RGFP966

RGFP966 is an HDAC3 inhibitor with IC50 of 0.08 μM in cell-free assay, exhibits > 200-fold selectivity over other HDAC.

RGFP966 Chemical Structure

RGFP966 Chemical Structure

CAS: 1396841-57-8

Selleck's RGFP966 has been cited by 101 publications

Purity & Quality Control

Batch: Purity: 99.74%
99.74

Products often used together with RGFP966

Tubastatin A


RGFP966 and Tubastatin A decrease total HDAC activity in HLMVEC and reduce the inflammatory and hyper-permeability response to LPS in mice.

Birmpas C, et al. The FASEB Journal 29 (2015): 411-4.

(+)-JQ1


RGFP966 and JQ1 dramatically reduces tumor volume and growth rate and suppresses tumor growth via induction of apoptosis in the glioma xenograft mouse model.

Wang Q, et al. Mol Cancer Ther. 2020 Dec;19(12):2542-2553.

Osimertinib (AZD9291)


RGFP966 and Osimertinib induce apoptosis and upregulate active BIM in PC-9BIMi2−/− cells.

Tanimoto A, et al. Clin Cancer Res. 2017 Jun 15;23(12):3139-3149.

TSA (Trichostatin A)


RGFP966 and Trichostatin A increases the expression of AKAP12 at both the mRNA and protein levels.

He P, et al. Int J Oncol. 2018 Apr;52(4):1305-1316.

Romidepsin


Romidepsin induces cell death more strongly than RGFP966 in UCC VM-CUB1 and UM-UC-3 cells.

Hoffmann MJ, et al. Genes (Basel). 2021 Feb 11;12(2):260.

RGFP966 Related Products

Signaling Pathway

Choose Selective HDAC Inhibitors

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
APL cells Function assay ≤2 μM 48 h DMSO RGFP966 did not induce apoptosis in APL cells but did reduce clonogenicity and increased maturation. 26447190
Em-Myc lymphoma cells Function assay ≤1 μM 48 h DMSO Cell proliferated significantly more slowly than vehicle-treated controls in the presence or absence of pro-survival BCL-2 overexpression 26447190
HH and Hut78 cells Proliferation assay 10 μM 0, 24, 48, 72 h DMSO Both cell lines were sensitive to treatment with 10 μM 966. However, Hut78 cells exhibited a greater sensitivity than HH cells. 23894374
HH Function assay 10 μM 24 h DMSO increases the acetylation at H3K9/K14, H3K27, and H4K5 23894374
Hut78 Function assay 10 μM 24 h DMSO increases the acetylation at H3K9/K14, H3K27, and H4K5 23894374
HL60 Antiproliferative assay 48 hrs Antiproliferative activity against human HL60 cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay, IC50 = 1.64 μM. 29940115
K562 Antiproliferative assay 48 hrs Antiproliferative activity against human K562 cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay, IC50 = 1.64 μM. 29940115
HEL Antiproliferative assay 48 hrs Antiproliferative activity against human HEL cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay, IC50 = 1.64 μM. 29940115
HL60 Antiproliferative assay 48 hrs Antiproliferative activity against human HL60 cells after 48 hrs by CCK-8 assay, IC50 = 21.71 μM. 29940115
K562 Antiproliferative assay 48 hrs Antiproliferative activity against human K562 cells after 48 hrs by CCK-8 assay, IC50 = 21.71 μM. 29940115
HEL Antiproliferative assay 48 hrs Antiproliferative activity against human HEL cells after 48 hrs by CCK-8 assay, IC50 = 21.71 μM. 29940115
Sf9 Function assay 60 mins Inhibition of full length human C-terminal His-tagged HDAC3/N-terminal GST-tagged NCOR2 (395 to 489 residues) expressed in baculovirus infected Sf9 insect cells using substrate measured after 60 mins by colorimetric method 29541372
Click to View More Cell Line Experimental Data

Biological Activity

Description RGFP966 is an HDAC3 inhibitor with IC50 of 0.08 μM in cell-free assay, exhibits > 200-fold selectivity over other HDAC.
Targets
HDAC3 [1]
(Cell-free assay)
80 nM
In vitro
In vitro RGFP966 is a slow-on/slow-off, competitive tight-binding HDAC inhibitor, with an IC50 of 0.08μM for HDAC3 and no effective inhibition of any other HDAC at concentrations up to 15μM. [1] RGFP966 treatment on two CTCL cell lines for 24 hours prior to western blot analysis resulted in increased acetylation at H3K9/K14, H3K27, and H4K5, but not H3K56ac. RGFP966 decreases cell growth in CTCL (cutaneous T cell lymphoma) cell lines due to increased apoptosis that is associated with DNA damage and impaired S phase progression. RGFP966 causes a significant reduction in DNA replication fork velocity within the first hour of drug treatment. [2]
Kinase Assay Deacetylation assays
Deacetylation assays are based on the homogenous fluorescence release assay. Purified recombinant enzymes are incubated with serial-diluted inhibitors at the concentrations indicated in the figures, with pre-incubation times ranging from 0 to 3 hours, in the standard HDAC buffer. Acetyl-Lys(Ac)-AMC substrate (at 10 μM, corresponding to the Km for both HDAC1 and HDAC3) is added after the pre-incubation period. The reaction is allowed to run for 1 hour. The trypsin peptidase developer, at final concentration of 5mg/ml, is added after 1 hour, and the fluorescence emission is then measured using a Tecan M200 96-well plate reader.
Cell Research Cell lines HH and Hut78 CTCL cell lines
Concentrations ~10μM
Incubation Time 24 to 72 h
Method Cells are counted and split into T25 (Corning) flasks at 26105 cells/mL. Cells are then treated with DMSO, or HDIs once at hour 0. 100 ml aliquots are taken in triplicate from each flask at 0 hr, 24 hrs, 48 hrs, and 72 hrs after treatment, distributed into a flat bottom 96-well plate, and 10 ml of alamar blue added to each well. After a 4 hr incubation, fluorescence is measured using the Biotek Synergy MX Microplate Reader.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-STAT3 / Acetyl-STAT3 / STAT3 / Ac-H3 / Ac-H4 H3K9K14ac / H3 / H3K56ac / H3K27ac / H4K5ac 28338101
In Vivo
In vivo RGFP966 treatment (10 mg/kg) enhances long-term memory for object memory. RGFP966 (3 or 10 mg/kg, s.c.) facilitates extinction and prevents reinstatement of cocaine- conditioned place preference. [1]
Animal Research Animal Models Mouse
Dosages 10 mg/kg, 10.0 mL/kg
Administration s.c.

Chemical Information & Solubility

Molecular Weight 362.4 Formula

C21H19FN4O

CAS No. 1396841-57-8 SDF Download RGFP966 SDF
Smiles C1=CC=C(C=C1)C=CCN2C=C(C=N2)C=CC(=O)NC3=C(C=C(C=C3)F)N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 72 mg/mL ( (198.67 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

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.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.

Frequently Asked Questions

Question 1:
Does this product S7229 specifically inhibit HDAC3? Or does it target other HDACs as well?

Answer:
In the paper, it is indicated that "RGFP966 is specific for HDAC3, with an IC50 of 0.08 μM and no effective inhibition of any other HDAC at concentrations up to 15 μM. ". However, we did not preform experiment to confirm this data. Please refer to the following link for detailed information: http://www.pnas.org/content/110/7/2647.long

Tags: buy RGFP966|RGFP966 ic50|RGFP966 price|RGFP966 cost|RGFP966 solubility dmso|RGFP966 purchase|RGFP966 manufacturer|RGFP966 research buy|RGFP966 order|RGFP966 mouse|RGFP966 chemical structure|RGFP966 mw|RGFP966 molecular weight|RGFP966 datasheet|RGFP966 supplier|RGFP966 in vitro|RGFP966 cell line|RGFP966 concentration|RGFP966 nmr|RGFP966 in vivo|RGFP966 clinical trial|RGFP966 inhibitor|RGFP966 Epigenetics inhibitor