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GSK591 | GSK591 : Inhibitor of PRMT5
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

Targets Biochemical/Biophysical Potency Cellular Potency
PRMT5
  • IC50:4 nM
  • IC50:3 nM
Inhibitor
10 nM - 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
No inhibition of 20 Protein methyltransferases at 50 uM (PRMT8, PRMT1, PRMT3, PRMT6, PRMT7, CARM1, D ...
Selectivity Assessment Description:
Unknown

Potency
Cellular
In Vitro

PRMT5

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

Orthogonal Probes def

EPZ015666
DS-437

Chemical Information

Molecular Formula C22H28N4O2
SMILEs O=C(NC[C@H](O)CN1CCc2ccccc2C1)c1ccnc(NC2CCC2)c1
InChI InChI=1S/C22H28N4O2/c27-20(15-26-11-9-16-4-1-2-5-18(16)14-26)13-24-22(28)17-8-10-23-21(12-17)25-19-6-3-7-19/h1-2,4-5,8,10,12,19-20,27H,3,6-7,9,11,13-15H2,(H,23,25)(H,24,28)/t20-/m0/s1
Molecular weight 380.22 Da
AlogP 2.1949999999999985
HBond acceptors 6
HBond donors 3
Atoms 56

References

Publications

    Cross References

    GDSC2

    Vendors

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

    Expert Reviews

    by SERP
    (on 18 May 2016 )
    Cellular Use Rating
    In Model Organisms
    ( The reviewer did not leave any comments )
    by SERP
    (on 30 May 2016 )
    Cellular Use Rating
    ( The reviewer did not leave any comments )
    by SERP
    (on 4 Jun 2016 )
    Cellular Use Rating
    GSK591 is an excellent probe to investigate PRMT5 function in cells. For in vivo work, EPZ015666 is a more suitable compound.
    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