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E7449 | Inhibitor of PARP1, PARP2, TNKS, TNKS2
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 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
PARP1
  • IC50:1.0 nM
PARP2
  • IC50:1.2 nM
TNKS
  • IC50:115 nM
TNKS2
    Inhibitor
    Up to 1 uM

    Selectivity

    In Vitro Selectivity Assessment
    Potency Assay Off-Target:
    In PARylation assays with human PARPs, E7449 was only active against PARP1, PARP2, TNKS, and TNKS2.

    Potency
    Cellular
    In Vitro

    PARP1

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.18632/oncotarget.5846

    PARP2

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.18632/oncotarget.5846

    TNKS

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.18632/oncotarget.5846

    TNKS2

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.18632/oncotarget.5846

    In Vivo Validations

    Mouse
    Dose: 30-100 mg/kg
    Route of delivery: Oral
    Organ of interest (O): hair follicle, tumor xenograft

    DOI Reference: 10.18632/oncotarget.5846

    Orthogonal Probes def

    Olaparib
    Talazoparib
    AZ6102

    Chemical Information

    Molecular Formula C18H15N5O
    SMILEs O=c1[nH]nc2[nH]c(CN3Cc4ccccc4C3)nc3cccc1c32
    InChI InChI=1S/C18H15N5O/c24-18-13-6-3-7-14-16(13)17(21-22-18)20-15(19-14)10-23-8-11-4-1-2-5-12(11)9-23/h1-7H,8-10H2,(H,22,24)(H,19,20,21)
    Molecular weight 317.13 Da
    AlogP 2.3944
    HBond acceptors 6
    HBond donors 2
    Atoms 39

    References

    Publications

    Cross References

    Vendors

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

    Expert Reviews

    by SERP
    (on 8 Sept 2016 )
    Cellular Use Rating
    In Model Organisms
    E7449 is a potent inhibitor of PARP1 and PARP2 (IC50: 1-2 nM), which, unlike many other PARP inhibitors also has significant activity against Tankyrases 1 and 2 (ca. 100 nM). It has been extensively...
    by SERP
    (on 3 Jan 2017 )
    Cellular Use Rating
    In Model Organisms
    Users should be aware that this compound will trap PARP on DNA, a property not all PARP inhibitors possess. Compounds are reported to have good selelctivity over PARP3 and PARP6-16, with PARP4 described...
    by SERP
    (on 29 Jul 2017 )
    Cellular Use Rating
    In Model Organisms
    The probe appears to be selective against other PARPs and the on-target pharmacology is well-characterized, but there are no data regarding broader off-target profiling - this should be better understood...
    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