Name: RGFP966
Price: 260.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    RGFP966 is a selective inhibitor of HDAC3 with IC50 value of 80 nM [1].
    HDAC3 (histone deacetylase 3) is an isoform of HDACs family and plays an important role in DNA transcriptional regulation. It has been shown that HDACs involves in a variety of biologic processes, like DNA repair, replication, transcription and chromatin structure. Many studies have shown that HDACs is the most highly expressed class I HDAC in the brain and involves in learning and memory process negatively [2].
    RGFP966 is a potent HDAC3 inhibitor and has no inhibition on other HDACs at the concentration up to 15 μM. Using a substrate-dependent biochemical assay to investigate RGFP966 inhibition of HDACs, and results showed that it inhibited HDAC3 with IC50 value of 80 nM while had no effective inhibition on other HDACs [1]. When tested with cutaneous T cell lymphoma (CTCL) cell lines with RGFP966, the cell growth were significantly decreased by inhibiting HDAC3 which increased cell apoptosis [3].
    In male C57BL/6J mice model, trained them in object recognition (ORM) and location-dependent object recognition (OLM) with a subthreshold period after administration of RGFP966 significantly increased the novel object preference and enhanced enhanced long-term OLM in a dose-dependent manner [1].
    
    [1]. Malvaez, M., et al., HDAC3-selective inhibitor enhances extinction of cocaine-seeking behavior in a persistent manner. Proc Natl Acad Sci U S A, 2013. 110(7): p. 2647-52.
    [2]. Rogge, G.A., et al., HDAC3 is a negative regulator of cocaine-context-associated memory formation. J Neurosci, 2013. 33(15): p. 6623-32.
    [3]. Wells, C.E., et al., Inhibition of histone deacetylase 3 causes replication stress in cutaneous T cell lymphoma. PLoS One, 2013. 8(7): p. e68915.
- Properties
  - Alternative Name
    
    RGFP 966;RGFP-966
    
    CAS Number
    
    1357389-11-7;1396841-57-8
    
    Molecular Formula
    
    C21H19FN4O
    
    Molecular Weight
    
    362.4
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in H2O; ≥18.12 mg/mL in DMSO; ≥2.94 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Zhang M, Urabe G, et al. "HDAC6 Regulates the MRTF-A/SRF Axis and Vascular Smooth Muscle Cell Plasticity." JACC Basic Transl Sci. 2018 Dec 31;3(6):782-795. PMID:30623138
    2. Huang L, Lai WH, et al. "Elimination of HIV-1 Latently Infected Cells by Gnidimacrin and a Selective HDAC Inhibitor." ACS Med Chem Lett. 2018 Feb 6;9(3):268-273. PMID:29541372
    3. Topper MJ, Vaz M, et al. "Epigenetic Therapy Ties MYC Depletion to Reversing Immune Evasion and Treating Lung Cancer." Cell. 2017 Nov 30;171(6):1284-1300.e21. PMID:29195073
    4. Sun XY, Qu Y, et al. "Novel histone deacetylase inhibitor N25 exerts anti-tumor effects and induces autophagy in human glioma cells by inhibiting HDAC3."Oncotarget. 2017 Sep 8;8(43):75232-75242. PMID:29088860

RGFP966

RGFP966

Background

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