Art. -Nr.: HY-13909

RGFP966

54 Cited Publications

Kundenbewertung

Based on 54 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).

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Reinheit: 99.81%
CAS. Nr.: 1357389-11-7
Formel: C₂₁H₁₉FN₄O
Molecular Weight:362.40

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

RGFP966 Chemical Structure

CAS. Nr.: 1357389-11-7

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (54)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

HDAC3

80 nM (IC₅₀)

Alle HDAC Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HEL	IC₅₀	1.64 μM Compound: 29; RGFP966	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	[PMID: 29940115]
HEL	IC₅₀	21.71 μM Compound: 29; RGFP966	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	[PMID: 29940115]
HL-60	IC₅₀	1.64 μM Compound: 29; RGFP966	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	[PMID: 29940115]
HL-60	IC₅₀	21.71 μM Compound: 29; RGFP966	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	[PMID: 29940115]
K562	IC₅₀	1.64 μM Compound: 29; RGFP966	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	[PMID: 29940115]
K562	IC₅₀	21.71 μM Compound: 29; RGFP966	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	[PMID: 29940115]

In Vitro

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.

In Vivo

RGFP966 (10 and 25 mg/kg) treatment significantly improves body weight, rotarod performance and several measures of motor function in the open field locomoter test^[3]. RGFP966 at a 10 mg/kg dose penetrates the blood-brain barrier into rat auditory cortex with typical pharmacokinetics, which together establish feasibility for the modulation of A1 plasticity due to action in the auditory cortex^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 1357389-11-7
Appearance Solid
Molecular Weight 362.40
Formel C₂₁H₁₉FN₄O
Color White to off-white
SMILES

O=C(NC1=CC=C(F)C=C1N)/C=C/C2=CN(C/C=C/C3=CC=CC=C3)N=C2
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (54)

All WBIn Vivo ImagingIFIPIHC

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Journal Impact Factor

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
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.
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
Cell Death Differ

NKAP acts with HDAC3 to prevent R-loop associated genome instability. [Abstract]

2023 Jul;30(7):1811-1828. PMID: 37322264
Autophagy

Deacetylation of ATG16L1 is required for LC3-associated lysosomal microautophagy. [Abstract]

2025 Aug 28:1-15. PMID: 40851277
Adv Sci (Weinh)

The Probiotic Parabacteroides johnsonii Ameliorates Metabolic Disorders Through Promoting BCAAs to BSCFAs Conversion. [Abstract]

2025 Aug 7:e02624. PMID: 40772426
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
Nucleic Acids Res

ATXN3 controls DNA replication and transcription by regulating chromatin structure. [Abstract]

2023 Jun 23;51(11):5396-5413. PMID: 36971114
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.
Redox Biol

Methylation reader MBD2-mediated GPX4 transcriptional repression drives ovarian granulosa cell ferroptosis in PCOS. [Abstract]

2026 Mar:90:104034. PMID: 41576700
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

Modeling high-risk Wilms tumors enables the discovery of therapeutic vulnerability. [Abstract]

2024 Sep 27:101770. PMID: 39368485
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
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).
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 Mar 19;9(4):423. PMID: 29555935
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.
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
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
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
Clin Transl Med

DNTTIP1 drives leukaemogenesis through MiDAC-mediated epigenetic silencing of BMF. [Abstract]

2026 Feb;16(2):e70603. PMID: 41603084
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
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
Food Biosci

2024 Dec.
J Bone Miner Res

Hdac3-deficiency increases senescence-associated distention of satellite DNA and telomere-associated foci in osteoprogenitor cells. [Abstract]

2024 Jun 6:zjae085. PMID: 38843356
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
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
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
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
mBio

Desaminotyrosine promotes tuft cell expansion and integrates intestinal type 2 immunity. [Abstract]

2026 Feb 11;17(2):e0328925. PMID: 41575215
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
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
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
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
J Mol Med (Berl)

Combination of PARP inhibitor and temozolomide to suppress chordoma progression. [Abstract]

2019 Aug;97(8):1183-1193. PMID: 31201471
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
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
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
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
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.
Pancreatology

HDAC3 modulates cancer immunity via increasing PD-L1 expression in pancreatic cancer. [Abstract]

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.
bioRxiv

2026 Jun 5.
Res Sq

2026 Apr 30.
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
Research Square Print

2023 Feb 7.
bioRxiv

May 10, 2022.
Patent

US20180263995A1.

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.90 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working 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.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 7.69 mg/mL (21.22 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protokoll

Kinase Assay^[2]

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 λ_em=460 nm and λ_ex=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.

Cell Assay^[2]

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 AQ_ueous 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.

Animal Administration^[3]^[4]

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.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

RGFP966

54 Cited Publications

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RGFP966

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

CNS-Penetrant Compound Library

Anti-Aging Compound Library

Covalent Screening Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

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