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CPI-169 | SAM competitive inhibitor of EZH2, EZH1
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 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
  • IC 50:0.24 nM
  • EC 50:41 nM
EZH1
  • IC 50:6.4 nM
  • EC50:41 nM
SAM competitive inhibitor
Up to 500 nM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
No activity was detected against a panel of 30 protein methyltransferases with the exception of EZH2 ...
Selectivity Assessment Description:
No activity was detected against a panel of 30 protein methyltransferases with the exception of EZH2 ...

Potency
Cellular
In Vitro

EZH2

Mode of Action: SAM competitive inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1016/j.chembiol.2014.09.017

EZH1

Mode of Action: SAM competitive inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1016/j.chembiol.2014.09.017

In Vivo Validations

Mouse
Dose: 50-200 mg/kg
Route of delivery: Subcutaneous
Organ of interest (O): KARPA-422 xenograft
Target engagement assay: Indirect, inhibition of protein substrate (H3K27) methylation in tumors.

DOI Reference: 10.1016/j.chembiol.2014.09.017

Orthogonal Probes def

UNC1999
EPZ011989

Chemical Information

Molecular Formula C27H36N4O5S
SMILEs CCS(=O)(=O)N1CCC([C@@H](C)n2c(C)c(C(=O)NCc3c(OC)cc(C)[nH]c3=O)c3ccccc32)CC1
InChI InChI=1S/C27H36N4O5S/c1-6-37(34,35)30-13-11-20(12-14-30)18(3)31-19(4)25(21-9-7-8-10-23(21)31)27(33)28-16-22-24(36-5)15-17(2)29-26(22)32/h7-10,15,18,20H,6,11-14,16H2,1-5H3,(H,28,33)(H,29,32)/t18-/m1/s1
Molecular weight 528.24 Da
AlogP 3.50774
HBond acceptors 9
HBond donors 2
Atoms 73

Vendors

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Expert Reviews

by SERP
(on 19 Aug 2016 )
Cellular Use Rating
In Model Organisms
CPI-169 is a member of a family of structurally related, pyridone based EZH2 inibitors that also includes compounds such as UNC1999 and GSK-343. With the exception of EZH1, CPI-169 is highly selective...
by SERP
(on 8 Sept 2016 )
Cellular Use Rating
In Model Organisms
Subcutaneous treatment with CPI-169 (200 mg/kg twice daily) in KARPAS-422 mouse xengraft model showed >60%% tumor growth inhibition after 28 days.
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