GSK J4 HCl (GSKJ4 HCl)

Catalog No.S7070

For research use only.

GSK J4 HCl is a cell permeable prodrug of GSK J1, which is the first selective inhibitor of the H3K27 histone demethylase JMJD3 and UTX with IC50 of 60 nM in a cell-free assay and inactive against a panel of demethylases of the JMJ family.

GSK J4 HCl (GSKJ4 HCl) Chemical Structure

CAS No. 1797983-09-5

Selleck's GSK J4 HCl (GSKJ4 HCl) has been cited by 47 publications

Purity & Quality Control

Choose Selective Histone Demethylase Inhibitors

Biological Activity

Description GSK J4 HCl is a cell permeable prodrug of GSK J1, which is the first selective inhibitor of the H3K27 histone demethylase JMJD3 and UTX with IC50 of 60 nM in a cell-free assay and inactive against a panel of demethylases of the JMJ family.
Targets
JMJD3 [1]
(Cell-free assay)
60 nM
In vitro

GSK J4 HCl is an ethyl ester derivative of the JMJD3 selective histone demethylase inhibitor GSK-J1 with an IC50 value greater than 50 μM in vitro. GSK J4 HCl is used to probe the consequences of demethylation of H3K27me3. In human primary macrophages, GSK-J4 inhibits the lipopolysaccharide-induced production of cytokines, including pro-inflammatory tumour necrosis factor (TNF). In addition, GSK-J4 prevents the lipopolysaccharide-induced loss of H3K27me3 associated with the TNF transcription start sites and blocked the recruitment of RNA polymerase II. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CUTLL1 MXnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MmHkNkDPxE1? MmTOSG1UVw>? M2HoXIFn\mWldIOgZ4VtdCCpcn;3eIg> MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTF|MkW0PUc,OjVzM{K1OFk9N2F-
CUTLL1 NFGz[FZCeG:ydH;zbZMh[XO|YYm= M1:1bVIh|ryP MV3EUXNQ NHjuPJdqdmS3Y3XzJIFxd3C2b4Ppdy=> NHLiWok9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUGzNlU1QSd-MkWxN|I2PDl:L3G+
CUTLL1 M1rZdmZ2dmO2aX;uJIF{e2G7 NHLrXoQzKM7:TR?= MnfySG1UVw>? MWTpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 NUjucY51RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWxN|I2PDlpPkK1NVMzPTR7PD;hQi=>
CUTLL1 NFHFd3FMcW6jc3WgZZN{[Xl? MorKOkDPxE1? M2S5VGROW09? MWfs[YFleyC2bzDpcoNz\WG|ZXSgTFNMOjevZUO= MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTF|MkW0PUc,OjVzM{K1OFk9N2F-
SF7761 MUPLbY5ie2ViYYPzZZk> NX\5WXJvPiEQvF2= Ml[5SG1UVw>? NUjvOYhvcW6lcnXhd4V{KEt{NzDt[ZRpgWyjdHnvci=> MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTRyMU[5N{c,OjV2MEG2PVM9N2F-
SF8628 MlKzT4lv[XOnIHHzd4F6 NW\Nb|B{PiEQvF2= NX\ONFNiTE2VTx?= NFHLbmNqdmO{ZXHz[ZMhUzJ6IH3leIh6dGG2aX;u MoPmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV2MEG2PVMoRjJ3NECxOlk{RC:jPh?=
H3.3 NEfnWo9McW6jc3WgZZN{[Xl? MmTXOkDPxE1? M{fIUGROW09? M1vVTolv[3KnYYPld{BMOjlibXX0bJlt[XSrb36= NVWzVmlURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW0NFE3QTNpPkK1OFAyPjl|PD;hQi=>
SF9012 NGjNOWhMcW6jc3WgZZN{[Xl? MXK2JO69VQ>? NW\EdVlkTE2VTx?= M4HDdIlv[3KnYYPld{BMOzBibXX0bJlt[XSrb36= MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTRyMU[5N{c,OjV2MEG2PVM9N2F-
SF9402 M1jGZmtqdmG|ZTDhd5NigQ>? M4nVTVYh|ryP Mnn4SG1UVw>? MkS2bY5kemWjc3XzJGs{OSCvZYTofYxifGmxbh?= MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTRyMU[5N{c,OjV2MEG2PVM9N2F-
SF9427 M3rUPWtqdmG|ZTDhd5NigQ>? MliyOkDPxE1? NIDJZZpFVVOR M2DBTYlv[3KnYYPld{BMOzJibXX0bJlt[XSrb36= M2\VWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NECxOlk{Lz5{NUSwNVY6OzxxYU6=
human astrocytes NW[4PIpOU2mwYYPlJIF{e2G7 MV[2JO69VQ>? MW\EUXNQ MmHPbY5kemWjc3XzJGs{OyCvZYTofYxifGmxbh?= MnPBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV2MEG2PVMoRjJ3NECxOlk{RC:jPh?=
SF7761 NEK4e21Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MmWwOkDPxE1? MXTEUXNQ Ml;mbY5pcWKrdIOgT|I4VSCpbHnvcYEh[2WubDDndo94fGh? MknZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV2MEG2PVMoRjJ3NECxOlk{RC:jPh?=
SF8628 MVPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MUS2JO69VQ>? M1\PXmROW09? NICybG5qdmirYnn0d{BMOjiPIHfsbY9u[SClZXzsJIdzd3e2aB?= MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTRyMU[5N{c,OjV2MEG2PVM9N2F-
H3.3 NXzMe4d4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnLIOkDPxE1? M1TofmROW09? M3roUYlvcGmkaYTzJGszQU1iZ3zpc41iKGOnbHyg[5Jwf3Sq MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTRyMU[5N{c,OjV2MEG2PVM9N2F-
SF9012 NFvuVWhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHPUZYM3KM7:TR?= NUD5T2x7TE2VTx?= NVfjeYlicW6qaXLpeJMhUzNyTTDncIlwdWFiY3XscEBoem:5dHi= NIXJdpY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUSwNVY6Oyd-MkW0NFE3QTN:L3G+
SF9402 Mn\XS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M{\hdlYh|ryP M4\6ZmROW09? MXTpcohq[mm2czDLN|FOKGeuaX;tZUBk\WyuIHfyc5d1cA>? NI\5W2U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUSwNVY6Oyd-MkW0NFE3QTN:L3G+
SF9427 MUfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NUL4Snc3PiEQvF2= MUfEUXNQ NGDWUIJqdmirYnn0d{BMOzKPIHfsbY9u[SClZXzsJIdzd3e2aB?= M4HDbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NECxOlk{Lz5{NUSwNVY6OzxxYU6=
human astrocytes MnHCS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NEPFcVU3KM7:TR?= MWrEUXNQ M2WxfolvcGmkaYTzJGs{O01iZ3zpc41iKGOnbHyg[5Jwf3Sq MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTRyMU[5N{c,OjV2MEG2PVM9N2F-
TG neurons NYDPOFMxTnWwY4Tpc44h[XO|YYm= Mn;UOVAh|ryP MXLEUXNQ NF;3TolqdmirYnn0d{BJW1ZvMTDy[YFkfGm4YYTpc44h\nKxbTDz[Y5{d3K7IH7leZJwdnN? M2\adVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NUWyO|IxLz5{NUW1NlczODxxYU6=
Th17 NHjGfJlHfW6ldHnvckBie3OjeR?= MVK4NEBvVQ>? MUjEUXNQ MlrqbY5pcWKrdIOgZ4VtdCCmaX\m[ZJmdnSrYYTpc44> M1OwWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OESwPVk{Lz5{NUi0NFk6OzxxYU6=
β-cells MUXGeY5kfGmxbjDhd5NigQ>? NVjmb5hLOjBizszN NHnPbXBFVVOR M4O2XIJtfW62czDJSm7PuyxiSXytNe6zNCCjbnSgWG5H|rFvaX7keYNm\CClaHXtc4tqdmViZ3Xu[UBmgHC{ZYPzbY9v MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjVyNUG5N{c,OjZ3MEWxPVM9N2F-
β-cells M4nlOGZ2dmO2aX;uJIF{e2G7 MXKyNEDPxE1? MYTEUXNQ MVjpcoR2[2W|IN8yMYNmdGxiZInz[pVv[3Srb36= NEe3XXU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkWwOVE6Oyd-Mk[1NFUyQTN:L3G+
ESCs MVLGeY5kfGmxbjDhd5NigQ>? MY[xMljjiIYEtV2= NXGybnFDTE2VTx?= NFT0ToRqdmS3Y3XzJGRPSSCmYX3h[4Uh[Wyxbnege4l1cCCjY4TpeoF1cW:wIH;mJJRp\SCGTlGg[IFu[WenIILld5BwdnOn MmTFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ5NUmxO|UoRjJ4N{W5NVc2RC:jPh?=
Raw 264.7 NYrafm5xTnWwY4Tpc44h[XO|YYm= MViwMlgyQTMkgJZCuW0> NEfRdZNFVVOR MmLBbY5pcWKrdIOgWG5HNc7zIIDyc4R2[3Srb36= MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjd5NkO2NEc,OjZ5N{[zOlA9N2F-
MCF7 NHnHfpBHfW6ldHnvckBie3OjeR?= Mlu0NUB1dyBzMDD1US=> M3HoU|MxKGi{cx?= M1\sV2lvcGmkaYTpc44hd2ZiS1TNOWEhcW5iaIXtZY4hVUOINzDj[YxteyCjc4Pld5Nm\CCjczDl[oZm[3Rib36gTFNMPG2nMzDt[ZRpgWyjdHnvckBt\X[nbIOgZZQhOSC2bzCxNEB2VSCjZoTldkA{OCCqcoOgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m| NWXNUmY1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CzPVI{PDlpPkOwN|kzOzR7PD;hQi=>
MCF7 MlLMSpVv[3Srb36gZZN{[Xl? MmTyNUB1dyBzMDD1US=> MmjpN|AhcHK| M4jPVmlvcGmkaYTpc44hd2ZiS1TNOWEhcW5iaIXtZY4hVUOINzDj[YxteyCjc4Pld5Nm\CCjczDl[oZm[3Rib36gTFNMOjevZUOgcYV1cHmuYYTpc44hdGW4ZXzzJIF1KDFidH:gNVAhfU1iYX\0[ZIhOzBiaILzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?= NGTjT4w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEO5NlM1QSd-M{CzPVI{PDl:L3G+
RAW264.7 MnqwNE45OiC3TR?= NHHXSnAzPCCqcoO= MV3Jcohq[mm2aX;uJI9nKEySUz3pcoR2[2WmIGTOSoFteGijIIDyc4R2[3Srb36gbY4hdW:3c3WgVmFYOjZ2LkegZ4VtdHNiMD64NkB2VSCjZoTldkAzPCCqcoOgZpkhTUyLU1G= MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjd5NkO2NEc,OjZ5N{[zOlA9N2F-
RAW264.7 MYqyOEBpenN? MW\Jcohq[mm2aX;uJI9nKEySUz3pcoR2[2WmIGTOSoFteGijIIDyc4R2[3Srb36gbY4hdW:3c3WgVmFYOjZ2LkegZ4VtdHNiYX\0[ZIhOjRiaILzJIJ6KEWOSWPB MlTUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ5N{[zOlAoRjJ4N{e2N|YxRC:jPh?=

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 90 mg/mL warmed
(198.25 mM)
Water 90 mg/mL
(198.25 mM)
Ethanol ''90 mg/mL warmed

Chemical Information

Molecular Weight 453.96
Formula

C24H27N5O2.HCl

CAS No. 1797983-09-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCOC(=O)CCNC1=CC(=NC(=N1)C2=CC=CC=N2)N3CCC4=CC=CC=C4CC3.Cl

In vivo Formulation Calculator (Clear solution)

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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.

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Molarity Calculator

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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:
I cannot get a clear solution when I dissolve the compound into water.

Answer:
S7070 GSK J4 HCl can be dissolved in 2% DMSO/dd H2O at 10 mg/mL as a clear solution. Water cannot dissolve it clear directly.

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