GSK J4 HCl (GSKJ4 HCl)

Catalog No.S7070

GSK J4 HCl (GSKJ4 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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Cited by 9 Publications

4 Customer Reviews

  • DIPG cells were seeded into 96-well plates and treated with panobinostat and GSK-J4 individually or in combination at the indicated concentrations for 72 hr in at least triplicate. Cell viabilities were then assessed using the CelltiterGlo assay relative to 0.1% DMSO control. Data shown as mean ± SD. *indicates the two drugs demonstrate synergy at that condition (i.e. CI < 1).

    Nat Med, 2015, 21(6):555-9. . GSK J4 HCl (GSKJ4 HCl) purchased from Selleck.

    Inhibition of JMJD3 mitigated the IL-1β-induced inflammatory response in the MH7A cells. The MH7A cells were transfected with control or JMJD3 siRNA or treated with the indicated concentrations of GSK-J4 (JMJD3 inhibitor) and were then stimulated with IL-1β for 24 h. Western blot analysis of JMJD3, TLR2, COX-2 and GAPDH expression (d).

    Cell Mol Immunol, 2018, doi:10.1038/s41423-018-0037-8. GSK J4 HCl (GSKJ4 HCl) purchased from Selleck.

  • GSK J4 inhibited PDGF-induced cyclin D1 and PCNA expression. The cells were preincubated for 4 h, with or without 10 mM GSK J4, followed by stimulation with 25 ng/ml PDGF-BB for 36 h. Cells were immunostained with anti-JMJD3 antibodies (green), and nuclei were stained with DAPI (blue) and analyzed by fluorescence microscopy.

    FASEB J, 2018, 32(7):4031-4042. GSK J4 HCl (GSKJ4 HCl) purchased from Selleck.

    GSK-J4 impaired hair cell regeneration after neomycin damage. (A–D) GSK-J4 reduced the numbers of GFP-positive (green) and FM1-43FX-positive (red) hair cells compared with DMSO-treated controls. Scale bars = 10 μm. (E,F) Quantitative analysis of the number of GFP-positive (E) or FM1-43FX-positive (F) hair cells per neuromast (NM) at different time points in DMSO-treated control and GSK-J4-treated larvae. In the 24-h group, n = 40 neuromasts (20 larvae) per group; in the 48-h group, n = 28 neuromasts (14 larvae) per group. ***p < 0.0001. Bars are mean ± sem. [24-h group: One-way ANOVA; GFP-positive cells: F(2, 117) = 96.94; FM1-43FX-positive cells: F(2, 117) = 114. 48-h group: One-way ANOVA; GFP-positive cells: F(2, 81) = 88.96; FM1-43FX-positive cells: F(2, 81) = 93.85].

    Front Mol Neurosci, 2017, doi: 10.3389/fnmol.2017.00051. GSK J4 HCl (GSKJ4 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 M{S5[Wdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NX;nTVJ[OiEQvF2= M3PsemROW09? M1nSS4Fn\mWldIOgZ4VtdCCpcn;3eIg> MYSyOVE{OjV2OR?=
CUTLL1 NULvZoo3SXCxcITvd4l{KGG|c3H5 MWiyJO69VQ>? NXP6[FRETE2VTx?= NHLtfHVqdmS3Y3XzJIFxd3C2b4Ppdy=> M3m4blI2OTN{NUS5
CUTLL1 MlzoSpVv[3Srb36gZZN{[Xl? MXGyJO69VQ>? NXHhZ3MzTE2VTx?= NEfUT2xqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 MmrWNlUyOzJ3NEm=
CUTLL1 NFO5emZMcW6jc3WgZZN{[Xl? NWLKTFRWPiEQvF2= M4Hrd2ROW09? M2HlTIxm[WS|IITvJIlv[3KnYYPl[EBJO0t{N33lNy=> NIPwR2QzPTF|MkW0PS=>
SF7761 MWHLbY5ie2ViYYPzZZk> MVS2JO69VQ>? NWLXUVdbTE2VTx?= MW\pcoNz\WG|ZYOgT|I4KG2ndHj5cIF1cW:w M3Xy[lI2PDBzNkmz
SF8628 MnLKT4lv[XOnIHHzd4F6 MVy2JO69VQ>? M4Hic2ROW09? MlzTbY5kemWjc3XzJGszQCCvZYTofYxifGmxbh?= MofENlU1ODF4OUO=
H3.3 NXjxOmxLU2mwYYPlJIF{e2G7 NYrxSpRVPiEQvF2= MWfEUXNQ NHrQfYhqdmO{ZXHz[ZMhUzJ7IH3leIh6dGG2aX;u NFWwVnozPTRyMU[5Ny=>
SF9012 NYHXVFJ6U2mwYYPlJIF{e2G7 MWC2JO69VQ>? NIDQU3NFVVOR NIHofpRqdmO{ZXHz[ZMhUzNyIH3leIh6dGG2aX;u MXeyOVQxOTZ7Mx?=
SF9402 Mn[2T4lv[XOnIHHzd4F6 NEfkZ|c3KM7:TR?= MVfEUXNQ M1;RTolv[3KnYYPld{BMOzFibXX0bJlt[XSrb36= NWj1VoN5OjV2MEG2PVM>
SF9427 NXLHeWVNU2mwYYPlJIF{e2G7 MUS2JO69VQ>? M{D0cGROW09? NYfOcoNPcW6lcnXhd4V{KEt|MjDt[ZRpgWyjdHnvci=> MnnENlU1ODF4OUO=
human astrocytes MmnTT4lv[XOnIHHzd4F6 NF7HcI03KM7:TR?= M3W0RmROW09? M1H6TYlv[3KnYYPld{BMOzNibXX0bJlt[XSrb36= M{HiVVI2PDBzNkmz
SF7761 MYHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnrhOkDPxE1? NFzIbXpFVVOR M3[5WolvcGmkaYTzJGszP01iZ3zpc41iKGOnbHyg[5Jwf3Sq M4\3RlI2PDBzNkmz
SF8628 MlLHS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1jFZlYh|ryP M3znfmROW09? MlPRbY5pcWKrdIOgT|I5VSCpbHnvcYEh[2WubDDndo94fGh? NXzkfpY{OjV2MEG2PVM>
H3.3 MkfES5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M{n5cFYh|ryP M3jlNGROW09? NXjER4w2cW6qaXLpeJMhUzJ7TTDncIlwdWFiY3XscEBoem:5dHi= M{jLU|I2PDBzNkmz
SF9012 MnT3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYq2JO69VQ>? MXzEUXNQ NXnYXW9KcW6qaXLpeJMhUzNyTTDncIlwdWFiY3XscEBoem:5dHi= MWmyOVQxOTZ7Mx?=
SF9402 M4fvNWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1vyfVYh|ryP M{HzR2ROW09? NIT1OW9qdmirYnn0d{BMOzGPIHfsbY9u[SClZXzsJIdzd3e2aB?= MlPFNlU1ODF4OUO=
SF9427 MYLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnL4OkDPxE1? NX2wWVRuTE2VTx?= M4TPSolvcGmkaYTzJGs{Ok1iZ3zpc41iKGOnbHyg[5Jwf3Sq M1\XNFI2PDBzNkmz
human astrocytes NW\jTnNLT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NH3ad4s3KM7:TR?= MYTEUXNQ MlH4bY5pcWKrdIOgT|M{VSCpbHnvcYEh[2WubDDndo94fGh? NYn5dVVnOjV2MEG2PVM>
TG neurons M3jvRmZ2dmO2aX;uJIF{e2G7 MY[1NEDPxE1? NGLXNHVFVVOR MmX0bY5pcWKrdIOgTHNXNTFicnXhZ5RqfmG2aX;uJIZzd21ic3Xud49zgSCwZYXyc45{ Mn6wNlU2PTJ5MkC=
Th17 M4DF[2Z2dmO2aX;uJIF{e2G7 NFHh[IQ5OCCwTR?= MVXEUXNQ NF3ITYhqdmirYnn0d{Bk\WyuIHTp[oZmemWwdHnheIlwdg>? NHv4WZUzPTh2MEm5Ny=>
β-cells M1nwfmZ2dmO2aX;uJIF{e2G7 MmnoNlAh|ryP NYC0bVh7TE2VTx?= Mm\PZox2dnS|IFnGUu6{NCCLbD2x{tItKGGwZDDUUmbPuS2rbnT1Z4VlKGOqZX3vb4lv\SCpZX7lJIV5eHKnc4Ppc44> NUnT[FJUOjZ3MEWxPVM>
β-cells NU\oSogxTnWwY4Tpc44h[XO|YYm= MmLHNlAh|ryP NGq4W|ZFVVOR MofIbY5lfWOnczFOtk1k\WyuIHT5d4Z2dmO2aX;u MlS4NlY2ODVzOUO=
ESCs MoLlSpVv[3Srb36gZZN{[Xl? NXLzXlBXOS564pEFxtVO NUDRT5h3TE2VTx?= NInkbJdqdmS3Y3XzJGRPSSCmYX3h[4Uh[Wyxbnege4l1cCCjY4TpeoF1cW:wIH;mJJRp\SCGTlGg[IFu[WenIILld5BwdnOn NVXKbndOOjZ5NUmxO|U>
Raw 264.7 MkOySpVv[3Srb36gZZN{[Xl? NUHMdVVXOC56MUmy5qCGyrWP NGTWfWlFVVOR M4TOWolvcGmkaYTzJHRPTi4QsTDwdo9lfWO2aX;u MV[yOlc4PjN4MB?=

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

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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).

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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

If you have any other enquiries, please leave a message.

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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