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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1 Customer Review

  • 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.

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 Mnu1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NV7Scld[OiEQvF2= M1XLfWROW09? NIjHUFFi\m[nY4TzJINmdGxiZ4Lve5Rp MlizNlUyOzJ3NEm=
CUTLL1 M1vnW2Fxd3C2b4Ppd{Bie3OjeR?= NUPHV5Q3OiEQvF2= NYjRVI9YTE2VTx?= MoLobY5lfWOnczDhdI9xfG:|aYO= MmnmNlUyOzJ3NEm=
CUTLL1 NI\Vcm5HfW6ldHnvckBie3OjeR?= NWnyWmdbOiEQvF2= NW\KPIl4TE2VTx?= M2\POolv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= MlrSNlUyOzJ3NEm=
CUTLL1 MVXLbY5ie2ViYYPzZZk> NF\CXGo3KM7:TR?= M1HsXWROW09? M2XzZoxm[WS|IITvJIlv[3KnYYPl[EBJO0t{N33lNy=> Mo\HNlUyOzJ3NEm=
SF7761 MY\LbY5ie2ViYYPzZZk> MWG2JO69VQ>? M4naT2ROW09? Ml33bY5kemWjc3XzJGszPyCvZYTofYxifGmxbh?= M1vJPFI2PDBzNkmz
SF8628 MUXLbY5ie2ViYYPzZZk> NGnVbZg3KM7:TR?= MYTEUXNQ M2C5R4lv[3KnYYPld{BMOjhibXX0bJlt[XSrb36= NWftbncxOjV2MEG2PVM>
H3.3 NXLXU|NRU2mwYYPlJIF{e2G7 M4\Bd|Yh|ryP NYHjWHk4TE2VTx?= NWDtfJlPcW6lcnXhd4V{KEt{OTDt[ZRpgWyjdHnvci=> M37ycFI2PDBzNkmz
SF9012 MVnLbY5ie2ViYYPzZZk> MkTVOkDPxE1? MVvEUXNQ Mn;wbY5kemWjc3XzJGs{OCCvZYTofYxifGmxbh?= NUOzT5FoOjV2MEG2PVM>
SF9402 NGi3fGhMcW6jc3WgZZN{[Xl? NXnkZYIxPiEQvF2= NXvhRZg2TE2VTx?= NHq1SYlqdmO{ZXHz[ZMhUzNzIH3leIh6dGG2aX;u NILnNWUzPTRyMU[5Ny=>
SF9427 NWXSU3JHU2mwYYPlJIF{e2G7 NUDae49wPiEQvF2= MlfpSG1UVw>? MkHlbY5kemWjc3XzJGs{OiCvZYTofYxifGmxbh?= NEHQZYgzPTRyMU[5Ny=>
human astrocytes Ml62T4lv[XOnIHHzd4F6 MUW2JO69VQ>? NVrmd3N[TE2VTx?= M3fWWYlv[3KnYYPld{BMOzNibXX0bJlt[XSrb36= M4XFTFI2PDBzNkmz
SF7761 MWDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1rz[VYh|ryP NGe5NmhFVVOR M3OzU4lvcGmkaYTzJGszP01iZ3zpc41iKGOnbHyg[5Jwf3Sq MlPYNlU1ODF4OUO=
SF8628 MoriS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mn\yOkDPxE1? Mn7SSG1UVw>? Ml\4bY5pcWKrdIOgT|I5VSCpbHnvcYEh[2WubDDndo94fGh? M2\zTFI2PDBzNkmz
H3.3 MWfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWHoXHA{PiEQvF2= MX3EUXNQ M3PLW4lvcGmkaYTzJGszQU1iZ3zpc41iKGOnbHyg[5Jwf3Sq MmHYNlU1ODF4OUO=
SF9012 M4rX[Gdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NEXMcZo3KM7:TR?= NU\sSXpGTE2VTx?= NFXHdYVqdmirYnn0d{BMOzCPIHfsbY9u[SClZXzsJIdzd3e2aB?= NGDkUG8zPTRyMU[5Ny=>
SF9402 NEHQZ|VIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1WzcVYh|ryP MoHzSG1UVw>? MlrabY5pcWKrdIOgT|MyVSCpbHnvcYEh[2WubDDndo94fGh? M{TRdFI2PDBzNkmz
SF9427 NEjPdlFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUC2JO69VQ>? NYXRZ2ZkTE2VTx?= NUXzWndGcW6qaXLpeJMhUzN{TTDncIlwdWFiY3XscEBoem:5dHi= M13idVI2PDBzNkmz
human astrocytes NHv6VJBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NV;5SXBlPiEQvF2= NYjmcHNHTE2VTx?= M3XiUolvcGmkaYTzJGs{O01iZ3zpc41iKGOnbHyg[5Jwf3Sq MUiyOVQxOTZ7Mx?=
TG neurons MWjGeY5kfGmxbjDhd5NigQ>? M1POXVUxKM7:TR?= NVSzN5F4TE2VTx?= MYXpcohq[mm2czDIV3YuOSC{ZXHjeIl3[XSrb36g[pJwdSC|ZX7zc5J6KG6ndYLvcpM> NFTjT3gzPTV3MkeyNC=>
Th17 MoTzSpVv[3Srb36gZZN{[Xl? M1LFO|gxKG6P NHzJeXlFVVOR NYXm[mxucW6qaXLpeJMh[2WubDDkbYZn\XKnboTpZZRqd25? NFvKOJYzPTh2MEm5Ny=>
β-cells M1O3TmZ2dmO2aX;uJIF{e2G7 NV7ud4J{OjBizszN MULEUXNQ M1rLdIJtfW62czDJSm7PuyxiSXytNe6zNCCjbnSgWG5H|rFvaX7keYNm\CClaHXtc4tqdmViZ3Xu[UBmgHC{ZYPzbY9v Ml\NNlY2ODVzOUO=
β-cells MoXxSpVv[3Srb36gZZN{[Xl? MWqyNEDPxE1? M2e1eWROW09? M3jpeIlv\HWlZYOg{tIu[2WubDDkfZNnfW6ldHnvci=> NVP1XJpIOjZ3MEWxPVM>
ESCs MoDHSpVv[3Srb36gZZN{[Xl? MmG4NU456oDHwsXN MmDmSG1UVw>? NFvPOJNqdmS3Y3XzJGRPSSCmYX3h[4Uh[Wyxbnege4l1cCCjY4TpeoF1cW:wIH;mJJRp\SCGTlGg[IFu[WenIILld5BwdnOn MXuyOlc2QTF5NR?=
Raw 264.7 NInpXWlHfW6ldHnvckBie3OjeR?= M3i5dVAvQDF7MvMAieK2VQ>? NFziXphFVVOR NIHScHJqdmirYnn0d{BVVkZvzsGgdJJw\HWldHnvci=> NIX1OoszPjd5NkO2NC=>

... 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

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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

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

  • * 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