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CPI-1205 | CPI-1205 : 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
  • IC50:2 nM
  • EC50:32 nM
SAM competitive
45 nM up to 1 uM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - EZH1: 52 nM

Potency Assay Off-Target:
CPI-1205 was selective for EZH2 over 30 additional protein and DNA methyltransferases.
Selectivity Assessment Description:
CPI-1205 had limited activity against P450 enzymes as well as 54 transporters, receptors and ion ...

Potency
Cellular
In Vitro

EZH2

Mode of Action: SAM competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.6b01315

In Vivo Validations

Mouse
Dose: 1 mg/kg (IV), 100 mg/kg (PO)
Route of delivery: Intravenous, Oral
Plasma half life: 0.402 h (IV)
Systemic clearance: 2.16 L/h/kg (IV)
Organ of interest (O): Karpas-422 xenograft
Target engagement assay: CPI-1205 decreased H3K27me3 levels in tumor tissue.

DOI Reference: 10.1021/acs.jmedchem.6b01315

Orthogonal Probes def

CPI-360
GSK343
EPZ-6438

Chemical Information

Molecular Formula C27H33F3N4O3
SMILEs COc1cc(C)[nH]c(=O)c1CNC(=O)c1c(C)n([C@H](C)C2CCN(CC(F)(F)F)CC2)c2ccccc12
InChI InChI=1S/C27H33F3N4O3/c1-16-13-23(37-4)21(25(35)32-16)14-31-26(36)24-18(3)34(22-8-6-5-7-20(22)24)17(2)19-9-11-33(12-10-19)15-27(28,29)30/h5-8,13,17,19H,9-12,14-15H2,1-4H3,(H,31,36)(H,32,35)/t17-/m1/s1
Molecular weight 518.25 Da
AlogP 4.72034
HBond acceptors 7
HBond donors 2
Atoms 70

References

Publications

Cross References

canSARChEMBLBindingDB

Vendors

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Expert Reviews

by SERP
(on 17 Jul 2017 )
Cellular Use Rating
In Model Organisms
This tool molecule adds another EZH2 inhibitor with slightly different biochemical potency and selectivity over the closely related EZH1. As such, the suite of tools provides an increasingly robust...
by SERP
(on 24 Jul 2017 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
by SERP
(on 2 Dec 2020 )
Cellular Use Rating
In Model Organisms
CPI-1205 is a Phase I/II agent designed to selectively target the EZH2 component of the polycomb repressor complex (PRC). It is a well designed, and well described pharmacological tool with well defined...
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