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 NX3KRnRXT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4TMcFIh|ryP MYjEUXNQ MWTh[oZm[3S|IHPlcIwh\3Kxd4To M4XWOVI2OTN{NUS5
CUTLL1 NEDsUm5CeG:ydH;zbZMh[XO|YYm= NEm5UoczKM7:TR?= MWHEUXNQ NF;wV4NqdmS3Y3XzJIFxd3C2b4Ppdy=> NES4NZgzPTF|MkW0PS=>
CUTLL1 NY\CPGlCTnWwY4Tpc44h[XO|YYm= MoXoNkDPxE1? NUPCT4FiTE2VTx?= MmHibY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= M2XZVlI2OTN{NUS5
CUTLL1 NF;aO4JMcW6jc3WgZZN{[Xl? NFHOTpo3KM7:TR?= Mn\PSG1UVw>? M1G4W4xm[WS|IITvJIlv[3KnYYPl[EBJO0t{N33lNy=> MluwNlUyOzJ3NEm=
SF7761 NVjCdmtOU2mwYYPlJIF{e2G7 M1npcVYh|ryP MlH2SG1UVw>? Ml7ibY5kemWjc3XzJGszPyCvZYTofYxifGmxbh?= M1rxbFI2PDBzNkmz
SF8628 MYHLbY5ie2ViYYPzZZk> NVzKRlZRPiEQvF2= NWH5Uo5VTE2VTx?= NGLOOW9qdmO{ZXHz[ZMhUzJ6IH3leIh6dGG2aX;u NWHudpVYOjV2MEG2PVM>
H3.3 M{LVUGtqdmG|ZTDhd5NigQ>? NVHlWYFpPiEQvF2= MliySG1UVw>? MWjpcoNz\WG|ZYOgT|I6KG2ndHj5cIF1cW:w NXHxcIV[OjV2MEG2PVM>
SF9012 M2jCTmtqdmG|ZTDhd5NigQ>? NIDLSlk3KM7:TR?= MnG5SG1UVw>? MkDEbY5kemWjc3XzJGs{OCCvZYTofYxifGmxbh?= NVLDWXo3OjV2MEG2PVM>
SF9402 MnXFT4lv[XOnIHHzd4F6 MWW2JO69VQ>? Mn72SG1UVw>? M{PUfIlv[3KnYYPld{BMOzFibXX0bJlt[XSrb36= M2XLXlI2PDBzNkmz
SF9427 MVvLbY5ie2ViYYPzZZk> MlTROkDPxE1? NEnmfmxFVVOR NVTJc2pPcW6lcnXhd4V{KEt|MjDt[ZRpgWyjdHnvci=> MnXSNlU1ODF4OUO=
human astrocytes Ml\lT4lv[XOnIHHzd4F6 NID5NWg3KM7:TR?= NHzXfXpFVVOR MVrpcoNz\WG|ZYOgT|M{KG2ndHj5cIF1cW:w MUiyOVQxOTZ7Mx?=
SF7761 M3P1eGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYnZW4FZPiEQvF2= MYLEUXNQ MULpcohq[mm2czDLNldOKGeuaX;tZUBk\WyuIHfyc5d1cA>? NUn3bWU3OjV2MEG2PVM>
SF8628 MX\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3HHNFYh|ryP MXHEUXNQ NEe1ZWhqdmirYnn0d{BMOjiPIHfsbY9u[SClZXzsJIdzd3e2aB?= MUKyOVQxOTZ7Mx?=
H3.3 NYH5PIFWT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYWyZZNWPiEQvF2= MYLEUXNQ NH24cY9qdmirYnn0d{BMOjmPIHfsbY9u[SClZXzsJIdzd3e2aB?= MkT4NlU1ODF4OUO=
SF9012 MVfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHrmZ2Q3KM7:TR?= MXHEUXNQ M2\yTolvcGmkaYTzJGs{OE1iZ3zpc41iKGOnbHyg[5Jwf3Sq M3fwVFI2PDBzNkmz
SF9402 MVjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYL3NZF4PiEQvF2= M1HSPGROW09? M1y2eYlvcGmkaYTzJGs{OU1iZ3zpc41iKGOnbHyg[5Jwf3Sq NGXrUmozPTRyMU[5Ny=>
SF9427 MmPyS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVS2JO69VQ>? M3zpcGROW09? NIjSZ3JqdmirYnn0d{BMOzKPIHfsbY9u[SClZXzsJIdzd3e2aB?= NUG1N2RvOjV2MEG2PVM>
human astrocytes NYDqU4ZXT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnL0OkDPxE1? MXPEUXNQ NX75dVJJcW6qaXLpeJMhUzN|TTDncIlwdWFiY3XscEBoem:5dHi= NUPhbZpCOjV2MEG2PVM>
TG neurons MmPLSpVv[3Srb36gZZN{[Xl? M1X4SVUxKM7:TR?= NGnXOm9FVVOR MmD1bY5pcWKrdIOgTHNXNTFicnXhZ5RqfmG2aX;uJIZzd21ic3Xud49zgSCwZYXyc45{ NXLaV2loOjV3NUK3NlA>
Th17 Ml[xSpVv[3Srb36gZZN{[Xl? NGfW[4U5OCCwTR?= NUj6eYxVTE2VTx?= Mme3bY5pcWKrdIOgZ4VtdCCmaX\m[ZJmdnSrYYTpc44> NXPTZ|V3OjV6NEC5PVM>
β-cells M{HsSGZ2dmO2aX;uJIF{e2G7 NWPaN4V3OjBizszN NFfQfmdFVVOR M4HQWIJtfW62czDJSm7PuyxiSXytNe6zNCCjbnSgWG5H|rFvaX7keYNm\CClaHXtc4tqdmViZ3Xu[UBmgHC{ZYPzbY9v MY[yOlUxPTF7Mx?=
β-cells MnXTSpVv[3Srb36gZZN{[Xl? M{HSdFIxKM7:TR?= MXrEUXNQ M4jQV4lv\HWlZYOg{tIu[2WubDDkfZNnfW6ldHnvci=> NE\RUlgzPjVyNUG5Ny=>
ESCs NV\1O3htTnWwY4Tpc44h[XO|YYm= MV6xMljjiIYEtV2= MVzEUXNQ MnjtbY5lfWOnczDEUmEh\GGvYXflJIFtd26pIIfpeIgh[WO2aY\heIlwdiCxZjD0bIUhTE6DIHThcYFo\SC{ZYPwc45{\Q>? MYqyOlc2QTF5NR?=
Raw 264.7 NFPibG1HfW6ldHnvckBie3OjeR?= MnLNNE45OTl{4pEFxtVO NVHFPHlXTE2VTx?= MX\pcohq[mm2czDUUmYu|rFicILv[JVkfGmxbh?= NITPZ4YzPjd5NkO2NC=>

... 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 <1 mg/mL
In vivo 2% DMSO+dd H2O 10 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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

Bio Calculators

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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