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 MlriS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NInwOVUzKM7:TR?= NXexSZZlTE2VTx?= NInVUo9i\m[nY4TzJINmdGxiZ4Lve5Rp M2jLXFI2OTN{NUS5
CUTLL1 MlPWRZBweHSxc3nzJIF{e2G7 NUj3WW5SOiEQvF2= MXXEUXNQ NUXuVpJ2cW6mdXPld{BieG:ydH;zbZM> NGL5NWEzPTF|MkW0PS=>
CUTLL1 MVXGeY5kfGmxbjDhd5NigQ>? M3TGSlIh|ryP MonVSG1UVw>? NVvt[oRbcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> NX7nR2NwOjVzM{K1OFk>
CUTLL1 MXfLbY5ie2ViYYPzZZk> M2LvWFYh|ryP MVPEUXNQ NVGzWHZwdGWjZIOgeI8hcW6lcnXhd4VlKEh|S{K3cYU{ NGDXfmczPTF|MkW0PS=>
SF7761 NHLrUlBMcW6jc3WgZZN{[Xl? M3T6[lYh|ryP M1nzU2ROW09? M{XtO4lv[3KnYYPld{BMOjdibXX0bJlt[XSrb36= MmrFNlU1ODF4OUO=
SF8628 M2rHdGtqdmG|ZTDhd5NigQ>? MlnkOkDPxE1? MUHEUXNQ MYXpcoNz\WG|ZYOgT|I5KG2ndHj5cIF1cW:w MVGyOVQxOTZ7Mx?=
H3.3 MUfLbY5ie2ViYYPzZZk> MVe2JO69VQ>? Ml3JSG1UVw>? MoW1bY5kemWjc3XzJGszQSCvZYTofYxifGmxbh?= NWTWNZRiOjV2MEG2PVM>
SF9012 NIHjclNMcW6jc3WgZZN{[Xl? NYi5[JE2PiEQvF2= MWDEUXNQ NES5WWdqdmO{ZXHz[ZMhUzNyIH3leIh6dGG2aX;u Ml3hNlU1ODF4OUO=
SF9402 NF\F[HJMcW6jc3WgZZN{[Xl? NXHhc5VPPiEQvF2= NILRPZJFVVOR M1;3UYlv[3KnYYPld{BMOzFibXX0bJlt[XSrb36= M3PvdVI2PDBzNkmz
SF9427 NXTQNYdKU2mwYYPlJIF{e2G7 M4nqS|Yh|ryP M3HPOWROW09? MUHpcoNz\WG|ZYOgT|MzKG2ndHj5cIF1cW:w M3e0[lI2PDBzNkmz
human astrocytes NGLJc5lMcW6jc3WgZZN{[Xl? NV;iNopLPiEQvF2= NYLnVFNwTE2VTx?= MVPpcoNz\WG|ZYOgT|M{KG2ndHj5cIF1cW:w NWXLbY1TOjV2MEG2PVM>
SF7761 NH34SXdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NIfu[Fk3KM7:TR?= NFPBU3pFVVOR M37WO4lvcGmkaYTzJGszP01iZ3zpc41iKGOnbHyg[5Jwf3Sq M3z4SFI2PDBzNkmz
SF8628 M120cmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4[5V|Yh|ryP MYLEUXNQ MULpcohq[mm2czDLNlhOKGeuaX;tZUBk\WyuIHfyc5d1cA>? M2[3[FI2PDBzNkmz
H3.3 MYDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NV3BdFY4PiEQvF2= NEj1cWVFVVOR M{DOOYlvcGmkaYTzJGszQU1iZ3zpc41iKGOnbHyg[5Jwf3Sq NWmxW5ZPOjV2MEG2PVM>
SF9012 M2ntOGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NUCxXpd3PiEQvF2= MknlSG1UVw>? M2qzTYlvcGmkaYTzJGs{OE1iZ3zpc41iKGOnbHyg[5Jwf3Sq MWqyOVQxOTZ7Mx?=
SF9402 NWXPc5N1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4OyeVYh|ryP NIjibVFFVVOR MoDEbY5pcWKrdIOgT|MyVSCpbHnvcYEh[2WubDDndo94fGh? M2fnNVI2PDBzNkmz
SF9427 M{C2[2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NF\6N4g3KM7:TR?= M3TKN2ROW09? M1u4OYlvcGmkaYTzJGs{Ok1iZ3zpc41iKGOnbHyg[5Jwf3Sq NHXQd|YzPTRyMU[5Ny=>
human astrocytes MVPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3HnPFYh|ryP NYHZbm5jTE2VTx?= NV\we5pxcW6qaXLpeJMhUzN|TTDncIlwdWFiY3XscEBoem:5dHi= NXHwR49LOjV2MEG2PVM>
TG neurons NGjGW4dHfW6ldHnvckBie3OjeR?= MX21NEDPxE1? M4HY[GROW09? MnPDbY5pcWKrdIOgTHNXNTFicnXhZ5RqfmG2aX;uJIZzd21ic3Xud49zgSCwZYXyc45{ NYe3fFlrOjV3NUK3NlA>
Th17 M323emZ2dmO2aX;uJIF{e2G7 NIT6OYs5OCCwTR?= MV;EUXNQ NHPPSnhqdmirYnn0d{Bk\WyuIHTp[oZmemWwdHnheIlwdg>? NXTKbJhpOjV6NEC5PVM>
β-cells MYrGeY5kfGmxbjDhd5NigQ>? MYWyNEDPxE1? M2qwUmROW09? NFzudlVjdHWwdIOgTWZP|rNuIFnsMVHPuixiYX7kJHRPTs7zLXnu[JVk\WRiY3jlcY9scW6nIHflcoUh\XiycnXzd4lwdg>? M{[zclI3PTB3MUmz
β-cells NETqU49HfW6ldHnvckBie3OjeR?= NXXhdIpIOjBizszN MnPBSG1UVw>? NFXaVlVqdmS3Y3XzJO6zNWOnbHyg[Jl{\nWwY4Tpc44> NV65eYQ6OjZ3MEWxPVM>
ESCs MXfGeY5kfGmxbjDhd5NigQ>? M3rsPVEvQOLChdM1US=> NXHSUGViTE2VTx?= M2DHWYlv\HWlZYOgSG5CKGSjbXHn[UBidG:wZzD3bZRpKGGldHn2ZZRqd25ib3[geIhmKESQQTDkZY1i\2VicnXzdI9ve2V? MWSyOlc2QTF5NR?=
Raw 264.7 M374b2Z2dmO2aX;uJIF{e2G7 NEnMZZoxNjhzOUNihKXDvU1? Ml;5SG1UVw>? NVjrN|FjcW6qaXLpeJMhXE6ILd8xJJBzd2S3Y4Tpc44> MU[yOlc4PjN4MB?=

... 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

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):
    C3=C2/X C3: LOG(C3):
    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.

Related Antibodies

Histone Demethylase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID