GSK J4 HCl

Catalog No.S7070

GSK J4 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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2 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 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. GSK J4 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 NULiOG1zT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MomzNkDPxE1? MXfEUXNQ M3jXbYFn\mWldIOgZ4VtdCCpcn;3eIg> MnzvNlUyOzJ3NEm=
CUTLL1 NWrtelh2SXCxcITvd4l{KGG|c3H5 MUeyJO69VQ>? NUTibmxwTE2VTx?= MlexbY5lfWOnczDhdI9xfG:|aYO= NG\td3IzPTF|MkW0PS=>
CUTLL1 NVXzZpF[TnWwY4Tpc44h[XO|YYm= MlfMNkDPxE1? NWq1OoNqTE2VTx?= NFTmVpVqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 MUeyOVE{OjV2OR?=
CUTLL1 MlPST4lv[XOnIHHzd4F6 Mn33OkDPxE1? MoDlSG1UVw>? NFG2fI1t\WGmczD0c{BqdmO{ZXHz[YQhUDONMkft[VM> M2f0UFI2OTN{NUS5
SF7761 NFPxdYxMcW6jc3WgZZN{[Xl? NGSwOmw3KM7:TR?= MkXxSG1UVw>? MXvpcoNz\WG|ZYOgT|I4KG2ndHj5cIF1cW:w MYKyOVQxOTZ7Mx?=
SF8628 M2PXS2tqdmG|ZTDhd5NigQ>? MXq2JO69VQ>? MVrEUXNQ MUjpcoNz\WG|ZYOgT|I5KG2ndHj5cIF1cW:w NV;0WXpWOjV2MEG2PVM>
H3.3 NYfEdHBjU2mwYYPlJIF{e2G7 MmfqOkDPxE1? M{f1cmROW09? Ml3WbY5kemWjc3XzJGszQSCvZYTofYxifGmxbh?= MXmyOVQxOTZ7Mx?=
SF9012 NIfucJVMcW6jc3WgZZN{[Xl? NFjFU3U3KM7:TR?= MmLjSG1UVw>? NWO4Tlk{cW6lcnXhd4V{KEt|MDDt[ZRpgWyjdHnvci=> M17pblI2PDBzNkmz
SF9402 M3jjOmtqdmG|ZTDhd5NigQ>? NXTQN4M{PiEQvF2= NY[4Zm5pTE2VTx?= NG\mUFVqdmO{ZXHz[ZMhUzNzIH3leIh6dGG2aX;u MmLrNlU1ODF4OUO=
SF9427 M{nYSGtqdmG|ZTDhd5NigQ>? MUO2JO69VQ>? NGfzT3BFVVOR NYXZTotScW6lcnXhd4V{KEt|MjDt[ZRpgWyjdHnvci=> MU[yOVQxOTZ7Mx?=
human astrocytes NGPiUI5McW6jc3WgZZN{[Xl? M{OwblYh|ryP M1LJOmROW09? MWLpcoNz\WG|ZYOgT|M{KG2ndHj5cIF1cW:w MmTINlU1ODF4OUO=
SF7761 NVXQXJF4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWjPU5hWPiEQvF2= MnTWSG1UVw>? MX7pcohq[mm2czDLNldOKGeuaX;tZUBk\WyuIHfyc5d1cA>? M4DVclI2PDBzNkmz
SF8628 NEX1PFJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1;DeVYh|ryP NV\hTXh1TE2VTx?= MmfmbY5pcWKrdIOgT|I5VSCpbHnvcYEh[2WubDDndo94fGh? MYWyOVQxOTZ7Mx?=
H3.3 NW\s[ZhKT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFSxN2E3KM7:TR?= MmHLSG1UVw>? NIrzXJVqdmirYnn0d{BMOjmPIHfsbY9u[SClZXzsJIdzd3e2aB?= M4TuXFI2PDBzNkmz
SF9012 M2\hU2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2XlcFYh|ryP MWTEUXNQ MkL4bY5pcWKrdIOgT|MxVSCpbHnvcYEh[2WubDDndo94fGh? Ml;vNlU1ODF4OUO=
SF9402 NFPOcGVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3vGeFYh|ryP NYToUVNwTE2VTx?= NH7Lb5hqdmirYnn0d{BMOzGPIHfsbY9u[SClZXzsJIdzd3e2aB?= NFjaeGIzPTRyMU[5Ny=>
SF9427 M3HOVWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3nFOFYh|ryP MoTwSG1UVw>? MUnpcohq[mm2czDLN|JOKGeuaX;tZUBk\WyuIHfyc5d1cA>? NFjRd24zPTRyMU[5Ny=>
human astrocytes NEH2fm9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHnrd203KM7:TR?= M3fac2ROW09? MV3pcohq[mm2czDLN|NOKGeuaX;tZUBk\WyuIHfyc5d1cA>? M1vBTFI2PDBzNkmz
TG neurons M3fWTmZ2dmO2aX;uJIF{e2G7 M3jofFUxKM7:TR?= MXzEUXNQ MX7pcohq[mm2czDIV3YuOSC{ZXHjeIl3[XSrb36g[pJwdSC|ZX7zc5J6KG6ndYLvcpM> MlzGNlU2PTJ5MkC=
Th17 MVLGeY5kfGmxbjDhd5NigQ>? MlHZPFAhdk1? M4G4bmROW09? NV7JOmhNcW6qaXLpeJMh[2WubDDkbYZn\XKnboTpZZRqd25? NV\DVnJlOjV6NEC5PVM>
β-cells NGqxb5VHfW6ldHnvckBie3OjeR?= MkS3NlAh|ryP MnfrSG1UVw>? M2[2doJtfW62czDJSm7PuyxiSXytNe6zNCCjbnSgWG5H|rFvaX7keYNm\CClaHXtc4tqdmViZ3Xu[UBmgHC{ZYPzbY9v Mmf0NlY2ODVzOUO=
β-cells Mn3qSpVv[3Srb36gZZN{[Xl? M{[0NVIxKM7:TR?= Mlu3SG1UVw>? M1fLcYlv\HWlZYOg{tIu[2WubDDkfZNnfW6ldHnvci=> M3vxXVI3PTB3MUmz
ESCs MoPMSpVv[3Srb36gZZN{[Xl? MVOxMljjiIYEtV2= NFTxUGJFVVOR M3u5SIlv\HWlZYOgSG5CKGSjbXHn[UBidG:wZzD3bZRpKGGldHn2ZZRqd25ib3[geIhmKESQQTDkZY1i\2VicnXzdI9ve2V? MWmyOlc2QTF5NR?=
Raw 264.7 MWjGeY5kfGmxbjDhd5NigQ>? NEnmVIgxNjhzOUNihKXDvU1? MkeySG1UVw>? NUnmcnhncW6qaXLpeJMhXE6ILd8xJJBzd2S3Y4Tpc44> NIHKOYszPjd5NkO2NC=>

... 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 individually and in order:
2% DMSO+dd H2O
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
Synonyms N/A

Bio Calculators

Molarity Calculator

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

Mass (g) = Concentration (mol/L) × Volume (L) × 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:

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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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    C2=C1/X C2: LOG(C2):
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    C4=C3/X C4: LOG(C4):
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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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  • * Indicates a Required Field

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