IF 14
PMID: 39434145 ↗RGFP966
Catalog No.: GC14285Purity:>98.00%Synonyms: RGFP 966;RGFP-966
RGFP966 is an N-(o-aminophenyl) carboxamide HDAC inhibitor with an IC50 of 0.08 μM for HDAC3, It is a class of slow on/slow off competitive tight binding inhibitors targeting HDAC3.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1357389-11-7
10mM (in 1mL DMSO)In Stock
$79.00
1
5mgIn Stock
$62.00
1
25mgIn Stock
$141.00
1
100mgIn Stock
$456.00
1
200mgIn Stock
$686.00
1
| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 10mM (in 1mL DMSO) | $79.00 | In Stock | 1 | |
| 5mg | $62.00 | In Stock | 1 | |
| 25mg | $141.00 | In Stock | 1 | |
| 100mg | $456.00 | In Stock | 1 | |
| 200mg | $686.00 | In Stock | 1 |
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com
Citations
3 publicationsPublications from researchers using this productDescription
RGFP966 is an N-(o-aminophenyl) carboxamide HDAC inhibitor with an IC50 of 0.08 μM for HDAC3, It is a class of slow on/slow off competitive tight binding inhibitors targeting HDAC3. RGFP966 has been demonstrated to suppress inflammatory responses in various inflammatory diseases [1-3].
RGFP966(1μM ;20 h) attenuates the inflammatory gene expression in LPS/IFNγ-stimulated RAW 264.7 macrophage[3]. RGFP966(10-25μM;48h) inhibited both proliferation and migration of HCC cells[4].
RGFP966(10 mg/kg;6h before SBI) inhibited the upregulation of HDAC3 and saved the nerve cells around the damaged area in surgical brain injury (SBI) rats[5]. RGFP966(10 mg/kg/day;i.p; 5days) could improve the LPS-induced depressive-like behaviors in mice. RGFP966 treatment downregulated the expression levels of toll-like receptor 4 (TLR4), nucleotide-binding oligomerization domain-like receptor pyrin domain-containing-3 (NLRP3), caspase-1, and interleukin-1β (IL-1β) [6]. RGFP966(10 mg/kg or 20 mg/kg) reduce HDAC3 expression and HDAC3 activities, and then eosinophils and mast cells recruitment, goblet cells proliferation and inflammatory cytokines levels are decreased, resulting in the alleviation of allergic and inflammatory responses in allergic rhinitis (AR) mice [7].
References:
[1]. Malvaez M, McQuown SC, et,al. HDAC3-selective inhibitor enhances extinction of cocaine-seeking behavior in a persistent manner. Proc Natl Acad Sci U S A. 2013 Feb 12;110(7):2647-52. doi: 10.1073/pnas.1213364110. Epub 2013 Jan 7. PMID: 23297220; PMCID: PMC3574934.
[2]. Chou CJ, Herman D, et,al. Pimelic diphenylamide 106 is a slow, tight-binding inhibitor of class I histone deacetylases. J Biol Chem. 2008 Dec 19;283(51):35402-9. doi: 10.1074/jbc.M807045200. Epub 2008 Oct 24. PMID: 18953021; PMCID: PMC2602898.
[3]. Leus NG, van der Wouden PE, et,al. HDAC 3-selective inhibitor RGFP966 demonstrates anti-inflammatory properties in RAW 264.7 macrophages and mouse precision-cut lung slices by attenuating NF-κB p65 transcriptional activity. Biochem Pharmacol. 2016 May 15;108:58-74. doi: 10.1016/j.bcp.2016.03.010. Epub 2016 Mar 16. PMID: 26993378; PMCID: PMC4844503.
[4]. Yu X, Yang F, et,al. RGFP966 Suppresses Tumor Growth and Migration Through Inhibition of EGFR Expression in Hepatocellular Carcinoma Cells in vitro. Drug Des Devel Ther. 2020 Jan 10;14:121-128. doi: 10.2147/DDDT.S234871. PMID: 32021097; PMCID: PMC6959505.
[5]. Gu HP, Wu XF, et,al. RGFP966 exerts neuroprotective effect via HDAC3/Nrf2 pathway after surgical brain injury in rats. Heliyon. 2023 Jul 12;9(7):e18160. doi: 10.1016/j.heliyon.2023.e18160. PMID: 37539293; PMCID: PMC10395478.
[6]. Bian HT, Xiao L, et,al. RGFP966 is protective against lipopolysaccharide-induced depressive-like behaviors in mice by inhibiting neuroinflammation and microglial activation. Int Immunopharmacol. 2021 Dec;101(Pt B):108259. doi: 10.1016/j.intimp.2021.108259. Epub 2021 Oct 16. PMID: 34666303.
[7]. Zhang W, Sun X, et,al. RGFP966, a selective HDAC3 inhibitor, ameliorates allergic and inflammatory responses in an OVA-induced allergic rhinitis mouse model. Int Immunopharmacol. 2021 Apr;93:107400. doi: 10.1016/j.intimp.2021.107400. Epub 2021 Jan 30. PMID: 33529911.
Protocol
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Cell experiment [1]: |
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Cell lines |
Mouse RAW 264.7 macrophages |
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Preparation method |
Cells were incubated with 1μM RGFP966 for 20 h and stimulated with LPS/IFNγ for the last 4 h. |
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Reaction Conditions |
1μM ;20 h |
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Applications |
RGFP966 attenuates the inflammatory gene expression in LPS/IFNγ-stimulated RAW 264.7 macrophage. |
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Animal experiment [2]: |
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Animal models |
Adult male C57BL/6J mice (weight 20–22g) |
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Preparation method |
Mice were divided into four groups: control group, LPS group, LPS + RGFP966 group, and RGFP966 group. LPS was solubilized in phosphate-buffered saline (PBS) and intraperitoneally (i.p.) injected at a dosage of 1 mg/kg/day for a total of five injections. RGFP966 was diluted in dimethyl sulfoxide (DMSO), PEG300, and saline, and then, it was i.p. injected at a dosage of 10 mg/kg/day for a total of five injections. |
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Dosage form |
10 mg/kg/day;i.p; 5days |
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Applications |
RGFP966 treatment reversed the LPS-induced body weight changes in mice. |
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References: [1]. Leus NG, van der Wouden PE, et,al. HDAC 3-selective inhibitor RGFP966 demonstrates anti-inflammatory properties in RAW 264.7 macrophages and mouse precision-cut lung slices by attenuating NF-κB p65 transcriptional activity. Biochem Pharmacol. 2016 May 15;108:58-74. doi: 10.1016/j.bcp.2016.03.010. Epub 2016 Mar 16. PMID: 26993378; PMCID: PMC4844503. [2]. Bian HT, Xiao L, et,al. RGFP966 is protective against lipopolysaccharide-induced depressive-like behaviors in mice by inhibiting neuroinflammation and microglial activation. Int Immunopharmacol. 2021 Dec;101(Pt B):108259. doi: 10.1016/j.intimp.2021.108259. Epub 2021 Oct 16. PMID: 34666303. |
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Product Documents
Purity:>98.00%Appearance:A solid
Chemical Properties
CAS No.
1357389-11-7
Synonyms
RGFP 966;RGFP-966
SMILES
C1=CC=C(C=C1)C=CCN2C=C(C=N2)C=CC(=O)NC3=C(C=C(C=C3)F)N
Molecular Formula
C21H19FN4O
Molecular Weight
362.4
Solubility
≥ 18.12mg/mL in DMSO
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.
CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility
g/mol
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