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

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 MXnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1m1[|Ih|ryP MmnqSG1UVw>? NHXL[Hdi\m[nY4TzJINmdGxiZ4Lve5Rp NX\iOVd2OjVzM{K1OFk>
CUTLL1 NGTVOnJCeG:ydH;zbZMh[XO|YYm= NEXKdG4zKM7:TR?= Mk\6SG1UVw>? NY\oOHMxcW6mdXPld{BieG:ydH;zbZM> NGnh[IIzPTF|MkW0PS=>
CUTLL1 MULGeY5kfGmxbjDhd5NigQ>? MYqyJO69VQ>? NGXGOVVFVVOR NITGdo1qdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 M3HM[VI2OTN{NUS5
CUTLL1 NGKzR5hMcW6jc3WgZZN{[Xl? NGjBN4w3KM7:TR?= M{LVc2ROW09? Mo\ocIVi\HNidH:gbY5kemWjc3XkJGg{UzJ5bXWz NIjNZmwzPTF|MkW0PS=>
SF7761 M{S3eWtqdmG|ZTDhd5NigQ>? M2XDUlYh|ryP M33rU2ROW09? M1zXOIlv[3KnYYPld{BMOjdibXX0bJlt[XSrb36= NV;ncVJYOjV2MEG2PVM>
SF8628 NHjZOmpMcW6jc3WgZZN{[Xl? NXHjb29KPiEQvF2= MnHDSG1UVw>? M33kU4lv[3KnYYPld{BMOjhibXX0bJlt[XSrb36= NIHrO3gzPTRyMU[5Ny=>
H3.3 NYfSOFB2U2mwYYPlJIF{e2G7 NGHWT3c3KM7:TR?= MVnEUXNQ MmXmbY5kemWjc3XzJGszQSCvZYTofYxifGmxbh?= MlPFNlU1ODF4OUO=
SF9012 NFXHU25McW6jc3WgZZN{[Xl? NYPLdZkzPiEQvF2= MUTEUXNQ MY\pcoNz\WG|ZYOgT|MxKG2ndHj5cIF1cW:w MVqyOVQxOTZ7Mx?=
SF9402 NVO1dZozU2mwYYPlJIF{e2G7 NGfCfYk3KM7:TR?= NF20TYdFVVOR Mo\ubY5kemWjc3XzJGs{OSCvZYTofYxifGmxbh?= NYTTeJZiOjV2MEG2PVM>
SF9427 M1jvTWtqdmG|ZTDhd5NigQ>? NH\LPXA3KM7:TR?= NE\mRZVFVVOR MWLpcoNz\WG|ZYOgT|MzKG2ndHj5cIF1cW:w MViyOVQxOTZ7Mx?=
human astrocytes MUXLbY5ie2ViYYPzZZk> MmjXOkDPxE1? MoHZSG1UVw>? MkXjbY5kemWjc3XzJGs{OyCvZYTofYxifGmxbh?= M{TCfFI2PDBzNkmz
SF7761 NGP5WnFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MmrlOkDPxE1? NEXidVJFVVOR NHfzSVJqdmirYnn0d{BMOjePIHfsbY9u[SClZXzsJIdzd3e2aB?= Ml;INlU1ODF4OUO=
SF8628 Ml;pS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M17IVFYh|ryP MY\EUXNQ MmrJbY5pcWKrdIOgT|I5VSCpbHnvcYEh[2WubDDndo94fGh? MmrNNlU1ODF4OUO=
H3.3 M3\iVmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MWe2JO69VQ>? NGPQS4RFVVOR Ml;hbY5pcWKrdIOgT|I6VSCpbHnvcYEh[2WubDDndo94fGh? MmjoNlU1ODF4OUO=
SF9012 MVXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXXCT4NRPiEQvF2= M3rz[2ROW09? MWDpcohq[mm2czDLN|BOKGeuaX;tZUBk\WyuIHfyc5d1cA>? NGPVXpozPTRyMU[5Ny=>
SF9402 NU\5eJVOT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4PpW|Yh|ryP M4PCWmROW09? MU\pcohq[mm2czDLN|FOKGeuaX;tZUBk\WyuIHfyc5d1cA>? MnzoNlU1ODF4OUO=
SF9427 NXzMb|IxT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWS2JO69VQ>? NYTxXY5[TE2VTx?= MlLobY5pcWKrdIOgT|MzVSCpbHnvcYEh[2WubDDndo94fGh? MYiyOVQxOTZ7Mx?=
human astrocytes M1\LZWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MWW2JO69VQ>? MnzxSG1UVw>? NV\uSVRpcW6qaXLpeJMhUzN|TTDncIlwdWFiY3XscEBoem:5dHi= NIrVVYIzPTRyMU[5Ny=>
TG neurons NHz1UINHfW6ldHnvckBie3OjeR?= M3K2W|UxKM7:TR?= NXXzRppmTE2VTx?= MYrpcohq[mm2czDIV3YuOSC{ZXHjeIl3[XSrb36g[pJwdSC|ZX7zc5J6KG6ndYLvcpM> MonjNlU2PTJ5MkC=
Th17 NInFdG9HfW6ldHnvckBie3OjeR?= MYO4NEBvVQ>? MnPvSG1UVw>? NIrMSZNqdmirYnn0d{Bk\WyuIHTp[oZmemWwdHnheIlwdg>? NF[xcpAzPTh2MEm5Ny=>
β-cells MYLGeY5kfGmxbjDhd5NigQ>? MnvuNlAh|ryP NIrTNnVFVVOR MnfoZox2dnS|IFnGUu6{NCCLbD2x{tItKGGwZDDUUmbPuS2rbnT1Z4VlKGOqZX3vb4lv\SCpZX7lJIV5eHKnc4Ppc44> M1TKfFI3PTB3MUmz
β-cells NEjweGlHfW6ldHnvckBie3OjeR?= MYeyNEDPxE1? NEjBWoxFVVOR MmDnbY5lfWOnczFOtk1k\WyuIHT5d4Z2dmO2aX;u M3PZPFI3PTB3MUmz
ESCs NGHHeFhHfW6ldHnvckBie3OjeR?= NYfTc3lUOS564pEFxtVO MnflSG1UVw>? NYnqWINicW6mdXPld{BFVkFiZHHtZYdmKGGub37nJJdqfGhiYXP0bZZifGmxbjDv[kB1cGViRF7BJIRidWGpZTDy[ZNxd26|ZR?= NX31UWk1OjZ5NUmxO|U>
Raw 264.7 MnPESpVv[3Srb36gZZN{[Xl? MUewMlgyQTMkgJZCuW0> MX\EUXNQ MkfBbY5pcWKrdIOgWG5HNc7zIIDyc4R2[3Srb36= MX:yOlc4PjN4MB?=

... Click to View More Cell Line Experimental Data

Protocol

Solubility (25°C)

In vitro DMSO 90 mg/mL (198.25 mM) warming
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

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

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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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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