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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  • A, 5×106 HeLa, A549, 293T, and H1299 cells were seeded in 10-cm cell culture dishes on day 0 and treated with dimethyl sulfoxide, 10 μM CI994, or 1 μM RGFP966 for 12 h. Cell lysates were collected for Western blotting analysis of Apaf-1 and β-actin.

    J Biol Chem, 2016, 291(14):7386-95.. RGFP966 purchased from Selleck.

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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
HH  MlzOSpVv[3Srb36gRZN{[Xl? MV6xNEDDvU1? MWCyOEBp NFHBNGRFVVOR MYjpcoNz\WG|ZYOgeIhmKGGlZYT5cIF1cW:wIHH0JGg{UzlxS{G0MEBJO0t{NzygZY5lKEh2S{W= NYnDT3ZKOjN6OUSzO|Q>
Hut78  Ml6xSpVv[3Srb36gRZN{[Xl? Mnn0NVAhyrWP NX\me3J3OjRiaB?= M1yw[GROW09? NYX4bJR1cW6lcnXhd4V{KHSqZTDhZ4V1gWyjdHnvckBifCCKM1u5M2syPCxiSEPLNlctKGGwZDDIOGs2 NFX1OoIzOzh7NEO3OC=>

... Click to View More Cell Line Experimental Data

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]
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  • 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 <1 mg/mL
Ethanol <1 mg/mL
In vivo 1% DMSO+30% polyethylene glycol+1% Tween 80 30 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID