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GSK343 | GSK343 : SAM competitive inhibitor of EZH2
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
EZH2
  • Ki:1.2 nM
  • IC50:174 nM
SAM competitive
100 nM - 3 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
EZH2 IC50 = 0.004 uM; SET7 IC50 = 63 uM; PRMT3 IC50 = 74 uM; All others IC50 > 100 uM (DNMT1, DNMT ...

Potency
Cellular
In Vitro

EZH2

Mode of Action: SAM competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/ml3003346

Orthogonal Probes def

UNC1999
EPZ-6438
EPZ011989

Chemical Information

Molecular Formula C31H39N7O2
SMILEs CCCc1cc(C)[nH]c(=O)c1CNC(=O)c1cc(-c2ccnc(N3CCN(C)CC3)c2)cc2c1cnn2C(C)C
InChI InChI=1S/C31H39N7O2/c1-6-7-23-14-21(4)35-31(40)26(23)18-33-30(39)25-15-24(16-28-27(25)19-34-38(28)20(2)3)22-8-9-32-29(17-22)37-12-10-36(5)11-13-37/h8-9,14-17,19-20H,6-7,10-13,18H2,1-5H3,(H,33,39)(H,35,40)
Molecular weight 541.32 Da
AlogP 4.31022
HBond acceptors 9
HBond donors 2
Atoms 79

Vendors

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Expert Reviews

by SERP
(on 17 May 2016 )
Cellular Use Rating
( The reviewer did not leave any comments )
by SERP
(on 18 May 2016 )
Cellular Use Rating
GSK343 is an excellent potent and selective EZH2 probe suitable for cell culture. Use in animals is limited due to it being PgP substrate.
by SERP
(on 30 May 2016 )
Cellular Use Rating
The IC50 is ~300 nM for reduction of H3K37me3 in HCC1806 cells. Use GSK343 in parallel with UNC1999 as an orthogonal probe.

Portal Comments

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(last updated: 7 Nov 2023)

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