GSK J4 HCl (GSKJ4 HCl)

For research use only.

Catalog No.S7070

32 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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10mM (1mL in DMSO) USD 220 In stock
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Selleck's GSK J4 HCl (GSKJ4 HCl) has been cited by 32 publications

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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 Ml\PS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NUeyTI1{OiEQvF2= MXLEUXNQ NG\4VY9i\m[nY4TzJINmdGxiZ4Lve5Rp NUL2b45ORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWxN|I2PDlpPkK1NVMzPTR7PD;hQi=>
CUTLL1 NX7FU5hqSXCxcITvd4l{KGG|c3H5 MXKyJO69VQ>? MYPEUXNQ MXjpcoR2[2W|IHHwc5B1d3Orcx?= MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTF|MkW0PUc,OjVzM{K1OFk9N2F-
CUTLL1 M3vPR2Z2dmO2aX;uJIF{e2G7 M2e4O|Ih|ryP MX3EUXNQ M4jMNIlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= M3nySFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MUOyOVQ6Lz5{NUGzNlU1QTxxYU6=
CUTLL1 M2L5bGtqdmG|ZTDhd5NigQ>? NXnVRXRoPiEQvF2= NETlZmRFVVOR M3zuZoxm[WS|IITvJIlv[3KnYYPl[EBJO0t{N33lNy=> NYXWeIFHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWxN|I2PDlpPkK1NVMzPTR7PD;hQi=>
SF7761 M2rFV2tqdmG|ZTDhd5NigQ>? M4nYUVYh|ryP M2TPfGROW09? NYrpR4p7cW6lcnXhd4V{KEt{NzDt[ZRpgWyjdHnvci=> NH7HdXE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUSwNVY6Oyd-MkW0NFE3QTN:L3G+
SF8628 NGHsVoZMcW6jc3WgZZN{[Xl? MVi2JO69VQ>? Mn7tSG1UVw>? MXzpcoNz\WG|ZYOgT|I5KG2ndHj5cIF1cW:w NHXWOYU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUSwNVY6Oyd-MkW0NFE3QTN:L3G+
H3.3 NGXDNIhMcW6jc3WgZZN{[Xl? NUPVe45KPiEQvF2= M3;MW2ROW09? MU\pcoNz\WG|ZYOgT|I6KG2ndHj5cIF1cW:w M3;qfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NECxOlk{Lz5{NUSwNVY6OzxxYU6=
SF9012 NXvkUlU4U2mwYYPlJIF{e2G7 Mk\0OkDPxE1? NY\INIR1TE2VTx?= Ml3EbY5kemWjc3XzJGs{OCCvZYTofYxifGmxbh?= MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTRyMU[5N{c,OjV2MEG2PVM9N2F-
SF9402 Mly1T4lv[XOnIHHzd4F6 NFe2co03KM7:TR?= MX7EUXNQ M1:3Solv[3KnYYPld{BMOzFibXX0bJlt[XSrb36= NHPrdGk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUSwNVY6Oyd-MkW0NFE3QTN:L3G+
SF9427 MkfsT4lv[XOnIHHzd4F6 M{W2TFYh|ryP MUnEUXNQ MXPpcoNz\WG|ZYOgT|MzKG2ndHj5cIF1cW:w NVPMdIsxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW0NFE3QTNpPkK1OFAyPjl|PD;hQi=>
human astrocytes NIriZZBMcW6jc3WgZZN{[Xl? M37HfFYh|ryP NWnnOnRvTE2VTx?= MmThbY5kemWjc3XzJGs{OyCvZYTofYxifGmxbh?= MlPUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV2MEG2PVMoRjJ3NECxOlk{RC:jPh?=
SF7761 NELBbJVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFW5cms3KM7:TR?= M4DQR2ROW09? NETuN2tqdmirYnn0d{BMOjePIHfsbY9u[SClZXzsJIdzd3e2aB?= MnHzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV2MEG2PVMoRjJ3NECxOlk{RC:jPh?=
SF8628 NGnJUVZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2jUNFYh|ryP NX:wTodrTE2VTx?= MnnHbY5pcWKrdIOgT|I5VSCpbHnvcYEh[2WubDDndo94fGh? M3HRd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NECxOlk{Lz5{NUSwNVY6OzxxYU6=
H3.3 NX;zdWxWT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3rpRlYh|ryP NH\wemVFVVOR MlXYbY5pcWKrdIOgT|I6VSCpbHnvcYEh[2WubDDndo94fGh? NX;aVIZURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW0NFE3QTNpPkK1OFAyPjl|PD;hQi=>
SF9012 NW[2[m1iT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NETFfHQ3KM7:TR?= NIC5b|FFVVOR MkjEbY5pcWKrdIOgT|MxVSCpbHnvcYEh[2WubDDndo94fGh? MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTRyMU[5N{c,OjV2MEG2PVM9N2F-
SF9402 NWXMPJR2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NIjjZ|k3KM7:TR?= M{fX[2ROW09? NX;IWodrcW6qaXLpeJMhUzNzTTDncIlwdWFiY3XscEBoem:5dHi= MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTRyMU[5N{c,OjV2MEG2PVM9N2F-
SF9427 NIO3co5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mkn3OkDPxE1? M{\qNGROW09? NGLWXFRqdmirYnn0d{BMOzKPIHfsbY9u[SClZXzsJIdzd3e2aB?= NYDaTG1yRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW0NFE3QTNpPkK1OFAyPjl|PD;hQi=>
human astrocytes MUfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYnOc41nPiEQvF2= MXXEUXNQ MXnpcohq[mm2czDLN|NOKGeuaX;tZUBk\WyuIHfyc5d1cA>? NHHZPFI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUSwNVY6Oyd-MkW0NFE3QTN:L3G+
TG neurons MVjGeY5kfGmxbjDhd5NigQ>? NWTXVXZrPTBizszN NU\rcXVHTE2VTx?= NX\qNHdJcW6qaXLpeJMhUFOYLUGgdoVi[3SrdnH0bY9vKG[{b32gd4Vve2:{eTDu[ZVzd26| MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTV3MkeyNEc,OjV3NUK3NlA9N2F-
Th17 MnfZSpVv[3Srb36gZZN{[Xl? MkXaPFAhdk1? MnzCSG1UVw>? M{\CXIlvcGmkaYTzJINmdGxiZHnm[oVz\W62aXH0bY9v MlTYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6NEC5PVMoRjJ3OESwPVk{RC:jPh?=
β-cells MoPnSpVv[3Srb36gZZN{[Xl? NFHscFQzOCEQvF2= MXXEUXNQ MkP1Zox2dnS|IFnGUu6{NCCLbD2x{tItKGGwZDDUUmbPuS2rbnT1Z4VlKGOqZX3vb4lv\SCpZX7lJIV5eHKnc4Ppc44> M2rMeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NUC1NVk{Lz5{NkWwOVE6OzxxYU6=
β-cells Mmr3SpVv[3Srb36gZZN{[Xl? M4\TcVIxKM7:TR?= M2HRdmROW09? NInL[29qdmS3Y3XzJO6zNWOnbHyg[Jl{\nWwY4Tpc44> M1TIVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NUC1NVk{Lz5{NkWwOVE6OzxxYU6=
ESCs MVTGeY5kfGmxbjDhd5NigQ>? M4\CTVEvQOLChdM1US=> NYPJdppTTE2VTx?= NYjuR|VvcW6mdXPld{BFVkFiZHHtZYdmKGGub37nJJdqfGhiYXP0bZZifGmxbjDv[kB1cGViRF7BJIRidWGpZTDy[ZNxd26|ZR?= NWj0W3ZURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[3OVkyPzVpPkK2O|U6OTd3PD;hQi=>
Raw 264.7 MV7GeY5kfGmxbjDhd5NigQ>? MXOwMlgyQTMkgJZCuW0> MYnEUXNQ M{n4Z4lvcGmkaYTzJHRPTi4QsTDwdo9lfWO2aX;u NGDPO3U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nke3OlM3OCd-Mk[3O|Y{PjB:L3G+
MCF7 NGTGPZRHfW6ldHnvckBie3OjeR?= M4n3UFEhfG9iMUCgeW0> NXv3Zm5UOzBiaILz NHjR[FNKdmirYnn0bY9vKG:oIFvEUVVCKGmwIHj1cYFvKE2FRkegZ4VtdHNiYYPz[ZN{\WRiYYOg[YZn\WO2IH;uJGg{UzSvZUOgcYV1cHmuYYTpc44hdGW4ZXzzJIF1KDFidH:gNVAhfU1iYX\0[ZIhOzBiaILzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?= M1ThOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{myN|Q6Lz5|MEO5NlM1QTxxYU6=
MCF7 M17C[mZ2dmO2aX;uJIF{e2G7 M{i2VFEhfG9iMUCgeW0> NULROXBsOzBiaILz NHzn[5VKdmirYnn0bY9vKG:oIFvEUVVCKGmwIHj1cYFvKE2FRkegZ4VtdHNiYYPz[ZN{\WRiYYOg[YZn\WO2IH;uJGg{UzJ5bXWzJI1mfGi7bHH0bY9vKGyndnXsd{BifCBzIITvJFExKHWPIHHmeIVzKDNyIHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= M2XZV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{myN|Q6Lz5|MEO5NlM1QTxxYU6=
RAW264.7 MYqwMlgzKHWP MnzKNlQhcHK| NYH5dZoxUW6qaXLpeIlwdiCxZjDMVHMucW6mdXPl[EBVVk[jbIDoZUBxem:mdXP0bY9vKGmwIH3veZNmKFKDV{K2OE44KGOnbHzzJFAvQDJidV2gZYZ1\XJiMkSgbJJ{KGK7IFXMTXNC NULIUVVNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[3O|Y{PjBpPkK2O|c3OzZyPD;hQi=>
RAW264.7 MkDQNlQhcHK| MkWwTY5pcWKrdHnvckBw\iCOUGOtbY5lfWOnZDDUUmZidHCqYTDwdo9lfWO2aX;uJIlvKG2xdYPlJHJCXzJ4ND63JINmdGy|IHHmeIVzKDJ2IHjyd{BjgSCHTFnTRS=> MknwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ5N{[zOlAoRjJ4N{e2N|YxRC:jPh?=

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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