GSK J4 HCl (GSKJ4 HCl)

For research use only.

Catalog No.S7070

37 publications

GSK J4 HCl (GSKJ4 HCl) Chemical Structure

CAS No. 1797983-09-5

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.

Selleck's GSK J4 HCl (GSKJ4 HCl) has been cited by 37 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 NFjT[YRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NH\ISZIzKM7:TR?= NXz2OJRbTE2VTx?= NEjP[3Ni\m[nY4TzJINmdGxiZ4Lve5Rp NGDnfW09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUGzNlU1QSd-MkWxN|I2PDl:L3G+
CUTLL1 MkK5RZBweHSxc3nzJIF{e2G7 NVfke2pyOiEQvF2= MWTEUXNQ M3f6Xolv\HWlZYOgZZBweHSxc3nz MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTF|MkW0PUc,OjVzM{K1OFk9N2F-
CUTLL1 M1jFWGZ2dmO2aX;uJIF{e2G7 M3\FTlIh|ryP M1[5NmROW09? MY\pcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 NYjvfVZRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWxN|I2PDlpPkK1NVMzPTR7PD;hQi=>
CUTLL1 NUHpbpl1U2mwYYPlJIF{e2G7 Mkf5OkDPxE1? NFvxRmlFVVOR MmrvcIVi\HNidH:gbY5kemWjc3XkJGg{UzJ5bXWz NHq2T3I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUGzNlU1QSd-MkWxN|I2PDl:L3G+
SF7761 M{DXU2tqdmG|ZTDhd5NigQ>? MWe2JO69VQ>? MmD3SG1UVw>? NG\I[WNqdmO{ZXHz[ZMhUzJ5IH3leIh6dGG2aX;u NUXGW25FRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW0NFE3QTNpPkK1OFAyPjl|PD;hQi=>
SF8628 Ml\QT4lv[XOnIHHzd4F6 NXPhUlB5PiEQvF2= MVfEUXNQ NWHmVoVLcW6lcnXhd4V{KEt{ODDt[ZRpgWyjdHnvci=> M363blxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NECxOlk{Lz5{NUSwNVY6OzxxYU6=
H3.3 MX7LbY5ie2ViYYPzZZk> MUC2JO69VQ>? NYrtSJZ5TE2VTx?= MYTpcoNz\WG|ZYOgT|I6KG2ndHj5cIF1cW:w NFrhdnA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUSwNVY6Oyd-MkW0NFE3QTN:L3G+
SF9012 Ml\pT4lv[XOnIHHzd4F6 MYG2JO69VQ>? Mn\4SG1UVw>? NFvUOWpqdmO{ZXHz[ZMhUzNyIH3leIh6dGG2aX;u NW\zeWhERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW0NFE3QTNpPkK1OFAyPjl|PD;hQi=>
SF9402 M13k[2tqdmG|ZTDhd5NigQ>? NIDve4E3KM7:TR?= M3;KVGROW09? NFflSFRqdmO{ZXHz[ZMhUzNzIH3leIh6dGG2aX;u NWflTlBFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW0NFE3QTNpPkK1OFAyPjl|PD;hQi=>
SF9427 MUDLbY5ie2ViYYPzZZk> NVXiZ41NPiEQvF2= NXvQdYp3TE2VTx?= MnS5bY5kemWjc3XzJGs{OiCvZYTofYxifGmxbh?= MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTRyMU[5N{c,OjV2MEG2PVM9N2F-
human astrocytes NU\VVJVqU2mwYYPlJIF{e2G7 MlfEOkDPxE1? NHTpU2dFVVOR NYnkSmZvcW6lcnXhd4V{KEt|MzDt[ZRpgWyjdHnvci=> MlHFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV2MEG2PVMoRjJ3NECxOlk{RC:jPh?=
SF7761 MUPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MUS2JO69VQ>? MWTEUXNQ M{T4c4lvcGmkaYTzJGszP01iZ3zpc41iKGOnbHyg[5Jwf3Sq NFjUNWE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUSwNVY6Oyd-MkW0NFE3QTN:L3G+
SF8628 NXPtVJB1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NEfTZlE3KM7:TR?= NHriTppFVVOR NFvWXGRqdmirYnn0d{BMOjiPIHfsbY9u[SClZXzsJIdzd3e2aB?= Mn\nQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV2MEG2PVMoRjJ3NECxOlk{RC:jPh?=
H3.3 M3\yZmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mk[zOkDPxE1? NUniSJQzTE2VTx?= MVrpcohq[mm2czDLNllOKGeuaX;tZUBk\WyuIHfyc5d1cA>? M2q2bVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NECxOlk{Lz5{NUSwNVY6OzxxYU6=
SF9012 NYe4VXZHT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYLpXGZDPiEQvF2= MVzEUXNQ NHO2cYpqdmirYnn0d{BMOzCPIHfsbY9u[SClZXzsJIdzd3e2aB?= MnS3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV2MEG2PVMoRjJ3NECxOlk{RC:jPh?=
SF9402 MmqyS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYG2JO69VQ>? NV3pRXBpTE2VTx?= MX7pcohq[mm2czDLN|FOKGeuaX;tZUBk\WyuIHfyc5d1cA>? M4LOSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NECxOlk{Lz5{NUSwNVY6OzxxYU6=
SF9427 MXjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWfTO5U3PiEQvF2= M{LiSmROW09? NHPkWlBqdmirYnn0d{BMOzKPIHfsbY9u[SClZXzsJIdzd3e2aB?= MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTRyMU[5N{c,OjV2MEG2PVM9N2F-
human astrocytes M2TVRWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlrOOkDPxE1? NXzpcmh1TE2VTx?= M371eYlvcGmkaYTzJGs{O01iZ3zpc41iKGOnbHyg[5Jwf3Sq MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTRyMU[5N{c,OjV2MEG2PVM9N2F-
TG neurons NGjBWItHfW6ldHnvckBie3OjeR?= NV3wUpJEPTBizszN MXXEUXNQ MXPpcohq[mm2czDIV3YuOSC{ZXHjeIl3[XSrb36g[pJwdSC|ZX7zc5J6KG6ndYLvcpM> M4rNWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NUWyO|IxLz5{NUW1NlczODxxYU6=
Th17 NEOySVNHfW6ldHnvckBie3OjeR?= M2nOfFgxKG6P M4fK[GROW09? MYXpcohq[mm2czDj[YxtKGSrZn\ldoVvfGmjdHnvci=> MmfQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6NEC5PVMoRjJ3OESwPVk{RC:jPh?=
β-cells NEXhPJRHfW6ldHnvckBie3OjeR?= NV\2XFV6OjBizszN MnrpSG1UVw>? NYDMO4J{[my3boTzJGlHVs7|LDDJcE0y|rJuIHHu[EBVVkcQsT3pcoR2[2WmIHPo[Y1wc2mwZTDn[Y5mKGW6cILld5Nqd25? NVG5WY1lRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[1NFUyQTNpPkK2OVA2OTl|PD;hQi=>
β-cells MkfzSpVv[3Srb36gZZN{[Xl? MlnoNlAh|ryP Ml:wSG1UVw>? NXviW5BxcW6mdXPld{DPui2lZXzsJIR6e2[3bnP0bY9v M2jUTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NUC1NVk{Lz5{NkWwOVE6OzxxYU6=
ESCs NXizW4MyTnWwY4Tpc44h[XO|YYm= MlXVNU456oDHwsXN M3[zTWROW09? Ml7ubY5lfWOnczDEUmEh\GGvYXflJIFtd26pIIfpeIgh[WO2aY\heIlwdiCxZjD0bIUhTE6DIHThcYFo\SC{ZYPwc45{\Q>? M13Zb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4N{W5NVc2Lz5{Nke1PVE4PTxxYU6=
Raw 264.7 NHG1WYJHfW6ldHnvckBie3OjeR?= MU[wMlgyQTMkgJZCuW0> MX7EUXNQ NGrtclJqdmirYnn0d{BVVkZvzsGgdJJw\HWldHnvci=> NUXLTXFuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[3O|Y{PjBpPkK2O|c3OzZyPD;hQi=>
MCF7 M{fVNGZ2dmO2aX;uJIF{e2G7 M{PuUlEhfG9iMUCgeW0> NYi5Z5dKOzBiaILz NXLRTVBKUW6qaXLpeIlwdiCxZjDLSG02SSCrbjDoeY1idiCPQ1[3JINmdGy|IHHzd4V{e2WmIHHzJIVn\mWldDDvckBJO0t2bXWzJI1mfGi7bHH0bY9vKGyndnXsd{BifCBzIITvJFExKHWPIHHmeIVzKDNyIHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= Mm\vQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB|OUKzOFkoRjNyM{myN|Q6RC:jPh?=
MCF7 MmTNSpVv[3Srb36gZZN{[Xl? NEnKXVQyKHSxIEGwJJVO MWSzNEBpenN? NIX0RXJKdmirYnn0bY9vKG:oIFvEUVVCKGmwIHj1cYFvKE2FRkegZ4VtdHNiYYPz[ZN{\WRiYYOg[YZn\WO2IH;uJGg{UzJ5bXWzJI1mfGi7bHH0bY9vKGyndnXsd{BifCBzIITvJFExKHWPIHHmeIVzKDNyIHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= M{CzTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{myN|Q6Lz5|MEO5NlM1QTxxYU6=
RAW264.7 MmnPNE45OiC3TR?= NIjOVVkzPCCqcoO= MY\Jcohq[mm2aX;uJI9nKEySUz3pcoR2[2WmIGTOSoFteGijIIDyc4R2[3Srb36gbY4hdW:3c3WgVmFYOjZ2LkegZ4VtdHNiMD64NkB2VSCjZoTldkAzPCCqcoOgZpkhTUyLU1G= MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjd5NkO2NEc,OjZ5N{[zOlA9N2F-
RAW264.7 MXGyOEBpenN? NEfBbIdKdmirYnn0bY9vKG:oIFzQV{1qdmS3Y3XkJHRPTmGucHjhJJBzd2S3Y4Tpc44hcW5ibX;1d4UhWkGZMk[0Mlch[2WubIOgZYZ1\XJiMkSgbJJ{KGK7IFXMTXNC MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjd5NkO2NEc,OjZ5N{[zOlA9N2F-

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Protocol

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

* 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 453.96
Formula

C24H27N5O2.HCl

CAS No. 1797983-09-5
Storage powder
in solvent
Synonyms N/A
Smiles CCOC(=O)CCNC1=CC(=NC(=N1)C2=CC=CC=N2)N3CCC4=CC=CC=C4CC3.Cl

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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.

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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.

Histone Demethylase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID