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CPI-360 | CPI-360 : SAM competitive inhibitor of EZH2
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 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
  • IC50:0.07 nM
  • IC50:2.5 nM
  • EC50:56 nM
SAM competitive
50 nM - 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
CPI-360 is 100-fold less potent against EZH1 than EZH2 and showed minimal activity against 30 additi ...
Selectivity Assessment Description:
Not available

Potency
Cellular
In Vitro

EZH2

Mode of Action: SAM competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1016/j.chembiol.2014.09.017

Orthogonal Probes def

GSK343
CPI-1205
EPZ-6438

Chemical Information

Molecular Formula C25H31N3O4
SMILEs COc1cc(C)[nH]c(=O)c1CNC(=O)c1c(C)n([C@H](C)C2CCOCC2)c2ccccc12
InChI InChI=1S/C25H31N3O4/c1-15-13-22(31-4)20(24(29)27-15)14-26-25(30)23-17(3)28(21-8-6-5-7-19(21)23)16(2)18-9-11-32-12-10-18/h5-8,13,16,18H,9-12,14H2,1-4H3,(H,26,30)(H,27,29)/t16-/m1/s1
Molecular weight 437.23 Da
AlogP 0.0
HBond acceptors 7
HBond donors 2
Atoms 63

References

Publications

Cross References

canSARChEMBLBindingDB

Vendors

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Expert Reviews

by SERP
(on 6 Jan 2017 )
Cellular Use Rating
In Model Organisms
The molelcule has excellent selectivity for H3K27Me3 (EZH2) over H3K27Me1 (EZH1) in cells, so this appears to be an excellent orthogonal molecule to existing probes.
by SERP
(on 12 Jan 2017 )
Cellular Use Rating
In Model Organisms
CPI-360 appears to be a potent and selective inhibitor of EZH2 in both biochemical and cellular assays, with selectivity over EZH1 and several other methytransferases. As such, it offers a useful tool...
by SERP
(on 4 Nov 2020 )
Cellular Use Rating
In Model Organisms
This probe has good selectivity and cell activity. However, the discoverers noted that in mice even at the very high subcutaneous dose of 200 mg/kg the "inadequate pharmacological properties of CPI-360...
The compound is very potent. The in vivo dose might need to adjusted when the in vivo exp need to be longer.
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