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, doi: 10.3389/fnmol.2017.00051. 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 MWLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWCyJO69VQ>? NWO2WmVuTE2VTx?= NHTwe5Fi\m[nY4TzJINmdGxiZ4Lve5Rp MX[yOVE{OjV2OR?=
CUTLL1 NFuxSlJCeG:ydH;zbZMh[XO|YYm= NEnid2MzKM7:TR?= NV7SbGdOTE2VTx?= MnPMbY5lfWOnczDhdI9xfG:|aYO= NVXTdpZYOjVzM{K1OFk>
CUTLL1 NYOyVYk3TnWwY4Tpc44h[XO|YYm= Mme2NkDPxE1? MX\EUXNQ MWHpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 M3fKRVI2OTN{NUS5
CUTLL1 NFLy[YJMcW6jc3WgZZN{[Xl? M1vtZVYh|ryP M1HseGROW09? NXOwfoVmdGWjZIOgeI8hcW6lcnXhd4VlKEh|S{K3cYU{ MUiyOVE{OjV2OR?=
SF7761 NUDTdY5[U2mwYYPlJIF{e2G7 MWK2JO69VQ>? NYOxRWVzTE2VTx?= M{PXWolv[3KnYYPld{BMOjdibXX0bJlt[XSrb36= NUfhcm1kOjV2MEG2PVM>
SF8628 NIq0ZYVMcW6jc3WgZZN{[Xl? NGn0RXE3KM7:TR?= NV3wOVBOTE2VTx?= NV;wZ4FrcW6lcnXhd4V{KEt{ODDt[ZRpgWyjdHnvci=> NFTvVZUzPTRyMU[5Ny=>
H3.3 Mlj1T4lv[XOnIHHzd4F6 M13yelYh|ryP NWTHNZFoTE2VTx?= M4fC[4lv[3KnYYPld{BMOjlibXX0bJlt[XSrb36= MUSyOVQxOTZ7Mx?=
SF9012 NHz1c3VMcW6jc3WgZZN{[Xl? NUXVWo02PiEQvF2= M1zlb2ROW09? NWT6O|JJcW6lcnXhd4V{KEt|MDDt[ZRpgWyjdHnvci=> M3HlTlI2PDBzNkmz
SF9402 M2\YUWtqdmG|ZTDhd5NigQ>? NYrTPWttPiEQvF2= MnnnSG1UVw>? NIHHe5BqdmO{ZXHz[ZMhUzNzIH3leIh6dGG2aX;u M1rGUFI2PDBzNkmz
SF9427 NYHldG9mU2mwYYPlJIF{e2G7 NVHEdpRFPiEQvF2= NWjLO3pJTE2VTx?= MoLUbY5kemWjc3XzJGs{OiCvZYTofYxifGmxbh?= NUDzdWJGOjV2MEG2PVM>
human astrocytes NG\kcI1McW6jc3WgZZN{[Xl? NXjKN4pEPiEQvF2= NGmwOlJFVVOR MoDjbY5kemWjc3XzJGs{OyCvZYTofYxifGmxbh?= NFXqNIMzPTRyMU[5Ny=>
SF7761 MnKyS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3v4eFYh|ryP NHnN[JBFVVOR MUXpcohq[mm2czDLNldOKGeuaX;tZUBk\WyuIHfyc5d1cA>? NHnLeZYzPTRyMU[5Ny=>
SF8628 NWjqNHJ1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmrzOkDPxE1? M{nnVWROW09? NGqzbY9qdmirYnn0d{BMOjiPIHfsbY9u[SClZXzsJIdzd3e2aB?= MYSyOVQxOTZ7Mx?=
H3.3 Mln4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NV;1VokxPiEQvF2= MoPjSG1UVw>? M{fhUolvcGmkaYTzJGszQU1iZ3zpc41iKGOnbHyg[5Jwf3Sq Mom2NlU1ODF4OUO=
SF9012 M2iwbWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXrtUGlMPiEQvF2= NHfEU25FVVOR NW\QSGJFcW6qaXLpeJMhUzNyTTDncIlwdWFiY3XscEBoem:5dHi= MlrpNlU1ODF4OUO=
SF9402 NE\PU4NIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MkHhOkDPxE1? NGPLW4lFVVOR M1uwSIlvcGmkaYTzJGs{OU1iZ3zpc41iKGOnbHyg[5Jwf3Sq MV[yOVQxOTZ7Mx?=
SF9427 Mn;lS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlW1OkDPxE1? M4XIcmROW09? NHLGOJZqdmirYnn0d{BMOzKPIHfsbY9u[SClZXzsJIdzd3e2aB?= M2HESVI2PDBzNkmz
human astrocytes M13SfWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2HsNVYh|ryP NGiydHdFVVOR M1ruXIlvcGmkaYTzJGs{O01iZ3zpc41iKGOnbHyg[5Jwf3Sq MlHDNlU1ODF4OUO=
TG neurons Mn;KSpVv[3Srb36gZZN{[Xl? M4e0blUxKM7:TR?= M{e3XGROW09? Mm\ObY5pcWKrdIOgTHNXNTFicnXhZ5RqfmG2aX;uJIZzd21ic3Xud49zgSCwZYXyc45{ NIjzWpEzPTV3MkeyNC=>
Th17 M3r5fmZ2dmO2aX;uJIF{e2G7 NH36OXc5OCCwTR?= NV23OZhQTE2VTx?= NG\6TlJqdmirYnn0d{Bk\WyuIHTp[oZmemWwdHnheIlwdg>? M1W2blI2QDRyOUmz
β-cells M{DTT2Z2dmO2aX;uJIF{e2G7 NVq5Uml1OjBizszN MUfEUXNQ M1u1ZYJtfW62czDJSm7PuyxiSXytNe6zNCCjbnSgWG5H|rFvaX7keYNm\CClaHXtc4tqdmViZ3Xu[UBmgHC{ZYPzbY9v MYWyOlUxPTF7Mx?=
β-cells NHfwcVFHfW6ldHnvckBie3OjeR?= M2XFdFIxKM7:TR?= NInLdW9FVVOR NXTnepBCcW6mdXPld{DPui2lZXzsJIR6e2[3bnP0bY9v M4nEOlI3PTB3MUmz
ESCs MkGySpVv[3Srb36gZZN{[Xl? NWfZeFMyOS564pEFxtVO NVrBfHhTTE2VTx?= NGnmOYlqdmS3Y3XzJGRPSSCmYX3h[4Uh[Wyxbnege4l1cCCjY4TpeoF1cW:wIH;mJJRp\SCGTlGg[IFu[WenIILld5BwdnOn NIfh[ZczPjd3OUG3OS=>
Raw 264.7 NF7zZllHfW6ldHnvckBie3OjeR?= MlzJNE45OTl{4pEFxtVO NWPYdHk1TE2VTx?= NEfWZ5JqdmirYnn0d{BVVkZvzsGgdJJw\HWldHnvci=> MVmyOlc4PjN4MB?=

... 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:
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

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:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

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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  • Computed Result

  • C1=C0/X C1: LOG(C1):
    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

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