CPI-169

SAM competitive inhibitor of EZH2, EZH1

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(2 ratings)

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Probe CPI-169 is in the process of SERP review.

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Information

EZH2
EZH1

SAM competitive inhibitor

Up to 500 nM

Probe Availability:

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

Off-Target Selectivity Assesments

Potency assay (off target): No activity was detected against a panel of 30 protein methyltransferases with the exception of EZH2 and EZH1.

Probe Selectivity in Vitro:

No activity was detected against a panel of 30 protein methyltransferases with the exception of EZH2 and EZH1.

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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

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: 8 Sept 2016 )