Catalog No.S7229

For research use only.

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

CAS No. 1396841-57-8

Selleck's RGFP966 has been cited by 77 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.
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
APL cells NWXSR21ITnWwY4Tpc44h[XO|YYm= M4PxXwKKrDJizszN MkfyOFghcA>? M4\Rb2ROW09? MnqyVmdHWDl4NjDkbYQhdm:2IHnu[JVk\SCjcH;weI9{cXNiaX6gRXBNKGOnbHzzJIJ2fCCmaXSgdoVlfWOnIHPsc45w\2WwaXPpeJkh[W6mIHnuZ5Jm[XOnZDDtZZR2emG2aX;uMi=> MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjR2N{G5NEc,OjZ2NEexPVA9N2F-
Em-Myc lymphoma cells MX7GeY5kfGmxbjDhd5NigQ>? M{PXXwKKrDFizszN M4ixPVQ5KGh? MWHEUXNQ NWDzOHZUS2WubDDwdo9tcW[ncnH0[YQhe2mpbnnmbYNidnSueTDtc5JmKHOub4fsfUB1cGGwII\lbIlkdGVvdILlZZRm\CClb370do9teyCrbjD0bIUheHKnc3XuZ4Uhd3JiYXLz[Y5k\SCxZjDwdo8ue3W{dnn2ZYwhSkOOLUKgc5ZmemW6cILld5Nqd25? NV;zNWpHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[0OFcyQTBpPkK2OFQ4OTlyPD;hQi=>
HH and Hut78 cells NH\1TW9Rem:uaX\ldoF1cW:wIHHzd4F6 M1P2VVExKM7:TR?= MlrPNEwhOjRuIES4MEA4OiCq M4O0cmROW09? MXHCc5RpKGOnbHygcIlv\XNid3Xy[UB{\W6|aYTpeoUhfG9idILlZZRu\W62IIfpeIghOTBizszNJFk3Pi5iSH;3[ZZmeixiSIX0O|gh[2WubIOg[ZhpcWKrdHXkJIEh\3KnYYTldkB{\W6|aYTpeol1gSC2aHHuJGhJKGOnbHzzMi=> M2X3XFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OEm0N|c1Lz5{M{i5OFM4PDxxYU6=
HH M3XRbGZ2dmO2aX;uJIF{e2G7 MoHnNVAh|ryP MlTzNlQhcA>? MVzEUXNQ M{DWc4lv[3KnYYPld{B1cGViYXPleJlt[XSrb36gZZQhUDONOT;LNVQtKEh|S{K3MEBidmRiSETLOS=> MmnJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6OUSzO|QoRjJ|OEm0N|c1RC:jPh?=
Hut78 NYO2flY3TnWwY4Tpc44h[XO|YYm= NIWyO4UyOCEQvF2= NF25Z3czPCCq NWPoSpp3TE2VTx?= MUTpcoNz\WG|ZYOgeIhmKGGlZYT5cIF1cW:wIHH0JGg{UzlxS{G0MEBJO0t{NzygZY5lKEh2S{W= M{PSN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OEm0N|c1Lz5{M{i5OFM4PDxxYU6=
HL60 Mo[4RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MnnQOFghcHK| M3vtT2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFy2NEBk\WyuczDh[pRmeiB2ODDodpMhcW5icILld4Vv[2Vib3[gTmFMOiCrbnjpZol1d3JiQ2nUMVM5PyCkeTDDR2suQCCjc4PhfUwhUUN3MDC9JFEvPjRizszNMi=> NHXJV4E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUm0NFEyPSd-Mkm5OFAyOTV:L3G+
K562 M{jzWWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MkjIOFghcHK| NYrWV4RLSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLOVYzKGOnbHzzJIFnfGW{IES4JIhzeyCrbjDwdoV{\W6lZTDv[kBLSUt{IHnubIljcXSxcjDDXXQuOzh5IHL5JGNEUy16IHHzd4F6NCCLQ{WwJF0hOS54NDFOwG0v MlXHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl7NECxNVUoRjJ7OUSwNVE2RC:jPh?=
HEL MUjBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NGToRos1QCCqcoO= M3njU2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFXMJINmdGy|IHHmeIVzKDR6IHjyd{BqdiCycnXz[Y5k\SCxZjDKRWszKGmwaHnibZRweiCFWWStN|g4KGK7IFPDT{05KGG|c3H5MEBKSzVyIE2gNU43PCEQvF2u M3XYVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7OUSwNVE2Lz5{OUm0NFEyPTxxYU6=
HL60 MlTQRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? Mn7yOFghcHK| MYHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiONkCgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KEOFSz24JIF{e2G7LDDJR|UxKD1iMkGuO|Eh|ryPLh?= NIr4R|g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUm0NFEyPSd-Mkm5OFAyOTV:L3G+
K562 NU[0PWs2SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M16zNFQ5KGi{cx?= NFzObZNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFu1OlIh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IFPDT{05KGG|c3H5MEBKSzVyIE2gNlEvPzFizszNMi=> MlmxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl7NECxNVUoRjJ7OUSwNVE2RC:jPh?=
HEL NHjjSYpCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NXL3d2xnPDhiaILz MmrxRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKRVygZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KEOFSz24JIF{e2G7LDDJR|UxKD1iMkGuO|Eh|ryPLh?= M3PkTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7OUSwNVE2Lz5{OUm0NFEyPTxxYU6=
Sf9 M2\1eGZ2dmO2aX;uJIF{e2G7 NWTtN5lKPjBibXnudy=> M{HzeGlvcGmkaYTpc44hd2ZiZoXscEBt\W6pdHigbJVu[W5iQz30[ZJucW6jbDDIbZMufGGpZ3XkJGhFSUN|L16teIVzdWmwYXygS3NVNXSjZ3fl[EBPS0:UMjCoN|k2KHSxIES4PUBz\XOrZIXld{kh\XiycnXzd4VlKGmwIHLhZ5Vtd3[rcoXzJIlv\mWldHXkJHNnQSCrboPlZ5Qh[2WubIOgeZNqdmdic4Xid5Rz[XSnIH3lZZN2emWmIHHmeIVzKDZyIH3pcpMh[nliY3;sc5JqdWW2cnnjJI1mfGixZB?= MnPjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl3NEGzO|IoRjJ7NUSxN|czRC:jPh?=
Methods Test Index PMID
Western blot p-STAT3 / Acetyl-STAT3 / STAT3 / Ac-H3 / Ac-H4 ; H3K9K14ac / H3 / H3K56ac / H3K27ac / H4K5ac 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 (from reference)

Kinase Assay:[1]
  • 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]
  • 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.
Animal Research:[1]
  • Animal Models: Mouse
  • Dosages: 10 mg/kg, 10.0 mL/kg
  • Administration: s.c.

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):
For best results, use promptly after mixing.


Chemical Information

Molecular Weight 362.4


CAS No. 1396841-57-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC=C(C=C1)C=CCN2C=C(C=N2)C=CC(=O)NC3=C(C=C(C=C3)F)N

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Frequently Asked Questions

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

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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