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EPZ005687 | EPZ005687 : SAM competitive of EZH2
RATINGS:
Cellular Use: (2 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 (Mutant:EZH2 WT, EZH2 Y641F, EZH2 A677G)
  • Ki:24 ± 7 nM
  • IC50:54 ± 5 nM
  • IC50:80 ± 30 nM
SAM competitive
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
EPZ005687 showed ∼50-fold selectivity for EZH2 over EZH1-containing PRC2. EPZ005687 was tested again ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
5.6 µM
Selectivity Assessment Description:
Western blot assessing different histone marks; histones were isolated from cells after treatment w ...

Potency
Cellular
In Vitro

EZH2 (Mutant:EZH2 WT, EZH2 Y641F, EZH2 A677G)

Mode of Action: SAM competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1038/nchembio.1084

Orthogonal Probes def

CPI-360
CPI-1205
JQEZ5

Chemical Information

Molecular Formula C32H37N5O3
SMILEs Cc1cc(C)c(CNC(=O)c2cc(-c3ccc(CN4CCOCC4)cc3)cc3c2cnn3C2CCCC2)c(O)n1
InChI InChI=1S/C32H37N5O3/c1-21-15-22(2)35-32(39)28(21)18-33-31(38)27-16-25(17-30-29(27)19-34-37(30)26-5-3-4-6-26)24-9-7-23(8-10-24)20-36-11-13-40-14-12-36/h7-10,15-17,19,26H,3-6,11-14,18,20H2,1-2H3,(H,33,38)(H,35,39)
Molecular weight 539.29 Da
AlogP 0.0
HBond acceptors 8
HBond donors 2
Atoms 77

References

Publications

Cross References

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Expert Reviews

by SERP
(on 2 Feb 2023 )
Cellular Use Rating
( The reviewer did not leave any comments )
by SERP+
(on 17 Jun 2024 )
Cellular Use Rating
This is a highly selective probe with a high potency in biochemical assays as well as in lymphoma cell lines. The probe shows a dose depended efficacy on mutated lymphoma cell lines but spares the wild...
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