RGFP966 (Synonyms: RGFP 966;RGFP-966) |
| Catalog No.GC14285 |
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
Sample solution is provided at 25 µL, 10mM.
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.
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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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| Cas No. | 1357389-11-7 | SDF | |
| Synonyms | RGFP 966;RGFP-966 | ||
| Canonical SMILES | C1=CC=C(C=C1)C=CCN2C=C(C=N2)C=CC(=O)NC3=C(C=C(C=C3)F)N | ||
| Formula | C21H19FN4O | M.Wt | 362.4 |
| Solubility | ≥ 18.12mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7594 mL | 13.7969 mL | 27.5938 mL |
| 5 mM | 0.5519 mL | 2.7594 mL | 5.5188 mL |
| 10 mM | 0.2759 mL | 1.3797 mL | 2.7594 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 8 reference(s) in Google Scholar.)
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