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 Ml3jS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYqyJO69VQ>? M1vvN2ROW09? MVTh[oZm[3S|IHPlcIwh\3Kxd4To M2e2[lI2OTN{NUS5
CUTLL1 MmTMRZBweHSxc3nzJIF{e2G7 NWX2ZoVJOiEQvF2= NXvOVlRMTE2VTx?= MX\pcoR2[2W|IHHwc5B1d3Orcx?= NH;qfFQzPTF|MkW0PS=>
CUTLL1 MkfiSpVv[3Srb36gZZN{[Xl? NEXFR2kzKM7:TR?= MnrLSG1UVw>? MnzMbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= NIrvXYYzPTF|MkW0PS=>
CUTLL1 NWPsOZpNU2mwYYPlJIF{e2G7 NHXxNpY3KM7:TR?= NU\GPJRETE2VTx?= M2PVV4xm[WS|IITvJIlv[3KnYYPl[EBJO0t{N33lNy=> M4i4SlI2OTN{NUS5
SF7761 MlXCT4lv[XOnIHHzd4F6 NVz2W5poPiEQvF2= MWDEUXNQ NH:yPYFqdmO{ZXHz[ZMhUzJ5IH3leIh6dGG2aX;u NYPBOolQOjV2MEG2PVM>
SF8628 M1\BUmtqdmG|ZTDhd5NigQ>? MWO2JO69VQ>? MVTEUXNQ MXrpcoNz\WG|ZYOgT|I5KG2ndHj5cIF1cW:w MVyyOVQxOTZ7Mx?=
H3.3 M1Ww[WtqdmG|ZTDhd5NigQ>? MoDiOkDPxE1? MnrVSG1UVw>? M1fPUolv[3KnYYPld{BMOjlibXX0bJlt[XSrb36= MVOyOVQxOTZ7Mx?=
SF9012 M4rPb2tqdmG|ZTDhd5NigQ>? M{Lv[|Yh|ryP MlnTSG1UVw>? NGCwNXpqdmO{ZXHz[ZMhUzNyIH3leIh6dGG2aX;u M{WwXlI2PDBzNkmz
SF9402 NI\UN2JMcW6jc3WgZZN{[Xl? MVS2JO69VQ>? NEmwUIFFVVOR NV\WUWZrcW6lcnXhd4V{KEt|MTDt[ZRpgWyjdHnvci=> MVGyOVQxOTZ7Mx?=
SF9427 M17BcWtqdmG|ZTDhd5NigQ>? NHz0Soo3KM7:TR?= MlKxSG1UVw>? MoT5bY5kemWjc3XzJGs{OiCvZYTofYxifGmxbh?= NFXITlMzPTRyMU[5Ny=>
human astrocytes NUTMSXpwU2mwYYPlJIF{e2G7 NV;uV2FoPiEQvF2= MoPFSG1UVw>? MV;pcoNz\WG|ZYOgT|M{KG2ndHj5cIF1cW:w M4PrcVI2PDBzNkmz
SF7761 Ml7US5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFraV2k3KM7:TR?= NVXqWo9UTE2VTx?= M2DmPYlvcGmkaYTzJGszP01iZ3zpc41iKGOnbHyg[5Jwf3Sq MUeyOVQxOTZ7Mx?=
SF8628 NFT5ZXVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NW\QWlNpPiEQvF2= MYHEUXNQ MlPobY5pcWKrdIOgT|I5VSCpbHnvcYEh[2WubDDndo94fGh? NF3UfWgzPTRyMU[5Ny=>
H3.3 MXPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkLTOkDPxE1? NI\WN2JFVVOR Mn[0bY5pcWKrdIOgT|I6VSCpbHnvcYEh[2WubDDndo94fGh? NIjM[lMzPTRyMU[5Ny=>
SF9012 M1rleWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MorOOkDPxE1? NHLYWJJFVVOR MULpcohq[mm2czDLN|BOKGeuaX;tZUBk\WyuIHfyc5d1cA>? M3mxWlI2PDBzNkmz
SF9402 MUPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXXlco86PiEQvF2= M1jPU2ROW09? NF7MUYFqdmirYnn0d{BMOzGPIHfsbY9u[SClZXzsJIdzd3e2aB?= Ml;NNlU1ODF4OUO=
SF9427 MWDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4rPXVYh|ryP NWj0S5U6TE2VTx?= NUP0OJZbcW6qaXLpeJMhUzN{TTDncIlwdWFiY3XscEBoem:5dHi= NGX0UWgzPTRyMU[5Ny=>
human astrocytes MkS4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M336PFYh|ryP MV\EUXNQ MVTpcohq[mm2czDLN|NOKGeuaX;tZUBk\WyuIHfyc5d1cA>? M{XNN|I2PDBzNkmz
TG neurons NVHMUIdITnWwY4Tpc44h[XO|YYm= MlLQOVAh|ryP M4TtNmROW09? NWrqXFFpcW6qaXLpeJMhUFOYLUGgdoVi[3SrdnH0bY9vKG[{b32gd4Vve2:{eTDu[ZVzd26| MonGNlU2PTJ5MkC=
Th17 M3jROGZ2dmO2aX;uJIF{e2G7 M3vhN|gxKG6P NIX3[FJFVVOR M1zYUIlvcGmkaYTzJINmdGxiZHnm[oVz\W62aXH0bY9v M{LmXFI2QDRyOUmz
β-cells NFvrUohHfW6ldHnvckBie3OjeR?= NXPCNo5EOjBizszN MXzEUXNQ NVn3b4gx[my3boTzJGlHVs7|LDDJcE0y|rJuIHHu[EBVVkcQsT3pcoR2[2WmIHPo[Y1wc2mwZTDn[Y5mKGW6cILld5Nqd25? MUGyOlUxPTF7Mx?=
β-cells M4j6XWZ2dmO2aX;uJIF{e2G7 NILsdYMzOCEQvF2= M3O2eGROW09? MYjpcoR2[2W|IN8yMYNmdGxiZInz[pVv[3Srb36= NWf5XXliOjZ3MEWxPVM>
ESCs NFf6b4lHfW6ldHnvckBie3OjeR?= NIHhOnUyNjkkgJZCuW0> NEPL[lRFVVOR NHLDUolqdmS3Y3XzJGRPSSCmYX3h[4Uh[Wyxbnege4l1cCCjY4TpeoF1cW:wIH;mJJRp\SCGTlGg[IFu[WenIILld5BwdnOn MXWyOlc2QTF5NR?=
Raw 264.7 M1\5UWZ2dmO2aX;uJIF{e2G7 MoLvNE45OTl{4pEFxtVO NYnPPIRDTE2VTx?= MULpcohq[mm2czDUUmYu|rFicILv[JVkfGmxbh?= MYWyOlc4PjN4MB?=

... Click to View More Cell Line Experimental Data

Protocol

Solubility (25°C)

In vitro DMSO 90 mg/mL warmed (198.25 mM)
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:

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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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