GSK J4 HCl (GSKJ4 HCl)

For research use only.

Catalog No.S7070

25 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.

Size Price Stock Quantity  
10mM (1mL in DMSO) EUR 216 In stock
EUR 167 In stock
EUR 560 In stock
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Selleck's GSK J4 HCl (GSKJ4 HCl) has been cited by 25 publications

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 MlfuS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NGDYd4gzKM7:TR?= MVPEUXNQ MWXh[oZm[3S|IHPlcIwh\3Kxd4To MmKwNlUyOzJ3NEm=
CUTLL1 M33KXWFxd3C2b4Ppd{Bie3OjeR?= M{DHWFIh|ryP NYm1XGlpTE2VTx?= NEnJ[FlqdmS3Y3XzJIFxd3C2b4Ppdy=> NXTZZ2x2OjVzM{K1OFk>
CUTLL1 MWXGeY5kfGmxbjDhd5NigQ>? MlPQNkDPxE1? MXHEUXNQ NHXR[XBqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 MomyNlUyOzJ3NEm=
CUTLL1 MmDhT4lv[XOnIHHzd4F6 NEjmSFI3KM7:TR?= MYrEUXNQ M2ftS4xm[WS|IITvJIlv[3KnYYPl[EBJO0t{N33lNy=> NIfG[lYzPTF|MkW0PS=>
SF7761 NVm1UZlHU2mwYYPlJIF{e2G7 M3fvdVYh|ryP MVHEUXNQ MlWwbY5kemWjc3XzJGszPyCvZYTofYxifGmxbh?= NUf6eZB5OjV2MEG2PVM>
SF8628 NVPYcYd2U2mwYYPlJIF{e2G7 M2LDc|Yh|ryP MlfRSG1UVw>? M3j0Xolv[3KnYYPld{BMOjhibXX0bJlt[XSrb36= NEP4ZYQzPTRyMU[5Ny=>
H3.3 NFLSZXhMcW6jc3WgZZN{[Xl? M3KybFYh|ryP NGfibopFVVOR NIjFS5FqdmO{ZXHz[ZMhUzJ7IH3leIh6dGG2aX;u NFLMTXMzPTRyMU[5Ny=>
SF9012 M2[0S2tqdmG|ZTDhd5NigQ>? MWC2JO69VQ>? Mk\zSG1UVw>? NF[3VFZqdmO{ZXHz[ZMhUzNyIH3leIh6dGG2aX;u MkDXNlU1ODF4OUO=
SF9402 MV\LbY5ie2ViYYPzZZk> M1[1SlYh|ryP NFPwXYdFVVOR MXjpcoNz\WG|ZYOgT|MyKG2ndHj5cIF1cW:w M3qy[FI2PDBzNkmz
SF9427 MlnHT4lv[XOnIHHzd4F6 MXq2JO69VQ>? MmHFSG1UVw>? MmTabY5kemWjc3XzJGs{OiCvZYTofYxifGmxbh?= NXXoWGJlOjV2MEG2PVM>
human astrocytes M2X4NWtqdmG|ZTDhd5NigQ>? M37IPVYh|ryP NF3RcGlFVVOR MWLpcoNz\WG|ZYOgT|M{KG2ndHj5cIF1cW:w Mo\oNlU1ODF4OUO=
SF7761 NULtO2ZHT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYXFfmwyPiEQvF2= M1nSSWROW09? MYrpcohq[mm2czDLNldOKGeuaX;tZUBk\WyuIHfyc5d1cA>? Mn\vNlU1ODF4OUO=
SF8628 M17GN2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmTMOkDPxE1? M4D0dmROW09? MYjpcohq[mm2czDLNlhOKGeuaX;tZUBk\WyuIHfyc5d1cA>? MnH0NlU1ODF4OUO=
H3.3 NEP4bXpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NEHh[3A3KM7:TR?= Mn7TSG1UVw>? MY\pcohq[mm2czDLNllOKGeuaX;tZUBk\WyuIHfyc5d1cA>? NEH0NHEzPTRyMU[5Ny=>
SF9012 M1PQVWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NUiwNWI{PiEQvF2= NGm0NldFVVOR MVXpcohq[mm2czDLN|BOKGeuaX;tZUBk\WyuIHfyc5d1cA>? MY[yOVQxOTZ7Mx?=
SF9402 NF7JcG5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NF;YfHk3KM7:TR?= NXTLNm9ITE2VTx?= MmTkbY5pcWKrdIOgT|MyVSCpbHnvcYEh[2WubDDndo94fGh? MnL6NlU1ODF4OUO=
SF9427 M{HhSGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2PzcVYh|ryP M{PZ[GROW09? NWi3ZnY3cW6qaXLpeJMhUzN{TTDncIlwdWFiY3XscEBoem:5dHi= MVWyOVQxOTZ7Mx?=
human astrocytes MlTFS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MonUOkDPxE1? NYDOcZdqTE2VTx?= NGrreGJqdmirYnn0d{BMOzOPIHfsbY9u[SClZXzsJIdzd3e2aB?= M4jBblI2PDBzNkmz
TG neurons M2PzZ2Z2dmO2aX;uJIF{e2G7 MYO1NEDPxE1? NHrtVHJFVVOR M{TybIlvcGmkaYTzJGhUXi1zIILlZYN1cX[jdHnvckBnem:vIIPlcpNwenlibnX1do9vew>? MmHCNlU2PTJ5MkC=
Th17 NYfkNolbTnWwY4Tpc44h[XO|YYm= MXW4NEBvVQ>? M1HIVGROW09? NVzrV4w1cW6qaXLpeJMh[2WubDDkbYZn\XKnboTpZZRqd25? MnTjNlU5PDB7OUO=
β-cells NGrJeW5HfW6ldHnvckBie3OjeR?= NE\TZW0zOCEQvF2= MYPEUXNQ NX;BUpQ2[my3boTzJGlHVs7|LDDJcE0y|rJuIHHu[EBVVkcQsT3pcoR2[2WmIHPo[Y1wc2mwZTDn[Y5mKGW6cILld5Nqd25? M3LjN|I3PTB3MUmz
β-cells MX;GeY5kfGmxbjDhd5NigQ>? MWCyNEDPxE1? M3rjd2ROW09? NYDqUYdvcW6mdXPld{DPui2lZXzsJIR6e2[3bnP0bY9v M3;aZlI3PTB3MUmz
ESCs M3vzZ2Z2dmO2aX;uJIF{e2G7 NY\3[G1jOS564pEFxtVO M17aUmROW09? M1jYVolv\HWlZYOgSG5CKGSjbXHn[UBidG:wZzD3bZRpKGGldHn2ZZRqd25ib3[geIhmKESQQTDkZY1i\2VicnXzdI9ve2V? NI\SN5czPjd3OUG3OS=>
Raw 264.7 NGfs[5FHfW6ldHnvckBie3OjeR?= NEn1[o4xNjhzOUNihKXDvU1? NHXmOoVFVVOR NWXBPXZ5cW6qaXLpeJMhXE6ILd8xJJBzd2S3Y4Tpc44> M1nSZlI3Pzd4M{[w

... Click to View More Cell Line Experimental Data

Protocol

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
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+dd H2O
For best results, use promptly after mixing.
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. 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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
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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 (mg) = Concentration (mM) × Volume (mL) × 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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  • Computed Result

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    C2=C1/X C2: LOG(C2):
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Molecular Weight Calculator

Molecular Weight Calculator

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Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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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