Chemical Probes logo
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
Download

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

      Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-3-yl)pyrimidin-4-yl)amino)propanoate

      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...
      Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria