RGFP966

Catalog No.S7229

RGFP966 Chemical Structure

Molecular Weight(MW): 362.4

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

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Cited by 23 Publications

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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

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Em-Myc lymphoma cells MVHGeY5kfGmxbjDhd5NigQ>? MlHO5qmlOSEQvF2= MkD6OFghcA>? MonKSG1UVw>? MonBR4VtdCCycn;sbYZmemG2ZXSgd4lodmmoaXPhcpRtgSCvb4LlJJNtd3eueTD0bIFvKH[naHnjcIUufHKnYYTl[EBkd262cn;sd{BqdiC2aHWgdJJme2WwY3Wgc5Ih[WK|ZX7j[UBw\iCycn:td5Vzfmm4YXygRmNNNTJib4\ldoV5eHKnc4Ppc44> NVXsZVAzOjZ2NEexPVA>
APL cells NWi3W205TnWwY4Tpc44h[XO|YYm= NXm4UVUx6onmMjFOwG0> M4fkUFQ5KGh? MVPEUXNQ M2fBXHJITlB7Nk[g[IllKG6xdDDpcoR2[2ViYYDvdJRwe2m|IHnuJGFRVCClZXzsd{BjfXRiZHnkJJJm\HWlZTDjcI9vd2enbnnjbZR6KGGwZDDpcoNz\WG|ZXSgcYF1fXKjdHnvck4> Mmm0NlY1PDdzOUC=
HH and Hut78 cells NVjJT2FbWHKxbHnm[ZJifGmxbjDhd5NigQ>? M2nUcVExKM7:TR?= NXnCVpRtOCxiMkSsJFQ5NCB5MjDo NEnPcmlFVVOR NFHqXVBDd3SqIHPlcIwhdGmwZYOge4Vz\SC|ZX7zbZRqfmVidH:geJJm[XSvZX70JJdqfGhiMUCg{txOKDl4Nj6gTI94\X[ncjygTJV1PzhiY3XscJMh\XiqaXLpeIVlKGFiZ4LlZZRmeiC|ZX7zbZRqfmm2eTD0bIFvKEiKIHPlcIx{Ng>? NHyxbWEzOzh7NEO3OC=>
HH M1vxe2Z2dmO2aX;uJIF{e2G7 NV64WJRmOTBizszN NYWzZVdNOjRiaB?= NYjz[GNuTE2VTx?= NHT5VmNqdmO{ZXHz[ZMhfGinIHHj[ZR6dGG2aX;uJIF1KEh|S{mvT|E1NCCKM1uyO{wh[W6mIFi0T|U> NXrZenlTOjN6OUSzO|Q>
Hut78 MYDGeY5kfGmxbjDhd5NigQ>? NUP5[GJROTBizszN NGP4TXUzPCCq M4XIUWROW09? MYLpcoNz\WG|ZYOgeIhmKGGlZYT5cIF1cW:wIHH0JGg{UzlxS{G0MEBJO0t{NzygZY5lKEh2S{W= MYOyN|g6PDN5NB?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-STAT3 / Acetyl-STAT3 / STAT3 / Ac-H3 / Ac-H4; 

PubMed: 28338101     


NK cells were treated with Entinostat, VPA and RGFP966. Phosphorylation, acetylation and total protein of STAT3 and acetylated histone H3/H4 were detected by western-blot. 

H3K9K14ac / H3 / H3K56ac / H3K27ac / H4K5ac; 

PubMed: 23894374     


Western blot analysis of Hut78 cell lines treated with DMSO, 10 nM Depsipeptide (Depsi), 10 µM 233, 10 µM 136, or 10 µM 966. Cells were treated for 24 hr and then harvested for protein isolation. Samples were run on the same gel and probed on the same mem䲧疝Ỵ疞㧀疜膉痘 瘿삨ՂᾰƌՂĀ 㺣痖帉痖Ѐ瑖堘𢡄빢᎒ՂĀ鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙圭堙𢡄玚Wᾰƌ ᾰƌ戤瘯Ɖ�෋䐺痖暼瘿�෋ᾰƌ �෋Ð㺣

28338101 23894374
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]

Protocol

Kinase Assay:[1]
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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:[2]
+ Expand
  • 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.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: Mouse
  • Formulation: dissolved in DMSO and diluted in a vehicle of 30% (wt/vol) hydroxypropyl-β-cyclodextrin and 100mM sodium acetate (pH 5.4).
  • Dosages: 10 mg/kg, 10.0 mL/kg
  • Administration: s.c.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 72 mg/mL (198.67 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5%DMSO+40%PEG300+10%Tween80+45%ddH2O
For best results, use promptly after mixing.
6.5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 362.4
Formula

C21H19FN4O

CAS No. 1396841-57-8
Storage powder
in solvent
Synonyms N/A

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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

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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID