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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 public comments)
        by SERP
        (on 7 Jun 2016)
        Cellular Use Rating
        (The reviewer did not leave any public 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