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A-196 | A-196 : Inhibitor of KMT5B, KMT5C
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (1 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
KMT5B
  • IC 50:25 nM
  • EC50:740 nM
  • EC50:262 nM
  • EC50:370 nM
KMT5C
  • IC 50:144 nM
    500-1000 nM

    Selectivity

    In Vitro Selectivity Assessment

    Potency: IC50

    Potency Assay Off-Target:
    Scintillation proximity assay. No activity was detected in assays with 29 methyltransferases at 1 or ...
    Selectivity Assessment Description:
    125 non-family targets including kinases, GPCRs, ion channels, and transporters (via Cerep and th ...

    Potency
    Cellular
    In Vitro

    KMT5B

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1038/nchembio.2282

    KMT5C

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1038/nchembio.2282

    Negative Control Compounds

    A-197
    SGC2043
    SMILES: CN(C1CCCC1)C2=NN=C(C3=CC=NC=C3)C4=C2C=C(C(=C4)Cl)Cl

    Chemical Information

    Molecular Formula C18H16Cl2N4
    SMILEs Clc1cc2c(NC3CCCC3)nnc(-c3ccncc3)c2cc1Cl
    InChI InChI=1S/C18H16Cl2N4/c19-15-9-13-14(10-16(15)20)18(22-12-3-1-2-4-12)24-23-17(13)11-5-7-21-8-6-11/h5-10,12H,1-4H2,(H,22,24)
    Molecular weight 358.08 Da
    AlogP 5.353100000000003
    HBond acceptors 4
    HBond donors 1
    Atoms 40

    Vendors

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

    Expert Reviews

    by SERP
    (on 15 Mar 2017)
    Cellular Use Rating
    (The reviewer did not leave any public comments)
    by SERP
    (on 21 Mar 2017)
    Cellular Use Rating
    (The reviewer did not leave any public comments)
    by SERP
    (on 30 Mar 2017)
    Cellular Use Rating
    In Model Organisms
    This probe represents the best in class for SUV420H1 and H2 - hitting the enzymes at 25 and 144 nM, respectively, with selectivity data against a wide panel of related epigenetic and other targets....
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    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