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A-366 | A-366 : Inhibitor of EHMT2 and EHMT1
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (2 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
EHMT2
  • IC 50:3.6 nM
  • % in:~50 at 3 uM
EHMT1
  • IC 50:38 nM
    Inhibitor
    300 nM - 5 uM

    Selectivity

    In Vitro Selectivity Assessment
    Potency Assay Off-Target:
    A-366 had no significant activity against 21 protein methyltransferases in a scintillation proximity ...
    Selectivity Assessment Description:
    A-366 had no significant activity against 21 protein methyltransferases in a scintillation proximity ...

    Potency
    Cellular
    In Vitro

    EHMT2

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1021/ml400496h

    EHMT1

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1021/ml400496h

    Negative Control Compounds

    DS607

    Orthogonal Probes def

    UNC0638
    BIX-01294
    UNC0642

    Chemical Information

    Molecular Formula C19H27N3O2
    SMILEs COc1cc2c(cc1OCCCN1CCCC1)N=C(N)C21CCC1
    InChI InChI=1S/C19H27N3O2/c1-23-16-12-14-15(21-18(20)19(14)6-4-7-19)13-17(16)24-11-5-10-22-8-2-3-9-22/h12-13H,2-11H2,1H3,(H2,20,21)
    Molecular weight 329.21 Da
    AlogP 2.983900000000001
    HBond acceptors 5
    HBond donors 2
    Atoms 51

    References

    Publications

    Cross References

    Vendors

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    Expert Reviews

    by SERP
    (on 17 May 2016 )
    Cellular Use Rating
    ( The reviewer did not leave any comments )
    by SERP
    (on 18 May 2016 )
    Cellular Use Rating
    In Model Organisms
    Allow 3 days for effect: reduction of H3K9me2 in PC3 cells (IC50 = 100 nM). Use A-366 in parallel with UNC0642 (as an orthogonal control).
    by SERP
    (on 30 May 2016 )
    Cellular Use Rating
    In Model Organisms
    A-366 is a cell active and selective probe that has fewer off target effects than UNC638.
    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