CPI-169

SAM competitive inhibitor of EZH2, EZH1

Structure

Information

Protein target names: EZH2, EZH1

Mechanism of action: SAM competitive inhibitor

Recommended in-cell concentration:
Up to 500 nM

In Vitro Validations

Uniprot ID: Q15910
Target Class: Epigenetic
Target SubClass: Protein methyltransferase
Potency: IC 50
Potency Value: 0.24 nM
Potency Assay: PRC2 enzyme inhibition assay (Y641N-EZH2 IC50=0.5 nM)
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Histone-lysine N-methyltransferase EZH2, KMT6, EZH ...

DOI Reference: 10.1016/j.chembiol.2014.09.017

In Cell Validations

In Vivo Data

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SERP ratings and comments


SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

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 and is suitable for both in vitro cell assays and in vivo work. The compound is not orally biovailable; however, in vivo PD modulation and efficacy in a tumor xenograft model was demonstated using subcutaneous administraton via a a twice daily dosing.

(last updated: 19 Aug 2016 )

SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 8 Sept 2016 )

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

Subcutaneous treatment with CPI-169 (200 mg/kg twice daily) in KARPAS-422 mouse xengraft model showed >60%% tumor growth inhibition after 28 days.

(last updated: 9 Sept 2016 )