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MS023 | MS023 : Non-competitive Inhibitor of PRMT1, PRMT6, CARM1, PRMT8, PRMT3
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
PRMT1
  • Ki:11 nM
  • IC50:9 nM
PRMT6
  • Ki:0.8 nM
  • IC50:56 nM
CARM1
  • Ki:23 nM
    PRMT8
    • Ki:1.3 nM
      PRMT3
      • Ki:55 nM
        Inhibitor
        5 nM - 2 uM

        Selectivity

        In Vitro Selectivity Assessment
        Potency Assay Off-Target:
        No activity was detected against 25 PKMTs, DNMT or Lysine demethylases up to 10 uM.
        Selectivity Assessment Description:
        No binding activity was detected against 9 methyllysine or methylarginine reader proteins in DSF or ...

        Potency
        Cellular
        In Vitro

        PRMT1

        Mode of Action: Inhibitor

        Structure-Activity-Relationship data available? Yes

        DOI Reference: 10.1021/acschembio.5b00839

        PRMT6

        Mode of Action: Inhibitor

        Structure-Activity-Relationship data available? Yes

        DOI Reference: 10.1021/acschembio.5b00839

        CARM1

        Mode of Action: Inhibitor

        Structure-Activity-Relationship data available? Yes

        DOI Reference: 10.1021/acschembio.5b00839

        PRMT8

        Mode of Action: Inhibitor

        Structure-Activity-Relationship data available? Yes

        DOI Reference: 10.1021/acschembio.5b00839

        PRMT3

        Mode of Action: Inhibitor

        Structure-Activity-Relationship data available? Yes

        DOI Reference: 10.1021/acschembio.5b00839

        Negative Control Compounds

        MS094

        Orthogonal Probes def

        SGC707
        EPZ020411

        Chemical Information

        Molecular Formula C17H25N3O
        SMILEs CC(C)Oc1ccc(-c2c[nH]cc2CN(C)CCN)cc1
        InChI InChI=1S/C17H25N3O/c1-13(2)21-16-6-4-14(5-7-16)17-11-19-10-15(17)12-20(3)9-8-18/h4-7,10-11,13,19H,8-9,12,18H2,1-3H3
        Molecular weight 287.20 Da
        AlogP 2.8594
        HBond acceptors 4
        HBond donors 3
        Atoms 46

        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 31 May 2016 )
        Cellular Use Rating
        ( The reviewer did not leave any comments )
        by SERP
        (on 7 Jun 2016 )
        Cellular Use Rating
        ( The reviewer did not leave any comments )
        by SERP
        (on 7 Jun 2016 )
        Cellular Use Rating
        MS023 is a potent and non-selective inhibitor of Type-1 PRMT's and is structurally related to the PRMT6 inhibitor EPZ020411. MS023 binding to PRMT6 has been confirmed using orthogonal assays, including...

        Portal Comments

        ...

        (last updated: 7 Nov 2023)

        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