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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

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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

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Expert Reviews

by SERP
(on 18 May 2016)
Cellular Use Rating
In Model Organisms
(The reviewer did not leave any public comments)
by SERP
(on 30 May 2016)
Cellular Use Rating
(The reviewer did not leave any public 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