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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

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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

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    Vendors

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    Expert Reviews

    by SERP
    (on 17 May 2016)
    Cellular Use Rating
    (The reviewer did not leave any public 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