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

  • Nat Med, 2015, 21(6):555-9. . GSK J4 HCl purchased from Selleck.

Purity & Quality Control

Choose Selective Histone Demethylase Inhibitors

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 NYWwNoJnT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGXSZnQzKM7:TR?= MWTEUXNQ MVTh[oZm[3S|IHPlcIwh\3Kxd4To MX[yOVE{OjV2OR?=
CUTLL1 NVvifm1kSXCxcITvd4l{KGG|c3H5 M4XEb|Ih|ryP MYXEUXNQ NE\DOmZqdmS3Y3XzJIFxd3C2b4Ppdy=> NFjFdJkzPTF|MkW0PS=>
CUTLL1 NH\SOJpHfW6ldHnvckBie3OjeR?= NUS3NpEyOiEQvF2= MUXEUXNQ NGHFXFBqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 MlfKNlUyOzJ3NEm=
CUTLL1 NUmzWXdkU2mwYYPlJIF{e2G7 MkfmOkDPxE1? M{LjcWROW09? NWTPU5dzdGWjZIOgeI8hcW6lcnXhd4VlKEh|S{K3cYU{ NGDQN48zPTF|MkW0PS=>
SF7761 NXzpfZJ3U2mwYYPlJIF{e2G7 NGCxbWI3KM7:TR?= MWjEUXNQ Mk\4bY5kemWjc3XzJGszPyCvZYTofYxifGmxbh?= MoToNlU1ODF4OUO=
SF8628 MWfLbY5ie2ViYYPzZZk> MmPBOkDPxE1? MkXRSG1UVw>? NF7ZS4xqdmO{ZXHz[ZMhUzJ6IH3leIh6dGG2aX;u MlXONlU1ODF4OUO=
H3.3 MnP6T4lv[XOnIHHzd4F6 MXK2JO69VQ>? M4HkXWROW09? MUDpcoNz\WG|ZYOgT|I6KG2ndHj5cIF1cW:w MWKyOVQxOTZ7Mx?=
SF9012 MYrLbY5ie2ViYYPzZZk> MX22JO69VQ>? NFTIdmpFVVOR MmDDbY5kemWjc3XzJGs{OCCvZYTofYxifGmxbh?= NF\NfVkzPTRyMU[5Ny=>
SF9402 MUHLbY5ie2ViYYPzZZk> M2DtTVYh|ryP M4HGdGROW09? NGfDbG1qdmO{ZXHz[ZMhUzNzIH3leIh6dGG2aX;u NY\qXYIzOjV2MEG2PVM>
SF9427 NHz1c5BMcW6jc3WgZZN{[Xl? NHPLNIs3KM7:TR?= NGPTfGxFVVOR MWfpcoNz\WG|ZYOgT|MzKG2ndHj5cIF1cW:w MkDSNlU1ODF4OUO=
human astrocytes MoS4T4lv[XOnIHHzd4F6 NUfEPIwzPiEQvF2= NYjtXGhxTE2VTx?= MkfTbY5kemWjc3XzJGs{OyCvZYTofYxifGmxbh?= NV;JZW1iOjV2MEG2PVM>
SF7761 MYTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGnicIQ3KM7:TR?= NUXKV3hlTE2VTx?= Mn76bY5pcWKrdIOgT|I4VSCpbHnvcYEh[2WubDDndo94fGh? NF3ZN|AzPTRyMU[5Ny=>
SF8628 Ml;nS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlfnOkDPxE1? MnWxSG1UVw>? MYLpcohq[mm2czDLNlhOKGeuaX;tZUBk\WyuIHfyc5d1cA>? NF7qSJczPTRyMU[5Ny=>
H3.3 Mn3pS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MknsOkDPxE1? MYLEUXNQ Mn63bY5pcWKrdIOgT|I6VSCpbHnvcYEh[2WubDDndo94fGh? MY[yOVQxOTZ7Mx?=
SF9012 NVH5ZWd[T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVO2JO69VQ>? NHnqUlhFVVOR Mnq1bY5pcWKrdIOgT|MxVSCpbHnvcYEh[2WubDDndo94fGh? MoK4NlU1ODF4OUO=
SF9402 NYP1VWt7T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVS2JO69VQ>? NYj4bWxFTE2VTx?= M2n2eolvcGmkaYTzJGs{OU1iZ3zpc41iKGOnbHyg[5Jwf3Sq NXrRe5V{OjV2MEG2PVM>
SF9427 M1TkZ2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NI\JXmQ3KM7:TR?= NIjyZ4ZFVVOR NFm0b|RqdmirYnn0d{BMOzKPIHfsbY9u[SClZXzsJIdzd3e2aB?= MnXJNlU1ODF4OUO=
human astrocytes Mlz2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYf5TZV5PiEQvF2= NIPrWHpFVVOR NFXXNXdqdmirYnn0d{BMOzOPIHfsbY9u[SClZXzsJIdzd3e2aB?= NFf4W2czPTRyMU[5Ny=>
TG neurons M{fBRmZ2dmO2aX;uJIF{e2G7 MmjrOVAh|ryP M4TmZ2ROW09? MmnzbY5pcWKrdIOgTHNXNTFicnXhZ5RqfmG2aX;uJIZzd21ic3Xud49zgSCwZYXyc45{ MWqyOVU2Ojd{MB?=
Th17 NITK[4xHfW6ldHnvckBie3OjeR?= NYjnRo9qQDBibl2= MWLEUXNQ NIS0VIZqdmirYnn0d{Bk\WyuIHTp[oZmemWwdHnheIlwdg>? MXqyOVg1ODl7Mx?=
β-cells M4WxXWZ2dmO2aX;uJIF{e2G7 MojtNlAh|ryP M{Hq[WROW09? NE\Ic5NjdHWwdIOgTWZP|rNuIFnsMVHPuixiYX7kJHRPTs7zLXnu[JVk\WRiY3jlcY9scW6nIHflcoUh\XiycnXzd4lwdg>? MmnRNlY2ODVzOUO=
β-cells MVLGeY5kfGmxbjDhd5NigQ>? MkWyNlAh|ryP MUPEUXNQ MmfMbY5lfWOnczFOtk1k\WyuIHT5d4Z2dmO2aX;u M4SyOFI3PTB3MUmz
ESCs MVrGeY5kfGmxbjDhd5NigQ>? MkfyNU456oDHwsXN MkP6SG1UVw>? NETLVFhqdmS3Y3XzJGRPSSCmYX3h[4Uh[Wyxbnege4l1cCCjY4TpeoF1cW:wIH;mJJRp\SCGTlGg[IFu[WenIILld5BwdnOn NIXPSHYzPjd3OUG3OS=>
Raw 264.7 MYjGeY5kfGmxbjDhd5NigQ>? MnPHNE45OTl{4pEFxtVO M{fUR2ROW09? M2XLRYlvcGmkaYTzJHRPTi4QsTDwdo9lfWO2aX;u M1L4UVI3Pzd4M{[w

... Click to View More Cell Line Experimental Data

Protocol

Solubility (25°C)

In vitro DMSO 90 mg/mL (198.25 mM) warming
Ethanol 90 mg/mL warmed (198.25 mM)
Water <1 mg/mL
In vivo 2% DMSO+dd H2O 10 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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

Molarity Calculator

Molarity Calculator

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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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

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Histone Demethylase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID