic screening platform for identifying chemical modulators of astrocyte reactivity. Nat.Neurosci. PMID: 38378993
If you know of a relevant reference for RGFP 966, please let us know.
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Keywords: RGFP 966, RGFP 966 supplier, RGFP966, potent, selective, HDAC, 3, inhibitors, inhibits, Class, I, HDACs, 6728, Tocris Bioscience
1 Citation for RGFP 966
Citations are publications that use Tocris products. Selected citations for RGFP 966 include:
Ting et al (2022) NF-κB-dependent repression of Sox18 transcription factor requires the epigenetic regulators histone deacetylases 1 and 2 in acute lung injury. Front Physiol 13 947537 PMID: 35991176
Do you know of a great paper that uses RGFP 966 from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Epigenetics Scientific Review
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.
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In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. This poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.
Epigenetics in Cancer Poster
This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.
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Rheumatoid arthritis (RA) is a chronic destructive inflammatory autoimmune disease that results from a breakdown in immune tolerance, for reasons that are as yet unknown. This poster summarizes the pathology of RA and the inflammatory processes involved, as well as describing some of the epigenetic modifications associated with the disease and the potential for targeting these changes in the discovery of new treatments.