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Chemical Structure| 1373423-53-0 Chemical Structure| 1373423-53-0

Structure of GSK-J4
CAS No.: 1373423-53-0

Chemical Structure| 1373423-53-0

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GSK J4 is a cell permeable prodrug rapidly hydrolyzed by macrophage esterases to GSK-J1, a potent selective jumonji H3K27 demethylase inhibitor and attenuates lipopolysaccharide (LPS)-induced proinflammatory cytokine production in primary human macrophages (IC50 = 9 μM for the inhibition of TNFα release).

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Product Details of GSK-J4

CAS No. :1373423-53-0
Formula : C24H27N5O2
M.W : 417.50
SMILES Code : O=C(OCC)CCNC1=NC(C2=NC=CC=C2)=NC(N3CCC4=CC=CC=C4CC3)=C1
MDL No. :MFCD22683852
InChI Key :WBKCKEHGXNWYMO-UHFFFAOYSA-N
Pubchem ID :71729975

Safety of GSK-J4

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of GSK-J4

epigenetics

Isoform Comparison

Biological Activity

Description
GSK-J4, acting as a robust dual inhibitor of the demethylases JMJD3/KDM6B and UTX/KDM6A with IC50 values of 8.6 μM and 6.6 μM respectively, curbs LPS-induced TNF-α output in human primary macrophages with an IC50 of 9 μM. It effectively maintains H3K27me3 levels in the nucleus, notably reducing the expression of multiple LPS-driven cytokines, including TNF-α.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.40mL

0.48mL

0.24mL

11.98mL

2.40mL

1.20mL

23.95mL

4.79mL

2.40mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

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