GSK J4 HCl (GSKJ4 HCl)
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.
Cited by 18 Publications
5 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 (GSKJ4 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 (GSKJ4 HCl) purchased from Selleck.
Inhibition of JMJD3 mitigated the IL-1β-induced inflammatory response in the MH7A cells. The MH7A cells were transfected with control or JMJD3 siRNA or treated with the indicated concentrations of GSK-J4 (JMJD3 inhibitor) and were then stimulated with IL-1β for 24 h. Western blot analysis of JMJD3, TLR2, COX-2 and GAPDH expression (d).
Cell Mol Immunol, 2018, doi:10.1038/s41423-018-0037-8. GSK J4 HCl (GSKJ4 HCl) purchased from Selleck.
GSK J4 inhibited PDGF-induced cyclin D1 and PCNA expression. The cells were preincubated for 4 h, with or without 10 mM GSK J4, followed by stimulation with 25 ng/ml PDGF-BB for 36 h. Cells were immunostained with anti-JMJD3 antibodies (green), and nuclei were stained with DAPI (blue) and analyzed by fluorescence microscopy.
FASEB J, 2018, 32(7):4031-4042. GSK J4 HCl (GSKJ4 HCl) purchased from Selleck.
Effects of Kdm6 inhibitors on MPM cellular proliferation and cytokine expression. (A) NCI-H226 MPM cells were exposed to GSK-J1 at various concentrations for 48 h and effects on cellular proliferation were measured using a BrdU incorporation assay (n=3). (B) NCI-H226 and REN MPM cells were exposed to GSK-J4 at various concentrations for 48 h and effects on cellular proliferation were measured using a BrdU incorporation assay (n=3). RT-PCR analysis examining the effects of GSK-J4 on (C) CXCL1, (D) CXCL2 and (E) CXCL8/IL-8 in NCI-H226 cells treated for 24 h with GSK-J4 at a final concentration of 15 μM (n=3). Densitometric analysis following electrophoresis demonstrates significant induction of these pro-inflammatory cytokines/chemokines. Statistical significance was measured using either an unpaired Student's two-tailed t-test, or a one-way ANOVA with Dunnett's post-test (*P<0.05; **P<0.01; ***P<0.001).
Int J Oncol, 2017, 50(3):1044-1052. GSK J4 HCl (GSKJ4 HCl) purchased from Selleck.
Purity & Quality Control
Choose Selective Histone Demethylase Inhibitors
|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.|
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. 
|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(Data is from Selleck tests instead of citations):
2% DMSO+dd H2O
For best results, use promptly after mixing.
* 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.
|CAS No.||1373423-53-0(free base)|
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*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).
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 )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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.
Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.
Frequently Asked Questions
I cannot get a clear solution when I dissolve the compound into water.
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.