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RGFP966 is an HDAC3 inhibitor with IC50 of 0.08 μM, exhibits > 200-fold selectivity over other HDAC. Systemic treatment with RGFP966 facilitates extinction in mice in a manner resistant to reinstatement. A single treatment of RGFP966 enhances extinction of a previously established cocaine-conditioned place preference, while simultaneously enhancing long-term object-location memory within subjects. HDAC3 inhibition using a first in class selective inhibitor, RGFP966, resulted in decreased cell growth in CTCL cell lines due to increased apoptosis that was associated with DNA damage and impaired S phase progression. Selective inhibition of HDAC3 could be useful in treatment of CTCL by disrupting DNA replication of the rapidly cycling tumor cells, ultimately leading to cell death.
Another CAS# 1396841-57-8
Cancer Res. 2024 May 8.
HDAC Inhibition Increases CXCL12 Secretion to Recruit Natural Killer Cells in Peripheral T Cell Lymphoma | Cancer Research | American Association for Cancer Research
RGFP966 purchased from AbMole
FEBS J. 2024 Sep 09.
MOF-mediated acetylation of CDK9 promotes global transcription by modulating P-TEFb complex formation
RGFP966 purchased from AbMole
Cell Death Differ. 2023 Mar 9.
Targeting HDAC3 to overcome the resistance to ATRA or arsenic in acute promyelocytic leukemia through ubiquitination and degradation of PML-RARα
RGFP966 purchased from AbMole
Inflamm Res. 2022 Dec;71(12):1547-1557.
C/EBPβ enhances immunosuppression activity of myeloid-derived suppressor cells by a P300-mediated acetylation modification
RGFP966 purchased from AbMole
University of Otago. 2019.
Transcriptional effects of mood stabiliser drugs in a serotonergic cell line
RGFP966 purchased from AbMole
 |
Source | EMBO Mol Med (2018). Figure 2. RGFP966 |
| Method | Western blots | |
| Cell Lines | C4-2 cells | |
| Concentrations | 3 μM | |
| Incubation Time | 24 h | |
| Results | The HDAC3 inhibitor RGFP966 also undermined AKT ubiquitination |
| Molecular Weight | 362.4 |
| Formula | C21H19FN4O |
| CAS Number | 1357389-11-7 |
| Solubility (25°C) | DMSO 55 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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