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 18 Publications

5 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.

  • 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.

  • 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.

  • Effects of Kdm6 inhibitors on MPM cellular proliferation and cytokine expression. (A) NCI-H226 MPM cells were exposed to GSK-J1 at various concentrations for 48 h and effects on cellular proliferation were measured using a BrdU incorporation assay (n=3). (B) NCI-H226 and REN MPM cells were exposed to GSK-J4 at various concentrations for 48 h and effects on cellular proliferation were measured using a BrdU incorporation assay (n=3). RT-PCR analysis examining the effects of GSK-J4 on (C) CXCL1, (D) CXCL2 and (E) CXCL8/IL-8 in NCI-H226 cells treated for 24 h with GSK-J4 at a final concentration of 15 μM (n=3). Densitometric analysis following electrophoresis demonstrates significant induction of these pro-inflammatory cytokines/chemokines. Statistical significance was measured using either an unpaired Student's two-tailed t-test, or a one-way ANOVA with Dunnett's post-test (*P<0.05; **P<0.01; ***P<0.001).

    Int J Oncol, 2017, 50(3):1044-1052. 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 MWfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M{XORVIh|ryP M4PBVGROW09? M3POdYFn\mWldIOgZ4VtdCCpcn;3eIg> NVrVXWVGOjVzM{K1OFk>
CUTLL1 M2C4XmFxd3C2b4Ppd{Bie3OjeR?= MXmyJO69VQ>? MWnEUXNQ MmK5bY5lfWOnczDhdI9xfG:|aYO= MWmyOVE{OjV2OR?=
CUTLL1 MXTGeY5kfGmxbjDhd5NigQ>? NFnVcYQzKM7:TR?= NX[2WFY2TE2VTx?= MUfpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 NEHJfm8zPTF|MkW0PS=>
CUTLL1 NYnldGdYU2mwYYPlJIF{e2G7 MoLuOkDPxE1? Ml22SG1UVw>? NWfOc29ydGWjZIOgeI8hcW6lcnXhd4VlKEh|S{K3cYU{ NHLsTFgzPTF|MkW0PS=>
SF7761 M4nhZmtqdmG|ZTDhd5NigQ>? MXW2JO69VQ>? MVPEUXNQ NGLLfFBqdmO{ZXHz[ZMhUzJ5IH3leIh6dGG2aX;u MlfGNlU1ODF4OUO=
SF8628 NYnuW2UxU2mwYYPlJIF{e2G7 Mmn0OkDPxE1? MWjEUXNQ MUXpcoNz\WG|ZYOgT|I5KG2ndHj5cIF1cW:w Mn\QNlU1ODF4OUO=
H3.3 NVHWfodUU2mwYYPlJIF{e2G7 M4\CWlYh|ryP NXHv[|c4TE2VTx?= MnPibY5kemWjc3XzJGszQSCvZYTofYxifGmxbh?= NIXTSpIzPTRyMU[5Ny=>
SF9012 MmLLT4lv[XOnIHHzd4F6 M2rWTlYh|ryP NXfoSIFlTE2VTx?= MnLKbY5kemWjc3XzJGs{OCCvZYTofYxifGmxbh?= MVqyOVQxOTZ7Mx?=
SF9402 M3PUfmtqdmG|ZTDhd5NigQ>? M2r5elYh|ryP NEm2S21FVVOR NGDDVIhqdmO{ZXHz[ZMhUzNzIH3leIh6dGG2aX;u M4DXe|I2PDBzNkmz
SF9427 NYDCcoNyU2mwYYPlJIF{e2G7 MlHkOkDPxE1? MV;EUXNQ MnS1bY5kemWjc3XzJGs{OiCvZYTofYxifGmxbh?= M{HYdlI2PDBzNkmz
human astrocytes M1LtV2tqdmG|ZTDhd5NigQ>? MV:2JO69VQ>? MoDQSG1UVw>? NWPvVJJrcW6lcnXhd4V{KEt|MzDt[ZRpgWyjdHnvci=> MWmyOVQxOTZ7Mx?=
SF7761 NU\DfYt5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWnJZlhyPiEQvF2= MmHzSG1UVw>? MV3pcohq[mm2czDLNldOKGeuaX;tZUBk\WyuIHfyc5d1cA>? NH\CVpQzPTRyMU[5Ny=>
SF8628 NW\FS3FQT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmHiOkDPxE1? NIL6[HhFVVOR NV3td|EycW6qaXLpeJMhUzJ6TTDncIlwdWFiY3XscEBoem:5dHi= MoLvNlU1ODF4OUO=
H3.3 NE\jU3JIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4j0XlYh|ryP MkP5SG1UVw>? NXPafnNycW6qaXLpeJMhUzJ7TTDncIlwdWFiY3XscEBoem:5dHi= MWSyOVQxOTZ7Mx?=
SF9012 NYniTFVFT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXy2JO69VQ>? M1mzTWROW09? M2TqfolvcGmkaYTzJGs{OE1iZ3zpc41iKGOnbHyg[5Jwf3Sq NF6yTmkzPTRyMU[5Ny=>
SF9402 NUnacWNzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXfxdohYPiEQvF2= M2jrbmROW09? NWjqbVhlcW6qaXLpeJMhUzNzTTDncIlwdWFiY3XscEBoem:5dHi= MnrmNlU1ODF4OUO=
SF9427 MmWzS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYfFc2F2PiEQvF2= NU\pR2R{TE2VTx?= MVXpcohq[mm2czDLN|JOKGeuaX;tZUBk\WyuIHfyc5d1cA>? NW\NUHdyOjV2MEG2PVM>
human astrocytes NV3C[29iT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NIfGV3E3KM7:TR?= MWnEUXNQ M1LsR4lvcGmkaYTzJGs{O01iZ3zpc41iKGOnbHyg[5Jwf3Sq NVy2fWZUOjV2MEG2PVM>
TG neurons NV7tWXltTnWwY4Tpc44h[XO|YYm= NITSN4U2OCEQvF2= MWXEUXNQ NYnlelRXcW6qaXLpeJMhUFOYLUGgdoVi[3SrdnH0bY9vKG[{b32gd4Vve2:{eTDu[ZVzd26| M1LTTlI2PTV{N{Kw
Th17 MX\GeY5kfGmxbjDhd5NigQ>? NIPaOlE5OCCwTR?= NFP4SJdFVVOR M1jwcIlvcGmkaYTzJINmdGxiZHnm[oVz\W62aXH0bY9v NFfNeGszPTh2MEm5Ny=>
β-cells MmPCSpVv[3Srb36gZZN{[Xl? NI\H[JYzOCEQvF2= MoHlSG1UVw>? M4WxNoJtfW62czDJSm7PuyxiSXytNe6zNCCjbnSgWG5H|rFvaX7keYNm\CClaHXtc4tqdmViZ3Xu[UBmgHC{ZYPzbY9v M1LlblI3PTB3MUmz
β-cells NFTRWpZHfW6ldHnvckBie3OjeR?= MU[yNEDPxE1? NHPGOplFVVOR M2PFWolv\HWlZYOg{tIu[2WubDDkfZNnfW6ldHnvci=> NG\MOHUzPjVyNUG5Ny=>
ESCs NV;mNHN7TnWwY4Tpc44h[XO|YYm= MX2xMljjiIYEtV2= M17Pb2ROW09? NXXLTGZOcW6mdXPld{BFVkFiZHHtZYdmKGGub37nJJdqfGhiYXP0bZZifGmxbjDv[kB1cGViRF7BJIRidWGpZTDy[ZNxd26|ZR?= M1\UT|I3PzV7MUe1
Raw 264.7 NV;6V5FYTnWwY4Tpc44h[XO|YYm= MoHCNE45OTl{4pEFxtVO MYjEUXNQ MV3pcohq[mm2czDUUmYu|rFicILv[JVkfGmxbh?= M2\QeFI3Pzd4M{[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 (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

Bio Calculators

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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