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GSK-J4 | GSK-J4 : Inhibitor Prodrug of KDM6A and KDM6B
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (1 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
KDM6A
      KDM6B
      • IC 50:60 nM
      • IC 50:9000 nM
      Prodrug
      1 nM - 5 uM

      Selectivity

      In Vitro Selectivity Assessment

      Potency: IC50 - KDM5B 950 nM, KDM5C 1760 nM

      Potency Assay Off-Target:
      Inactive against additional demethylases in thermal shift, MS and antibody-based assays
      Selectivity Assessment Description:
      Inactive against additional demethylases in thermal shift, MS and antibody-based assays. GSK-J1 had ...

      Potency
      Cellular
      In Vitro

      KDM6A

      Mode of Action: Prodrug

      Structure-Activity-Relationship data available? Yes

      DOI Reference: 10.1038/nature11262

      KDM6B

      Mode of Action: Prodrug

      Structure-Activity-Relationship data available? Yes

      DOI Reference: 10.1038/nature11262

      Negative Control Compounds

      GSK-J5

      Chemical Information

      Molecular Formula C24H27N5O2
      SMILEs CCOC(=O)CCNc1cc(N2CCc3ccccc3CC2)nc(-c2ccccn2)n1
      InChI InChI=1S/C24H27N5O2/c1-2-31-23(30)10-14-26-21-17-22(28-24(27-21)20-9-5-6-13-25-20)29-15-11-18-7-3-4-8-19(18)12-16-29/h3-9,13,17H,2,10-12,14-16H2,1H3,(H,26,27,28)
      Molecular weight 417.22 Da
      AlogP 0.0
      HBond acceptors 7
      HBond donors 1
      Atoms 58

      Expert Reviews

      by SERP
      (on 14 Jun 2016)
      Cellular Use Rating
      I could not find a broad selectivity assessment of GSK-J4 or its active carboxylic acid form. A broader assessment of the ester prodrug and the carboxylate is necessary before using this compound as...
      by SERP
      (on 20 Jun 2016)
      Cellular Use Rating
      GSK-J4 is the ester prodrug of the active (acid) component GSK-J1. The ester is designed to facilitate entry into cells where it is rapidly hydrolysed to the active acid and studies from the authors...
      by SERP
      (on 16 Nov 2020)
      Cellular Use Rating
      In Model Organisms
      Tested in mice at 5mg/kg delivery by i.p. injection (https://doi.org/10.1093/hmg/ddu376) as well as at 0.5mg/kg by i.p injection ( 10.1186/s13075-018-1560-9) therefore recommend 0.5-5 mg/kg i.p. in...
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