RGFP966
Based on 58 publication(s) in Google Scholar
RGFP966 is a highly selective HDAC3 inhibitor with an IC50 of 80 nM and shows no inhibition to other HDACs at concentrations up to 15 μM. RGFP966 can penetrate the blood brain barrier (BBB).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.81%
- No. CAS: 1357389-11-7
- Fòrmula: C21H19FN4O
- Peso molecular:362.40
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) RGFP966
More- Cancer Cell. 2024 Oct 14;42(10):1729-1746.e8. [Abstract]
- Cell. 2024 Jun 20;187(13):3409-3426.e24. [Abstract]
- Cell Metab. 2021 Dec 7;33(12):2355-2366.e8. [Abstract]
- Autophagy. 2025 Aug 28:1-15. [Abstract]
- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Redox Biol. 2026 Mar:90:104034. [Abstract]
- Mol Cell. 2020 Oct 1;80(1):43-58.e7. [Abstract]
- Nucleic Acids Res. 2023 Jun 23;51(11):5396-5413. [Abstract]
- Theranostics. 2021 Mar 20;11(11):5605-5619. [Abstract]
- Adv Sci (Weinh). 2025 Aug 7:e02624. [Abstract]
- Cell Rep Med. 2025 Jul 15;6(7):102215. [Abstract]
- Cell Rep Med. 2024 Oct 15;5(10):101770. [Abstract]
- Sci Adv. 2026 Jul 24;12(30):eaeg2060.
- Sci Adv. 2025 Feb 28;11(9):eadq2881. [Abstract]
- Cell Death Differ. 2023 Jul;30(7):1811-1828. [Abstract]
- Cell Death Dis. 2022 Aug 17;13(8):717. [Abstract]
- Cell Death Dis. 2021 May 18;12(6):501. [Abstract]
- Cell Death Dis. 2020 Sep 15;11(9):753. [Abstract]
- Cell Death Dis. 2018 Apr 1;9(4):423. [Abstract]
- Cancer Lett. 2026 Mar 28:218465. [Abstract]
- Cell Commun Signal. 2021 Mar 18;19(1):35. [Abstract]
- Cell Commun Signal. 2019 Mar 12;17(1):23. [Abstract]
- J Neuroinflammation. 2025 Nov 26;22(1):280. [Abstract]
- Int J Nanomedicine. 2026 Feb 14:21:577455. [Abstract]
- Antioxidants (Basel). 2026 Jul 20;15(7):898.
- Clin Transl Med. 2026 Feb;16(2):e70603. [Abstract]
- Cell Rep. 2021 Feb 16;34(7):108744. [Abstract]
- Br J Pharmacol. 2024 Oct;181(19):3663-3684. [Abstract]
- Cell Syst. 2018 Apr 25;6(4):424-443.e7. [Abstract]
- Mol Cancer Ther. 2020 Dec;19(12):2542-2553. [Abstract]
- J Agric Food Chem. 2024 Nov 6;72(44):24400-24416. [Abstract]
- Sci Technol Adv Mater. 2026 Jul 16.
- J Bone Miner Res. 2024 Aug 5;39(7):994-1007. [Abstract]
- Food Biosci. 2024 Dec.
- Drug Des Devel Ther. 2020 Jan 10:14:121-128. [Abstract]
- Pain. 2021 Feb 1;162(2):382-395. [Abstract]
- Clin Epigenetics. 2023 Nov 11;15(1):182. [Abstract]
- Int J Mol Sci. 2022 Apr 2;23(7):3980. [Abstract]
- Int Immunopharmacol. 2021 Dec;101(Pt B):108259. [Abstract]
- mBio. 2026 Feb 11;17(2):e0328925. [Abstract]
- J Mol Med (Berl). 2019 Aug;97(8):1183-1193. [Abstract]
- Cancers (Basel). 2022 Sep 28;14(19):4718. [Abstract]
- Cancers (Basel). 2022 Jan 18;14(3):457. [Abstract]
- J Neurochem. 2026 Jun;170(6):e70493. [Abstract]
- Front Physiol. 2019 Aug 20:10:1060. [Abstract]
- Fish Shellfish Immunol. 2023 Dec:143:109214. [Abstract]
- Lab Invest. 2023 Jun;103(6):100120. [Abstract]
- Reprod Biomed Online. 2023 Nov;47(5):103288. [Abstract]
- Pancreatology. 2019 Mar;19(2):383-389. [Abstract]
- Res Sq. 2026 Jun 15.
- bioRxiv. 2026 Jun 5.
- Res Sq. 2026 Apr 30.
- bioRxiv. 2025 Oct 20:2025.10.19.683261. [Abstract]
- bioRxiv. 2025 Apr 26:2025.04.23.650241. [Abstract]
- Heliyon. 2024 Oct 11;10(21):e39333. [Abstract]
- Research Square Print. 2023 Feb 7.
- bioRxiv. May 10, 2022.
- Patent. US20180263995A1.
Customer Validation & Images
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In Vivo Imaging
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IF
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IP
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IF
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WB
Actividad biológica
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HDAC3 80 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEL | IC50 |
1.64 μM
Compound: 29; RGFP966
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Antiproliferative activity against human HEL cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay
Antiproliferative activity against human HEL cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay
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[PMID: 29940115] |
| HEL | IC50 |
21.71 μM
Compound: 29; RGFP966
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Antiproliferative activity against human HEL cells after 48 hrs by CCK-8 assay
Antiproliferative activity against human HEL cells after 48 hrs by CCK-8 assay
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[PMID: 29940115] |
| HL-60 | IC50 |
1.64 μM
Compound: 29; RGFP966
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Antiproliferative activity against human HL60 cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay
Antiproliferative activity against human HL60 cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay
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[PMID: 29940115] |
| HL-60 | IC50 |
21.71 μM
Compound: 29; RGFP966
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Antiproliferative activity against human HL60 cells after 48 hrs by CCK-8 assay
Antiproliferative activity against human HL60 cells after 48 hrs by CCK-8 assay
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[PMID: 29940115] |
| K562 | IC50 |
1.64 μM
Compound: 29; RGFP966
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Antiproliferative activity against human K562 cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay
Antiproliferative activity against human K562 cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay
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[PMID: 29940115] |
| K562 | IC50 |
21.71 μM
Compound: 29; RGFP966
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Antiproliferative activity against human K562 cells after 48 hrs by CCK-8 assay
Antiproliferative activity against human K562 cells after 48 hrs by CCK-8 assay
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[PMID: 29940115] |
RGFP966 potently and selectively inhibits HDAC 3 with IC50 of 0.21 μM in RAW 264.7 macrophages, while HDACs 1 (IC50=5.6 μM), 2 (9.7 μM) and 8 (>100 μM), indicating a good level of selectivity for HDAC 3. The mRNA levels of HDACs 1, 2 and 3 are not significantly affected by RGFP966 in RAW 264.7 macrophages, whereas the HDAC 1 and HDAC 2 protein levels are slightly, though significantly, reduced upon RGFP966 treatment. Moreover, RGFP966 significantly reduced the transcriptional activity of NF-κB p65, whereas NF-κB p65 acetylation and localization remain unaltered[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1357389-11-7
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Appearance Solid
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Peso molecular 362.40
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Fòrmula C21H19FN4O
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Color White to off-white
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SMILES
O=C(NC1=CC=C(F)C=C1N)/C=C/C2=CN(C/C=C/C3=CC=CC=C3)N=C2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (58)
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Journal Impact Factor
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Most Recent
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Cancer Cell
Fusobacterium nucleatum facilitates anti-PD-1 therapy in microsatellite stable colorectal cancer. [Abstract]2024 Oct 14;42(10):1729-1746.e8. PMID: 39303724 -
Cell
Osr2 functions as a biomechanical checkpoint to aggravate CD8+ T cell exhaustion in tumor. [Abstract]2024 Jun 20;187(13):3409-3426.e24. PMID: 38744281 -
Cell Metab
Microbial regulation of hexokinase 2 links mitochondrial metabolism and cell death in colitis. [Abstract]2021 Dec 7;33(12):2355-2366.e8. PMID: 34847376 -
Autophagy
2025 Aug 28:1-15. PMID: 40851277 -
Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Redox Biol
Methylation reader MBD2-mediated GPX4 transcriptional repression drives ovarian granulosa cell ferroptosis in PCOS. [Abstract]2026 Mar:90:104034. PMID: 41576700 -
Mol Cell
Histone Deacetylase 3 Couples Mitochondria to Drive IL-1β-Dependent Inflammation by Configuring Fatty Acid Oxidation. [Abstract]2020 Oct 1;80(1):43-58.e7. PMID: 32937100
RGFP966 purchased from MedChemExpress. Usage Cited in: Mol Cell. 2020 Oct 1;80(1):43-58.e7. [Abstract]
LPS-primed BMDMs treated with RGFP966 (2-10 μM) 30 min before ATP. SNs and cell extracts (lysate) were analyzed by immunoblotting.
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Nucleic Acids Res
2023 Jun 23;51(11):5396-5413. PMID: 36971114 -
Theranostics
HDAC1 and 2 regulate endothelial VCAM-1 expression and atherogenesis by suppressing methylation of the GATA6 promoter. [Abstract]2021 Mar 20;11(11):5605-5619. PMID: 33859766 -
Adv Sci (Weinh)
The Probiotic Parabacteroides johnsonii Ameliorates Metabolic Disorders Through Promoting BCAAs to BSCFAs Conversion. [Abstract]2025 Aug 7:e02624. PMID: 40772426 -
Cell Rep Med
Epigenetic profiling identifies markers of endocrine resistance and therapeutic options for metastatic castration-resistant prostate cancer. [Abstract]2025 Jul 15;6(7):102215. PMID: 40609538 -
Cell Rep Med
2024 Oct 15;5(10):101770. PMID: 39368485 -
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Sci Adv
Local soft niches in mechanically heterogeneous primary tumors promote brain metastasis via mechanotransduction-mediated HDAC3 activity. [Abstract]2025 Feb 28;11(9):eadq2881. PMID: 40009679
RGFP966 purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Feb 28;11(9):eadq2881. [Abstract]
RGFP966 (10 mg/kg or 40 mg/kg; i.p.; every 2 days for 28 days) significantly increased the brain metastasis-free survival in a dose-dependent manner.
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Cell Death Differ
2023 Jul;30(7):1811-1828. PMID: 37322264 -
Cell Death Dis
Global crotonylome reveals hypoxia-mediated lamin A crotonylation regulated by HDAC6 in liver cancer. [Abstract]2022 Aug 17;13(8):717. PMID: 35977926 -
Cell Death Dis
IL-4 inhibits regulatory T cells differentiation by HDAC9-mediated epigenetic regulation. [Abstract]2021 May 18;12(6):501. PMID: 34006836 -
Cell Death Dis
Checkpoint regulator B7x is epigenetically regulated by HDAC3 and mediates resistance to HDAC inhibitors by reprogramming the tumor immune environment in colorectal cancer. [Abstract]2020 Sep 15;11(9):753. PMID: 32934224 -
Cell Death Dis
PIWIL2 suppresses Siah2-mediated degradation of HDAC3 and facilitates CK2α-mediated HDAC3 phosphorylation. [Abstract]2018 Apr 1;9(4):423. PMID: 29555935 -
Cancer Lett
HOX code-based stratification reveals RUNX1T1-HDAC reprogramming as a targetable driver of lineage plasticity across cancers. [Abstract]2026 Mar 28:218465. PMID: 41912135 -
Cell Commun Signal
Histone deacetylase 3 inhibition alleviates type 2 diabetes mellitus-induced endothelial dysfunction via Nrf2. [Abstract]2021 Mar 18;19(1):35. PMID: 33736642
RGFP966 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2021 Mar 18;19(1):35. [Abstract]
Representative immunofluorescence with CD31 from db/m mice, db/db mice, and RGFP966 or vehicle treated (10 mg/kg; s.c.) db/db mice aorta tissue sections. The red area represented endothelium and the nucleus was blue. Scale bars: 200 μm.
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Cell Commun Signal
Low levels of pyruvate induced by a positive feedback loop protects cholangiocarcinoma cells from apoptosis. [Abstract]2019 Mar 12;17(1):23. PMID: 30866966 -
J Neuroinflammation
FOXA2 regulated by HDAC3-mediated deacetylation attenuates neuropathic pain by modulating microglial lipid metabolism and synaptic pruning dysregulation. [Abstract]2025 Nov 26;22(1):280. PMID: 41299504
RGFP966 purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2025 Nov 26;22(1):280. [Abstract]
RGFP966 (1 µg/µL; i.t.; single dose) alleviated LDs accumulation in SDH. Scale bars: 100μm.
RGFP966 purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2025 Nov 26;22(1):280. [Abstract]
Level of lysine acetylation of FOXA2 in BV2 cells after treatment with vehicle (PBS) or RGFP966 (15 µM; 6 h).
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Int J Nanomedicine
LincRNA-p21: A Double-Edged Sword in Ethanol-Induced Liver Damage and Its Nanoparticle Solution. [Abstract]2026 Feb 14:21:577455. PMID: 41717312 -
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Clin Transl Med
2026 Feb;16(2):e70603. PMID: 41603084 -
Cell Rep
An acetyl-histone vulnerability in PI3K/AKT inhibition-resistant cancers is targetable by both BET and HDAC inhibitors. [Abstract]2021 Feb 16;34(7):108744. PMID: 33596421 -
Br J Pharmacol
Silibinin, a commonly used therapeutic agent for non-alcohol fatty liver disease, functions through upregulating intestinal expression of fibroblast growth factor 15/19. [Abstract]2024 Oct;181(19):3663-3684. PMID: 38839561 -
Cell Syst
A Library of Phosphoproteomic and Chromatin Signatures for Characterizing Cellular Responses to Drug Perturbations. [Abstract]2018 Apr 25;6(4):424-443.e7. PMID: 29655704 -
Mol Cancer Ther
A Combination of BRD4 and HDAC3 Inhibitors Synergistically Suppresses Glioma Stem Cell Growth by Blocking GLI1/IL6/STAT3 Signaling Axis. [Abstract]2020 Dec;19(12):2542-2553. PMID: 32999044 -
J Agric Food Chem
Butyrate Inhibits the HDAC8/NF-κB Pathway to Enhance Slc26a3 Expression and Improve the Intestinal Epithelial Barrier to Relieve Colitis. [Abstract]2024 Nov 6;72(44):24400-24416. PMID: 39440960 -
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J Bone Miner Res
Hdac3-deficiency increases senescence-associated distention of satellite DNA and telomere-associated foci in osteoprogenitor cells. [Abstract]2024 Aug 5;39(7):994-1007. PMID: 38843356 -
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Drug Des Devel Ther
RGFP966 Suppresses Tumor Growth and Migration Through Inhibition of EGFR Expression in Hepatocellular Carcinoma Cells in vitro. [Abstract]2020 Jan 10:14:121-128. PMID: 32021097 -
Pain
Histone deacetylase 3 in hippocampus contributes to memory impairment after chronic constriction injury of sciatic nerve in mice. [Abstract]2021 Feb 1;162(2):382-395. PMID: 32868749 -
Clin Epigenetics
Histone deacetylase 3 deletion in alveolar type 2 epithelial cells prevents bleomycin-induced pulmonary fibrosis. [Abstract]2023 Nov 11;15(1):182. PMID: 37951958 -
Int J Mol Sci
Butyrate Prevents Induction of CXCL10 and Non-Canonical IRF9 Expression by Activated Human Intestinal Epithelial Cells via HDAC Inhibition. [Abstract]2022 Apr 2;23(7):3980. PMID: 35409339 -
Int Immunopharmacol
RGFP966 is protective against lipopolysaccharide-induced depressive-like behaviors in mice by inhibiting neuroinflammation and microglial activation. [Abstract]2021 Dec;101(Pt B):108259. PMID: 34666303 -
mBio
2026 Feb 11;17(2):e0328925. PMID: 41575215 -
J Mol Med (Berl)
2019 Aug;97(8):1183-1193. PMID: 31201471 -
Cancers (Basel)
Histone Deacetylase 3 Governs β-Estradiol-ERα-Involved Endometrial Tumorigenesis via Inhibition of STING Transcription. [Abstract]2022 Sep 28;14(19):4718. PMID: 36230643 -
Cancers (Basel)
c-Myc Targets HDAC3 to Suppress NKG2DL Expression and Innate Immune Response in N-Type SCLC through Histone Deacetylation. [Abstract]2022 Jan 18;14(3):457. PMID: 35158730 -
J Neurochem
Effects of Lysine Deacetylation Inhibition Alone or in Combination With Arimoclomol on TDP-43 Proteinopathy. [Abstract]2026 Jun;170(6):e70493. PMID: 42283221 -
Front Physiol
The Therapeutic Effects of Treadmill Exercise on Osteoarthritis in Rats by Inhibiting the HDAC3/NF-KappaB Pathway in vivo and in vitro. [Abstract]2019 Aug 20:10:1060. PMID: 31481898
RGFP966 purchased from MedChemExpress. Usage Cited in: Front Physiol. 2019 Aug 20:10:1060. [Abstract]
Osteoarthritis rats are treated with RGFP966. Immunohistochemistry (IHC) was performed to measure relative inflammatory proteins in OA. Expression of collagen II in CG and OAG + RGFP966 group is higher than OAG by IHC.
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Fish Shellfish Immunol
Butyrate induces STAT3/HIF-1α/IL-22 signaling via GPCR and HDAC3 inhibition to activate autophagy in head kidney macrophages from turbot (Scophthalmus maximus L.). [Abstract]2023 Dec:143:109214. PMID: 37977544 -
Lab Invest
HDAC3 controls liver homeostasis more by facilitating DNA damage repair than by regulating transcription in hepatocytes. [Abstract]2023 Jun;103(6):100120. PMID: 36801398 -
Reprod Biomed Online
Reduced endometrial expression of histone deacetylase 3 in women with adenomyosis who complained of heavy menstrual bleeding. [Abstract]2023 Nov;47(5):103288. PMID: 37690341 -
Pancreatology
2019 Mar;19(2):383-389. PMID: 30670333
RGFP966 purchased from MedChemExpress. Usage Cited in: Pancreatology. 2019 Mar;19(2):383-389. [Abstract]
RGFP966 decreases PD-L1 expression in a time- and dose-dependent manner in pancreatic cancer cells.
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bioRxiv
Butyrate rescues chlorpyrifos-induced social deficits through inhibition of class I histone deacetylases. [Abstract]2025 Oct 20:2025.10.19.683261. PMID: 41280077 -
bioRxiv
A nuclear branched-chain amino acid catabolism pathway controls histone propionylation in pancreatic cancer. [Abstract]2025 Apr 26:2025.04.23.650241. PMID: 40568091 -
Heliyon
Role of HDAC3 in the epithelial-mesenchymal transition of retinal pigment epithelium cells: Implications for proliferative vitreoretinopathy. [Abstract]2024 Oct 11;10(21):e39333. PMID: 39524785 -
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Solvente y solubilidad
DMF : 50 mg/mL (137.97 mM; Need ultrasonic)
DMSO : 50 mg/mL (137.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.90 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 7.69 mg/mL (21.22 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
The respective human recombinant HDAC enzymes are incubated in absence and/or in presence of various concentrations RGFP966 and a pro-fluorogenic substrate at room temperature for 60 min. Next, the deacetylation reaction is stopped by the addition of the HDAC Stop Solution (6 mg/mL trypsin, 0.3 mM SAHA) in all wells and the plate is incubated at 37°C for 20 min. The release of the fluorescent 7-amino-4-methylcoumarin is monitored by measuring the fluorescence at λem=460 nm and λex=390 nm using a Synergy H1 plate reader. The fluorescence value of the background wells is subtracted from the fluorescence of the positive control, blank and inhibitor wells. Nonlinear regression is used to fit the data to the log(inhibitor) vs. response curve using GraphPad Prism[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
To investigate the influence of the HDAC 3-selective inhibitor RGFP966 on cell viability, RAW 264.7 macrophages, HBE cells and hASM cells are seeded in 96-well plates. To obtain identical cell density at the start of the experiments, RAW 264.7 macrophages are seeded at 25,000 cells/cm2, HBE cells and hASM cells are seeded at 70% confluency (based on surface area) and are serum-starved for 24 h prior incubation with RGFP966. Shortly before incubation with RGFP966, the medium is replaced by 100 μL fresh (if appropriate serum free) culture medium. Incubations with LPS and IFNγ are performed as described for HDAC 1-3 downregulation by siRNA. After 20 h of incubation with RGFP966, 20 μL of CellTiter 96 AQueous One Solution reagent is added to each well and incubated at 37°C for 1 h in the dark. The absorbance at 490 nm is measured using a Synergy H1 plate reader. LPS/IFNγ-stimulated cells without addition of RGFP966 are considered 100%[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[3]
N171-82Q transgenic mice are housed and maintained on a normal 12-h light/dark cycle with lights on at 6:00 a.m and free access to food and water. Mice are administered RGFP966 (10 or 25 mg/kg) for 10 weeks by S.C. injection (3 injections/week) beginning at 8 weeks of age. RGFP966 is dissolved with 75% polyethylene glycol 200/25% sodium acetate (6.25 mM); control mice received an equal volume of drug vehicle. Body weights are recorded twice per week. Mice are sacrificed at 18 weeks of age, 6 h after the final injection by overdose with isofluorane anesthesia. Brains are removed, and striata and cortex dissected out for gene expression assays or intracardially perfused with 4% paraformaldehyde.
Rats[4]
A total of thirty-three adult male Sprague Dawley rats (275-350 g) are used. Immediately following the daily training session, a posttraining systemic injection of either RGPF966 (10 mg/kg, s.c.) or vehicle (at a comparable volume to drug treatment) is delivered to each subject.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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 Feb 12;110(7):2647-52. [Content Brief]
[2]. Leus NG, 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. [Content Brief]
[3]. Jia H, et al. The Effects of Pharmacological Inhibition of Histone Deacetylase 3 (HDAC3) in Huntington's Disease Mice. PLoS One. 2016 Mar 31;11(3):e0152498. [Content Brief]
[4]. Bieszczad KM, et al. Histone Deacetylase Inhibition via RGFP966 Releases the Brakes on Sensory Cortical Plasticity and the Specificity of Memory Formation. J Neurosci. 2015 Sep 23;35(38):13124-32. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMF / DMSO | 1 mM | 2.7594 mL | 13.7969 mL | 27.5938 mL | 68.9845 mL |
| 5 mM | 0.5519 mL | 2.7594 mL | 5.5188 mL | 13.7969 mL | |
| 10 mM | 0.2759 mL | 1.3797 mL | 2.7594 mL | 6.8985 mL | |
| 15 mM | 0.1840 mL | 0.9198 mL | 1.8396 mL | 4.5990 mL | |
| 20 mM | 0.1380 mL | 0.6898 mL | 1.3797 mL | 3.4492 mL | |
| 25 mM | 0.1104 mL | 0.5519 mL | 1.1038 mL | 2.7594 mL | |
| 30 mM | 0.0920 mL | 0.4599 mL | 0.9198 mL | 2.2995 mL | |
| 40 mM | 0.0690 mL | 0.3449 mL | 0.6898 mL | 1.7246 mL | |
| 50 mM | 0.0552 mL | 0.2759 mL | 0.5519 mL | 1.3797 mL | |
| 60 mM | 0.0460 mL | 0.2299 mL | 0.4599 mL | 1.1497 mL | |
| 80 mM | 0.0345 mL | 0.1725 mL | 0.3449 mL | 0.8623 mL | |
| 100 mM | 0.0276 mL | 0.1380 mL | 0.2759 mL | 0.6898 mL |
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