GSK J4 HCl (GSKJ4 HCl)

For research use only.

Catalog No.S7070

23 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) USD 220 In stock
USD 170 In stock
USD 570 In stock
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Selleck's GSK J4 HCl (GSKJ4 HCl) has been cited by 23 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 M1LXSmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M{nISlIh|ryP MUDEUXNQ M336V4Fn\mWldIOgZ4VtdCCpcn;3eIg> M2rtW|I2OTN{NUS5
CUTLL1 M3vvfGFxd3C2b4Ppd{Bie3OjeR?= MWiyJO69VQ>? MX;EUXNQ M2O3c4lv\HWlZYOgZZBweHSxc3nz MlXWNlUyOzJ3NEm=
CUTLL1 NVvlTnlDTnWwY4Tpc44h[XO|YYm= MnrFNkDPxE1? MmjrSG1UVw>? NYjkOHBscW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> NWrGWnBzOjVzM{K1OFk>
CUTLL1 NYPmNHoxU2mwYYPlJIF{e2G7 NYLmN5JNPiEQvF2= MXLEUXNQ M{\5Xoxm[WS|IITvJIlv[3KnYYPl[EBJO0t{N33lNy=> MVmyOVE{OjV2OR?=
SF7761 NFvZeHZMcW6jc3WgZZN{[Xl? MmPoOkDPxE1? Mk\JSG1UVw>? M1L5R4lv[3KnYYPld{BMOjdibXX0bJlt[XSrb36= M1HnTlI2PDBzNkmz
SF8628 MnuxT4lv[XOnIHHzd4F6 M2\sSFYh|ryP M4PG[2ROW09? NUfsbHJxcW6lcnXhd4V{KEt{ODDt[ZRpgWyjdHnvci=> MUOyOVQxOTZ7Mx?=
H3.3 MlSxT4lv[XOnIHHzd4F6 NIK3V3E3KM7:TR?= MY\EUXNQ MWfpcoNz\WG|ZYOgT|I6KG2ndHj5cIF1cW:w NIXKS|IzPTRyMU[5Ny=>
SF9012 NXvnSYFsU2mwYYPlJIF{e2G7 MWq2JO69VQ>? M4j4ZmROW09? M1HmRolv[3KnYYPld{BMOzBibXX0bJlt[XSrb36= MmWwNlU1ODF4OUO=
SF9402 MYLLbY5ie2ViYYPzZZk> M1;MPFYh|ryP Moe2SG1UVw>? NHHWcHFqdmO{ZXHz[ZMhUzNzIH3leIh6dGG2aX;u NXjrfnNuOjV2MEG2PVM>
SF9427 NELrVWhMcW6jc3WgZZN{[Xl? NF;XXXo3KM7:TR?= NIHiXo5FVVOR NH23ToxqdmO{ZXHz[ZMhUzN{IH3leIh6dGG2aX;u MmnvNlU1ODF4OUO=
human astrocytes MWHLbY5ie2ViYYPzZZk> MkX3OkDPxE1? MYPEUXNQ NIfMT2tqdmO{ZXHz[ZMhUzN|IH3leIh6dGG2aX;u MoSzNlU1ODF4OUO=
SF7761 NW\rfFRzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUG2JO69VQ>? Mlj5SG1UVw>? MnW3bY5pcWKrdIOgT|I4VSCpbHnvcYEh[2WubDDndo94fGh? NY\WZlNyOjV2MEG2PVM>
SF8628 M{G4[mdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlXXOkDPxE1? NIm2dG1FVVOR M2jsTolvcGmkaYTzJGszQE1iZ3zpc41iKGOnbHyg[5Jwf3Sq NFfQU2IzPTRyMU[5Ny=>
H3.3 NXrLVG14T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MlnaOkDPxE1? NVHpcIpyTE2VTx?= MlrObY5pcWKrdIOgT|I6VSCpbHnvcYEh[2WubDDndo94fGh? Mm\uNlU1ODF4OUO=
SF9012 M17vUWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYHZfFd[PiEQvF2= MYrEUXNQ NX3QblFOcW6qaXLpeJMhUzNyTTDncIlwdWFiY3XscEBoem:5dHi= NXPEc3NLOjV2MEG2PVM>
SF9402 MXLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHPaTWc3KM7:TR?= MnPxSG1UVw>? NW\MXpNscW6qaXLpeJMhUzNzTTDncIlwdWFiY3XscEBoem:5dHi= M1;nRlI2PDBzNkmz
SF9427 NUDkfGdNT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2XpWVYh|ryP M1HGN2ROW09? M1\XXIlvcGmkaYTzJGs{Ok1iZ3zpc41iKGOnbHyg[5Jwf3Sq NV2wbJhxOjV2MEG2PVM>
human astrocytes M4rSZmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXXSSnA5PiEQvF2= MYnEUXNQ MlnvbY5pcWKrdIOgT|M{VSCpbHnvcYEh[2WubDDndo94fGh? NW\zUZNEOjV2MEG2PVM>
TG neurons NUnOd4NbTnWwY4Tpc44h[XO|YYm= MnLOOVAh|ryP NH[xVIVFVVOR M4r1V4lvcGmkaYTzJGhUXi1zIILlZYN1cX[jdHnvckBnem:vIIPlcpNwenlibnX1do9vew>? NX:2VWZ3OjV3NUK3NlA>
Th17 NYWzdWZYTnWwY4Tpc44h[XO|YYm= NUK1Zo5MQDBibl2= M1TsW2ROW09? NGTXfnNqdmirYnn0d{Bk\WyuIHTp[oZmemWwdHnheIlwdg>? NXjO[5p7OjV6NEC5PVM>
β-cells M1P1ZWZ2dmO2aX;uJIF{e2G7 NHPQXGwzOCEQvF2= M4HCT2ROW09? MUnicJVvfHNiSV\O{tMtKEmuLUJOtkwh[W6mIGTOSu6yNWmwZIXj[YQh[2inbX;rbY5mKGenbnWg[ZhxemW|c3nvci=> M1zZfFI3PTB3MUmz
β-cells MlOySpVv[3Srb36gZZN{[Xl? MU[yNEDPxE1? MnvySG1UVw>? MoewbY5lfWOnczFOtk1k\WyuIHT5d4Z2dmO2aX;u Mor2NlY2ODVzOUO=
ESCs M1L5U2Z2dmO2aX;uJIF{e2G7 MX2xMljjiIYEtV2= M3\Ge2ROW09? MVzpcoR2[2W|IFTORUBl[W2jZ3WgZYxwdmdid3n0bEBi[3SrdnH0bY9vKG:oIITo[UBFVkFiZHHtZYdmKHKnc4DvcpNm MVSyOlc2QTF5NR?=
Raw 264.7 M2\aXWZ2dmO2aX;uJIF{e2G7 NIfzcI8xNjhzOUNihKXDvU1? NGDpTHBFVVOR MkL5bY5pcWKrdIOgWG5HNc7zIIDyc4R2[3Srb36= NIP4b2gzPjd5NkO2NC=>

... 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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Molecular Weight Calculator

Molecular Weight Calculator

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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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