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

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.

    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.

  • 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 M1riVWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NX\TdYx5OiEQvF2= MnezSG1UVw>? Ml;3ZYZn\WO2czDj[YxtKGe{b4f0bC=> NHT0NZozPTF|MkW0PS=>
CUTLL1 MWLBdI9xfG:|aYOgZZN{[Xl? M2G1S|Ih|ryP MV7EUXNQ MYrpcoR2[2W|IHHwc5B1d3Orcx?= MVSyOVE{OjV2OR?=
CUTLL1 NUPaNmFoTnWwY4Tpc44h[XO|YYm= MWKyJO69VQ>? NWTHfZBTTE2VTx?= Mn;rbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= NFPpdXgzPTF|MkW0PS=>
CUTLL1 MXLLbY5ie2ViYYPzZZk> MVq2JO69VQ>? MUfEUXNQ NIrv[Jdt\WGmczD0c{BqdmO{ZXHz[YQhUDONMkft[VM> MoTMNlUyOzJ3NEm=
SF7761 NHnrTnVMcW6jc3WgZZN{[Xl? NH[wfpM3KM7:TR?= M37ae2ROW09? M2fqSolv[3KnYYPld{BMOjdibXX0bJlt[XSrb36= NFPQfFAzPTRyMU[5Ny=>
SF8628 M3L0W2tqdmG|ZTDhd5NigQ>? MV:2JO69VQ>? NGPOOWRFVVOR MnL5bY5kemWjc3XzJGszQCCvZYTofYxifGmxbh?= NEH6coYzPTRyMU[5Ny=>
H3.3 M2S4TGtqdmG|ZTDhd5NigQ>? M1HCWlYh|ryP M2H0TmROW09? MVLpcoNz\WG|ZYOgT|I6KG2ndHj5cIF1cW:w MlXnNlU1ODF4OUO=
SF9012 Mlf4T4lv[XOnIHHzd4F6 MYG2JO69VQ>? MlG1SG1UVw>? MYDpcoNz\WG|ZYOgT|MxKG2ndHj5cIF1cW:w MYSyOVQxOTZ7Mx?=
SF9402 Mly4T4lv[XOnIHHzd4F6 M{OyS|Yh|ryP M1rIWmROW09? MXLpcoNz\WG|ZYOgT|MyKG2ndHj5cIF1cW:w MXWyOVQxOTZ7Mx?=
SF9427 MUnLbY5ie2ViYYPzZZk> NF;HOYk3KM7:TR?= MlK2SG1UVw>? M3\6RYlv[3KnYYPld{BMOzJibXX0bJlt[XSrb36= NHvqPW0zPTRyMU[5Ny=>
human astrocytes MnrRT4lv[XOnIHHzd4F6 MWC2JO69VQ>? MV7EUXNQ MWfpcoNz\WG|ZYOgT|M{KG2ndHj5cIF1cW:w MofLNlU1ODF4OUO=
SF7761 NXPUeFVUT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MlLaOkDPxE1? NGD4bY1FVVOR M4HIXIlvcGmkaYTzJGszP01iZ3zpc41iKGOnbHyg[5Jwf3Sq NFHQclEzPTRyMU[5Ny=>
SF8628 NWr4R4g{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWe2JO69VQ>? NH7uNJRFVVOR MWXpcohq[mm2czDLNlhOKGeuaX;tZUBk\WyuIHfyc5d1cA>? NEXBSY4zPTRyMU[5Ny=>
H3.3 M2Gwfmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGHYNIY3KM7:TR?= NFe1R5ZFVVOR NETUbXZqdmirYnn0d{BMOjmPIHfsbY9u[SClZXzsJIdzd3e2aB?= M3T1NVI2PDBzNkmz
SF9012 NHzmOWFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MmH1OkDPxE1? MWnEUXNQ NHXYOIhqdmirYnn0d{BMOzCPIHfsbY9u[SClZXzsJIdzd3e2aB?= M4DuSFI2PDBzNkmz
SF9402 MV3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnrrOkDPxE1? NXLG[lNnTE2VTx?= MkLTbY5pcWKrdIOgT|MyVSCpbHnvcYEh[2WubDDndo94fGh? MmewNlU1ODF4OUO=
SF9427 NVnaU417T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYXV[ld1PiEQvF2= NVW5cGhGTE2VTx?= MYPpcohq[mm2czDLN|JOKGeuaX;tZUBk\WyuIHfyc5d1cA>? M{[weFI2PDBzNkmz
human astrocytes MXXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MmXEOkDPxE1? MmfMSG1UVw>? NEPaOYZqdmirYnn0d{BMOzOPIHfsbY9u[SClZXzsJIdzd3e2aB?= MVqyOVQxOTZ7Mx?=
TG neurons MlG3SpVv[3Srb36gZZN{[Xl? MoXOOVAh|ryP NGHTUZJFVVOR NUDIWVlIcW6qaXLpeJMhUFOYLUGgdoVi[3SrdnH0bY9vKG[{b32gd4Vve2:{eTDu[ZVzd26| M161XlI2PTV{N{Kw
Th17 MWnGeY5kfGmxbjDhd5NigQ>? M1OyeFgxKG6P M1W3b2ROW09? NX35UpNzcW6qaXLpeJMh[2WubDDkbYZn\XKnboTpZZRqd25? M1;Zd|I2QDRyOUmz
β-cells M3vQd2Z2dmO2aX;uJIF{e2G7 NY\Hc5U1OjBizszN MYXEUXNQ NW\k[5o{[my3boTzJGlHVs7|LDDJcE0y|rJuIHHu[EBVVkcQsT3pcoR2[2WmIHPo[Y1wc2mwZTDn[Y5mKGW6cILld5Nqd25? MnTmNlY2ODVzOUO=
β-cells NEfK[HhHfW6ldHnvckBie3OjeR?= MXuyNEDPxE1? Mn3XSG1UVw>? NGTPUYxqdmS3Y3XzJO6zNWOnbHyg[Jl{\nWwY4Tpc44> M{j0O|I3PTB3MUmz
ESCs NGfIT3pHfW6ldHnvckBie3OjeR?= MmfFNU456oDHwsXN NHLGfZZFVVOR MWXpcoR2[2W|IFTORUBl[W2jZ3WgZYxwdmdid3n0bEBi[3SrdnH0bY9vKG:oIITo[UBFVkFiZHHtZYdmKHKnc4DvcpNm MX:yOlc2QTF5NR?=
Raw 264.7 MXfGeY5kfGmxbjDhd5NigQ>? NXexVGlROC56MUmy5qCGyrWP NELuW3NFVVOR M1LPOYlvcGmkaYTzJHRPTi4QsTDwdo9lfWO2aX;u MoTENlY4PzZ|NkC=

... 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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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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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).

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Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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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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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