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TM-04-176-01 | TM-04-176-01 : ATP competitive inhibitor of PIP4K2C, PIP4K2A, PIP4K2B
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (0 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
PIP4K2C
  • Kd:3.4 nM
    PIP4K2A
    • IC50:2000 ± 450 nM
    PIP4K2B
    • IC50:9400 ± 7100 nM
    ATP competitive
    up to 10 uM

    Selectivity

    In Vitro Selectivity Assessment
    Potency Assay Off-Target:
    KINOMEscan profiling, consisting of 468 kinases at 1 uM. Selective against PI5P4Kβ ACVR2A ACVR2B TGF ...

    Potency
    Cellular
    In Vitro

    PIP4K2C

    Mode of Action: ATP competitive

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1021/acs.jmedchem.0c00227

    PIP4K2A

    Mode of Action: ATP competitive

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1021/acs.jmedchem.0c00227

    PIP4K2B

    Mode of Action: ATP competitive

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1021/acs.jmedchem.0c00227

    Chemical Information

    Molecular Formula C20H17N3O2S
    SMILEs CS(=O)(=O)Nc1ccc(-c2cncc(-c3cccc4[nH]ccc34)c2)cc1
    InChI InChI=1S/C20H17N3O2S/c1-26(24,25)23-17-7-5-14(6-8-17)15-11-16(13-21-12-15)18-3-2-4-20-19(18)9-10-22-20/h2-13,22-23H,1H3
    Molecular weight 363.10 Da
    AlogP 4.268400000000002
    HBond acceptors 5
    HBond donors 2
    Atoms 43

    References

    Publications

    Cross References

    canSARChEMBLBindingDB

    Vendors

    Note: This is not an exhaustive list and does not indicate endorsement by the portal.

    Expert Reviews

    by SERP
    (on 3 Apr 2023 )
    Cellular Use Rating
    Users are cautioned that selectivity data was collected at 1 µM so additional kinases may be inhibited when the compound is used above 1 µM.
    by SERP
    (on 6 Jun 2023 )
    Cellular Use Rating
    The phosphatidylinositol 5-phosphate 4-kinases (PI5P4Ks) play critical roles in regulating numerous cell signalling pathways and thus are are considered attractive therapeutic targets in different human...
    by SERP+
    (on 23 May 2024 )
    Cellular Use Rating
    An orthogonal assay would be nice as in-cellular assay eg. dose-response assay. In-vitro potency insufficient. No cytotoxicity data is available. Very selective compound up to 1 µM.
    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