GSK J4 HCl (GSKJ4 HCl)

For research use only.

Catalog No.S7070

35 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.

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Selleck's GSK J4 HCl (GSKJ4 HCl) has been cited by 35 publications

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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 NXzpNFhwT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NUTm[ZpsOiEQvF2= MYnEUXNQ NEjuXmxi\m[nY4TzJINmdGxiZ4Lve5Rp MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTF|MkW0PUc,OjVzM{K1OFk9N2F-
CUTLL1 MnPRRZBweHSxc3nzJIF{e2G7 M16x[FIh|ryP M33LPGROW09? NULY[3JYcW6mdXPld{BieG:ydH;zbZM> NEPCUHA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUGzNlU1QSd-MkWxN|I2PDl:L3G+
CUTLL1 NEPIbopHfW6ldHnvckBie3OjeR?= MmDCNkDPxE1? MofPSG1UVw>? M4f0OIlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= M{TNW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MUOyOVQ6Lz5{NUGzNlU1QTxxYU6=
CUTLL1 MVnLbY5ie2ViYYPzZZk> MV[2JO69VQ>? NWLlU2lUTE2VTx?= MkjNcIVi\HNidH:gbY5kemWjc3XkJGg{UzJ5bXWz MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTF|MkW0PUc,OjVzM{K1OFk9N2F-
SF7761 NWDRfnE4U2mwYYPlJIF{e2G7 NX7R[ZN3PiEQvF2= M1LHe2ROW09? NWXTPINncW6lcnXhd4V{KEt{NzDt[ZRpgWyjdHnvci=> NETmO4I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUSwNVY6Oyd-MkW0NFE3QTN:L3G+
SF8628 NVzBU|NNU2mwYYPlJIF{e2G7 M1HCT|Yh|ryP NF7INY5FVVOR M33nRolv[3KnYYPld{BMOjhibXX0bJlt[XSrb36= MmPYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV2MEG2PVMoRjJ3NECxOlk{RC:jPh?=
H3.3 NFTsU41McW6jc3WgZZN{[Xl? MX22JO69VQ>? NH;tWoFFVVOR MVzpcoNz\WG|ZYOgT|I6KG2ndHj5cIF1cW:w M2jTNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NECxOlk{Lz5{NUSwNVY6OzxxYU6=
SF9012 M4HaTWtqdmG|ZTDhd5NigQ>? NIKy[4o3KM7:TR?= M36yUGROW09? MoO3bY5kemWjc3XzJGs{OCCvZYTofYxifGmxbh?= NELaXFE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUSwNVY6Oyd-MkW0NFE3QTN:L3G+
SF9402 Ml35T4lv[XOnIHHzd4F6 NXew[YV5PiEQvF2= MoDMSG1UVw>? NVjt[JVUcW6lcnXhd4V{KEt|MTDt[ZRpgWyjdHnvci=> M4TuZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NECxOlk{Lz5{NUSwNVY6OzxxYU6=
SF9427 M3fSR2tqdmG|ZTDhd5NigQ>? Mn3xOkDPxE1? MWDEUXNQ MVTpcoNz\WG|ZYOgT|MzKG2ndHj5cIF1cW:w NGfMeHQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUSwNVY6Oyd-MkW0NFE3QTN:L3G+
human astrocytes NFfOfXlMcW6jc3WgZZN{[Xl? M1S4WVYh|ryP MXzEUXNQ M1PheYlv[3KnYYPld{BMOzNibXX0bJlt[XSrb36= NXrJTWJzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW0NFE3QTNpPkK1OFAyPjl|PD;hQi=>
SF7761 M3fnRmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGL4V3E3KM7:TR?= MYHEUXNQ M4PER4lvcGmkaYTzJGszP01iZ3zpc41iKGOnbHyg[5Jwf3Sq MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTRyMU[5N{c,OjV2MEG2PVM9N2F-
SF8628 M3H3d2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXvKSXpTPiEQvF2= M4PDO2ROW09? MkPrbY5pcWKrdIOgT|I5VSCpbHnvcYEh[2WubDDndo94fGh? MlrSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV2MEG2PVMoRjJ3NECxOlk{RC:jPh?=
H3.3 MUjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1rCc|Yh|ryP NX7XfHZWTE2VTx?= M2DxWYlvcGmkaYTzJGszQU1iZ3zpc41iKGOnbHyg[5Jwf3Sq M1rLOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NECxOlk{Lz5{NUSwNVY6OzxxYU6=
SF9012 M4f1bmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHHPNoc3KM7:TR?= NYK2UI1WTE2VTx?= MnPRbY5pcWKrdIOgT|MxVSCpbHnvcYEh[2WubDDndo94fGh? MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTRyMU[5N{c,OjV2MEG2PVM9N2F-
SF9402 M{j4V2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NIDl[2o3KM7:TR?= NFXGRpNFVVOR MkTpbY5pcWKrdIOgT|MyVSCpbHnvcYEh[2WubDDndo94fGh? NETO[Is9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUSwNVY6Oyd-MkW0NFE3QTN:L3G+
SF9427 MmXWS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnrtOkDPxE1? NX35W3Z5TE2VTx?= MVvpcohq[mm2czDLN|JOKGeuaX;tZUBk\WyuIHfyc5d1cA>? MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTRyMU[5N{c,OjV2MEG2PVM9N2F-
human astrocytes NHzjOG1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFXqWJo3KM7:TR?= MlPDSG1UVw>? MlfQbY5pcWKrdIOgT|M{VSCpbHnvcYEh[2WubDDndo94fGh? Mo\HQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV2MEG2PVMoRjJ3NECxOlk{RC:jPh?=
TG neurons M{[0N2Z2dmO2aX;uJIF{e2G7 M1TTOlUxKM7:TR?= MkXESG1UVw>? NHG1XGFqdmirYnn0d{BJW1ZvMTDy[YFkfGm4YYTpc44h\nKxbTDz[Y5{d3K7IH7leZJwdnN? NF;uXIM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUW1NlczOCd-MkW1OVI4OjB:L3G+
Th17 M1y2T2Z2dmO2aX;uJIF{e2G7 M1zjdlgxKG6P NH;vbpNFVVOR MlXlbY5pcWKrdIOgZ4VtdCCmaX\m[ZJmdnSrYYTpc44> Mk\jQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6NEC5PVMoRjJ3OESwPVk{RC:jPh?=
β-cells MmTKSpVv[3Srb36gZZN{[Xl? MX:yNEDPxE1? NUXCSpVpTE2VTx?= NWD6T4RZ[my3boTzJGlHVs7|LDDJcE0y|rJuIHHu[EBVVkcQsT3pcoR2[2WmIHPo[Y1wc2mwZTDn[Y5mKGW6cILld5Nqd25? MoTwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ3MEWxPVMoRjJ4NUC1NVk{RC:jPh?=
β-cells M2HEOWZ2dmO2aX;uJIF{e2G7 M1GyVVIxKM7:TR?= NXTCc5dCTE2VTx?= NGPxW3BqdmS3Y3XzJO6zNWOnbHyg[Jl{\nWwY4Tpc44> MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjVyNUG5N{c,OjZ3MEWxPVM9N2F-
ESCs NXrrc|cyTnWwY4Tpc44h[XO|YYm= NH:xd4YyNjkkgJZCuW0> NXrpSIM3TE2VTx?= NGLHeHBqdmS3Y3XzJGRPSSCmYX3h[4Uh[Wyxbnege4l1cCCjY4TpeoF1cW:wIH;mJJRp\SCGTlGg[IFu[WenIILld5BwdnOn NYH1RpJGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[3OVkyPzVpPkK2O|U6OTd3PD;hQi=>
Raw 264.7 NIPEc2FHfW6ldHnvckBie3OjeR?= NHPYe|kxNjhzOUNihKXDvU1? NVnwUlY2TE2VTx?= Mn\KbY5pcWKrdIOgWG5HNc7zIIDyc4R2[3Srb36= MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjd5NkO2NEc,OjZ5N{[zOlA9N2F-
MCF7 M1H6NGZ2dmO2aX;uJIF{e2G7 NVTuR3lpOSC2bzCxNEB2VQ>? M3fHcFMxKGi{cx?= M2LPTmlvcGmkaYTpc44hd2ZiS1TNOWEhcW5iaIXtZY4hVUOINzDj[YxteyCjc4Pld5Nm\CCjczDl[oZm[3Rib36gTFNMPG2nMzDt[ZRpgWyjdHnvckBt\X[nbIOgZZQhOSC2bzCxNEB2VSCjZoTldkA{OCCqcoOgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m| NXjMRotvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CzPVI{PDlpPkOwN|kzOzR7PD;hQi=>
MCF7 M1LRbmZ2dmO2aX;uJIF{e2G7 M2ruSlEhfG9iMUCgeW0> NXrVRpRPOzBiaILz MmL5TY5pcWKrdHnvckBw\iCNRF21RUBqdiCqdX3hckBOS0Z5IHPlcIx{KGG|c3Xzd4VlKGG|IHXm[oVkfCCxbjDIN2szP22nMzDt[ZRpgWyjdHnvckBt\X[nbIOgZZQhOSC2bzCxNEB2VSCjZoTldkA{OCCqcoOgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m| NFf6SW09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEO5NlM1QSd-M{CzPVI{PDl:L3G+
RAW264.7 M2nOWlAvQDJidV2= M3PFeFI1KGi{cx?= MVXJcohq[mm2aX;uJI9nKEySUz3pcoR2[2WmIGTOSoFteGijIIDyc4R2[3Srb36gbY4hdW:3c3WgVmFYOjZ2LkegZ4VtdHNiMD64NkB2VSCjZoTldkAzPCCqcoOgZpkhTUyLU1G= MmT1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ5N{[zOlAoRjJ4N{e2N|YxRC:jPh?=
RAW264.7 MoDDNlQhcHK| NUKxeW1FUW6qaXLpeIlwdiCxZjDMVHMucW6mdXPl[EBVVk[jbIDoZUBxem:mdXP0bY9vKGmwIH3veZNmKFKDV{K2OE44KGOnbHzzJIFnfGW{IEK0JIhzeyCkeTDFUGlUSQ>? MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjd5NkO2NEc,OjZ5N{[zOlA9N2F-

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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