GSK J4 HCl

Catalog No.S7070

GSK J4 HCl Chemical Structure

Molecular Weight(MW): 453.96

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.

Size Price Stock Quantity  
In DMSO USD 220 In stock
USD 170 In stock
USD 570 In stock
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1 Customer Review

  • Nat Med, 2015, 21(6):555-9. . GSK J4 HCl purchased from Selleck.

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 NITiU4xIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4jBVVIh|ryP NEj6fI9FVVOR MoSzZYZn\WO2czDj[YxtKGe{b4f0bC=> M2LrSFI2OTN{NUS5
CUTLL1 MnfSRZBweHSxc3nzJIF{e2G7 M{XCblIh|ryP MVfEUXNQ NH7zNoxqdmS3Y3XzJIFxd3C2b4Ppdy=> M4D6PVI2OTN{NUS5
CUTLL1 NXrEN3IzTnWwY4Tpc44h[XO|YYm= MnTDNkDPxE1? NF3Db5VFVVOR M3fOVIlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= NVnUVo9rOjVzM{K1OFk>
CUTLL1 M2jVV2tqdmG|ZTDhd5NigQ>? MX:2JO69VQ>? NEPDSZpFVVOR MoDMcIVi\HNidH:gbY5kemWjc3XkJGg{UzJ5bXWz Mn;oNlUyOzJ3NEm=
SF7761 MkfKT4lv[XOnIHHzd4F6 NE\3OVc3KM7:TR?= NYTF[2xqTE2VTx?= NYnxRVZLcW6lcnXhd4V{KEt{NzDt[ZRpgWyjdHnvci=> Ml36NlU1ODF4OUO=
SF8628 MXXLbY5ie2ViYYPzZZk> M2fYRVYh|ryP MUfEUXNQ MVfpcoNz\WG|ZYOgT|I5KG2ndHj5cIF1cW:w NGnP[48zPTRyMU[5Ny=>
H3.3 NEXn[YhMcW6jc3WgZZN{[Xl? MnLDOkDPxE1? MWTEUXNQ NUTzWZFDcW6lcnXhd4V{KEt{OTDt[ZRpgWyjdHnvci=> MWeyOVQxOTZ7Mx?=
SF9012 NWLVOJM2U2mwYYPlJIF{e2G7 NXPrXZlXPiEQvF2= M2nnWmROW09? MlzVbY5kemWjc3XzJGs{OCCvZYTofYxifGmxbh?= NEnxdW4zPTRyMU[5Ny=>
SF9402 NXjubFh3U2mwYYPlJIF{e2G7 M1zlSlYh|ryP NGnsSoxFVVOR NEjxWmpqdmO{ZXHz[ZMhUzNzIH3leIh6dGG2aX;u NFrieWQzPTRyMU[5Ny=>
SF9427 M3fkd2tqdmG|ZTDhd5NigQ>? NWPmdoxLPiEQvF2= MV\EUXNQ MWHpcoNz\WG|ZYOgT|MzKG2ndHj5cIF1cW:w Mor3NlU1ODF4OUO=
human astrocytes NGrzSJVMcW6jc3WgZZN{[Xl? MXK2JO69VQ>? MYTEUXNQ MUXpcoNz\WG|ZYOgT|M{KG2ndHj5cIF1cW:w MkKxNlU1ODF4OUO=
SF7761 NIjFVJNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXXYR4lrPiEQvF2= M4XUTGROW09? NGPpdm1qdmirYnn0d{BMOjePIHfsbY9u[SClZXzsJIdzd3e2aB?= NV7jfHpXOjV2MEG2PVM>
SF8628 MUjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHPXZYk3KM7:TR?= MXjEUXNQ MXPpcohq[mm2czDLNlhOKGeuaX;tZUBk\WyuIHfyc5d1cA>? NHPufYUzPTRyMU[5Ny=>
H3.3 NFPWUY5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M13WclYh|ryP NIL3U4RFVVOR NHPJfpBqdmirYnn0d{BMOjmPIHfsbY9u[SClZXzsJIdzd3e2aB?= NYjYV2ZSOjV2MEG2PVM>
SF9012 MVXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXfTV4pbPiEQvF2= MmPQSG1UVw>? NVjaXHJpcW6qaXLpeJMhUzNyTTDncIlwdWFiY3XscEBoem:5dHi= MYCyOVQxOTZ7Mx?=
SF9402 MX3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGDOS2Q3KM7:TR?= NWHxWHpVTE2VTx?= M2\5bIlvcGmkaYTzJGs{OU1iZ3zpc41iKGOnbHyg[5Jwf3Sq NF;HfVMzPTRyMU[5Ny=>
SF9427 MmfqS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWC2JO69VQ>? NVTmcWtOTE2VTx?= NGLuT2JqdmirYnn0d{BMOzKPIHfsbY9u[SClZXzsJIdzd3e2aB?= NVPKdWpPOjV2MEG2PVM>
human astrocytes MkPGS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MU[2JO69VQ>? NETHcm1FVVOR MlTLbY5pcWKrdIOgT|M{VSCpbHnvcYEh[2WubDDndo94fGh? M1zEd|I2PDBzNkmz
TG neurons M4LkN2Z2dmO2aX;uJIF{e2G7 M1vDSFUxKM7:TR?= NGP1NlVFVVOR NV\Be|k{cW6qaXLpeJMhUFOYLUGgdoVi[3SrdnH0bY9vKG[{b32gd4Vve2:{eTDu[ZVzd26| MXeyOVU2Ojd{MB?=
Th17 MnPnSpVv[3Srb36gZZN{[Xl? M2rtNVgxKG6P M2Kz[mROW09? M17RWolvcGmkaYTzJINmdGxiZHnm[oVz\W62aXH0bY9v MnnONlU5PDB7OUO=
β-cells MlPqSpVv[3Srb36gZZN{[Xl? NGTwPHczOCEQvF2= Ml3jSG1UVw>? NWPSdXVP[my3boTzJGlHVs7|LDDJcE0y|rJuIHHu[EBVVkcQsT3pcoR2[2WmIHPo[Y1wc2mwZTDn[Y5mKGW6cILld5Nqd25? NYjLfI1EOjZ3MEWxPVM>
β-cells MXPGeY5kfGmxbjDhd5NigQ>? MlXkNlAh|ryP MW\EUXNQ MXfpcoR2[2W|IN8yMYNmdGxiZInz[pVv[3Srb36= MnnRNlY2ODVzOUO=
ESCs NX7BWIV3TnWwY4Tpc44h[XO|YYm= NI\Pb5kyNjkkgJZCuW0> MoHKSG1UVw>? M1;BSIlv\HWlZYOgSG5CKGSjbXHn[UBidG:wZzD3bZRpKGGldHn2ZZRqd25ib3[geIhmKESQQTDkZY1i\2VicnXzdI9ve2V? MV6yOlc2QTF5NR?=
Raw 264.7 NHmwV2xHfW6ldHnvckBie3OjeR?= M1PnUVAvQDF7MvMAieK2VQ>? MWTEUXNQ MVLpcohq[mm2czDUUmYu|rFicILv[JVkfGmxbh?= MlX1NlY4PzZ|NkC=

... Click to View More Cell Line Experimental Data

Protocol

Solubility (25°C)

In vitro DMSO 90 mg/mL warmed (198.25 mM)
Ethanol 90 mg/mL warmed (198.25 mM)
Water slightly soluble or insoluble
In vivo Add solvents individually and in order:
2% DMSO+dd H2O
10 mg/mL

* 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. 1373423-53-0(free base)
Storage powder
in solvent
Synonyms N/A

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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

Tel: +1-832-582-8158 Ext:3

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Histone Demethylase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID