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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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 M1[4cmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3PBRlIh|ryP MUTEUXNQ NH[5PJFi\m[nY4TzJINmdGxiZ4Lve5Rp NGD0XYUzPTF|MkW0PS=>
CUTLL1 MYnBdI9xfG:|aYOgZZN{[Xl? NVrJSnVsOiEQvF2= NFzKNWJFVVOR MX7pcoR2[2W|IHHwc5B1d3Orcx?= M13ie|I2OTN{NUS5
CUTLL1 M4DiV2Z2dmO2aX;uJIF{e2G7 M1T3SFIh|ryP NH:4eJNFVVOR MoPjbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= MnPNNlUyOzJ3NEm=
CUTLL1 NEXnPYpMcW6jc3WgZZN{[Xl? NEPN[HE3KM7:TR?= NEewNJJFVVOR M{\kVoxm[WS|IITvJIlv[3KnYYPl[EBJO0t{N33lNy=> M3n2OVI2OTN{NUS5
SF7761 M1PXeGtqdmG|ZTDhd5NigQ>? Mkm0OkDPxE1? NEnSXnhFVVOR NFfMTphqdmO{ZXHz[ZMhUzJ5IH3leIh6dGG2aX;u NU\4UWhqOjV2MEG2PVM>
SF8628 M{fkSWtqdmG|ZTDhd5NigQ>? M2jQTlYh|ryP M{ntR2ROW09? NFf5W3NqdmO{ZXHz[ZMhUzJ6IH3leIh6dGG2aX;u NHLpc2UzPTRyMU[5Ny=>
H3.3 NUL4NIJYU2mwYYPlJIF{e2G7 NXHlOINrPiEQvF2= MlnjSG1UVw>? MWLpcoNz\WG|ZYOgT|I6KG2ndHj5cIF1cW:w MXGyOVQxOTZ7Mx?=
SF9012 MVnLbY5ie2ViYYPzZZk> MVm2JO69VQ>? NFfnN|BFVVOR Mk\pbY5kemWjc3XzJGs{OCCvZYTofYxifGmxbh?= Mn[1NlU1ODF4OUO=
SF9402 NUfLVo1yU2mwYYPlJIF{e2G7 NYDLWYxYPiEQvF2= M3XTcGROW09? Mlm4bY5kemWjc3XzJGs{OSCvZYTofYxifGmxbh?= NGf1OnQzPTRyMU[5Ny=>
SF9427 MWLLbY5ie2ViYYPzZZk> M16wWVYh|ryP NX;uSHB4TE2VTx?= M1rJWIlv[3KnYYPld{BMOzJibXX0bJlt[XSrb36= NIezcXgzPTRyMU[5Ny=>
human astrocytes MUjLbY5ie2ViYYPzZZk> NUjXOpNVPiEQvF2= Mnq4SG1UVw>? NIjxTGFqdmO{ZXHz[ZMhUzN|IH3leIh6dGG2aX;u MlXwNlU1ODF4OUO=
SF7761 NITvVG5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVW2JO69VQ>? NV;3cVVHTE2VTx?= NFTNc3FqdmirYnn0d{BMOjePIHfsbY9u[SClZXzsJIdzd3e2aB?= MoK0NlU1ODF4OUO=
SF8628 M2LzOWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmW0OkDPxE1? NVnacJg2TE2VTx?= MV7pcohq[mm2czDLNlhOKGeuaX;tZUBk\WyuIHfyc5d1cA>? MVuyOVQxOTZ7Mx?=
H3.3 MWXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXzXeWI1PiEQvF2= NXj0[FZNTE2VTx?= NYLmZ2JvcW6qaXLpeJMhUzJ7TTDncIlwdWFiY3XscEBoem:5dHi= NYTxV|FYOjV2MEG2PVM>
SF9012 NIjKXXdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXexVYZWPiEQvF2= M17vOmROW09? NYD5cIx3cW6qaXLpeJMhUzNyTTDncIlwdWFiY3XscEBoem:5dHi= MX2yOVQxOTZ7Mx?=
SF9402 M2n2XGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NIDVbJM3KM7:TR?= MWjEUXNQ NXLUeJN5cW6qaXLpeJMhUzNzTTDncIlwdWFiY3XscEBoem:5dHi= MUSyOVQxOTZ7Mx?=
SF9427 NH\mO|hIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2fWc|Yh|ryP MVPEUXNQ NXPONoJScW6qaXLpeJMhUzN{TTDncIlwdWFiY3XscEBoem:5dHi= NHj6S28zPTRyMU[5Ny=>
human astrocytes NHuzcHFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVK2JO69VQ>? NEDS[WhFVVOR NIjudIhqdmirYnn0d{BMOzOPIHfsbY9u[SClZXzsJIdzd3e2aB?= MVOyOVQxOTZ7Mx?=
TG neurons MX3GeY5kfGmxbjDhd5NigQ>? MnzhOVAh|ryP NUjzUHBmTE2VTx?= NXvEUnlucW6qaXLpeJMhUFOYLUGgdoVi[3SrdnH0bY9vKG[{b32gd4Vve2:{eTDu[ZVzd26| MXSyOVU2Ojd{MB?=
Th17 MnLISpVv[3Srb36gZZN{[Xl? NGLNfXM5OCCwTR?= NVzwRXp7TE2VTx?= MVfpcohq[mm2czDj[YxtKGSrZn\ldoVvfGmjdHnvci=> M4KxPVI2QDRyOUmz
β-cells M1TnPGZ2dmO2aX;uJIF{e2G7 NVzQd3NmOjBizszN MnjoSG1UVw>? NY[2S2xS[my3boTzJGlHVs7|LDDJcE0y|rJuIHHu[EBVVkcQsT3pcoR2[2WmIHPo[Y1wc2mwZTDn[Y5mKGW6cILld5Nqd25? MWKyOlUxPTF7Mx?=
β-cells NFHsW45HfW6ldHnvckBie3OjeR?= MYqyNEDPxE1? NGfmRXZFVVOR MV\pcoR2[2W|IN8yMYNmdGxiZInz[pVv[3Srb36= MUmyOlUxPTF7Mx?=
ESCs MkfCSpVv[3Srb36gZZN{[Xl? M{TMcFEvQOLChdM1US=> M2n1XGROW09? MXrpcoR2[2W|IFTORUBl[W2jZ3WgZYxwdmdid3n0bEBi[3SrdnH0bY9vKG:oIITo[UBFVkFiZHHtZYdmKHKnc4DvcpNm MmnmNlY4PTlzN{W=
Raw 264.7 Mm\ySpVv[3Srb36gZZN{[Xl? MoniNE45OTl{4pEFxtVO Mmq1SG1UVw>? M132UolvcGmkaYTzJHRPTi4QsTDwdo9lfWO2aX;u MYiyOlc4PjN4MB?=

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

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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