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KU-60019 | Inhibitor of ATM
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
ATM
  • IC50:6.3 nM
Inhibitor
1-10 uM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - ATR >10 uM, DNA-PK 1.7 uM

Potency Assay Off-Target:
KU-60019 had little to no activity against a panel of 229 protein kinases.

Potency
Cellular
In Vitro

ATM

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

Chemical Information

Molecular Formula C30H33N3O5S
SMILEs C[C@H]1CN(CC(=O)Nc2ccc3c(c2)Cc2cccc(-c4cc(=O)cc(N5CCOCC5)o4)c2S3)C[C@@H](C)O1
InChI InChI=1S/C30H33N3O5S/c1-19-16-32(17-20(2)37-19)18-28(35)31-23-6-7-27-22(13-23)12-21-4-3-5-25(30(21)39-27)26-14-24(34)15-29(38-26)33-8-10-36-11-9-33/h3-7,13-15,19-20H,8-12,16-18H2,1-2H3,(H,31,35)/t19-,20+
Molecular weight 547.21 Da
AlogP 4.2465
HBond acceptors 8
HBond donors 1
Atoms 72

References

Publications

    Cross References

    canSARChEMBLBindingDBGDSC1

    Expert Reviews

    by SERP
    (on 21 Jun 2016 )
    Cellular Use Rating
    In Model Organisms
    This compound has the potential to be a useful probe for ATM. It appears to be potent in an in vitro assay with an IC50 ~6.3 nM. In a kinase panel screen (229 kinases, compound tested at 1 uM), it appears...
    by SERP
    (on 6 Jan 2017 )
    Cellular Use Rating
    In Model Organisms
    KU-60019, alongside the precursor KU-59933, were the prototypical inhibitors of the DNA repair kinase ATM. This compound displays enhanced solubility and selectivity against key off-targets compared...
    by SERP
    (on 4 Nov 2020 )
    Cellular Use Rating
    In Model Organisms
    KU-60019 should be regarded as an unvalidated inhibitor of ATM kinase as no evidence of direct target engagement has been provided (e.g. SPR, CETSA) and although ATM kinase IC50 of 6 nM is reported...
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