A-366

protein substrate competitive inhibitor, SAM uncompetitive inhibitor of EHMT2, EHMT1

Structure

Information

Protein target names: EHMT2, EHMT1

Mechanism of action: protein substrate competitive inhibitor, SAM uncompetitive inhibitor

Recommended in-cell concentration:
300 nM - 5 uM
Primary References:

In Vitro Validations

Uniprot ID: Q96KQ7
Target Class: Epigenetic
Target SubClass: Protein methyltransferase
Potency: IC 50
Potency Value: 3.6 nM
Potency Assay: Peptide-based AlphaLISA, measuring the levels of H3K9 dimethylation
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Histone-lysine N-methyltransferase EHMT2, NG36, KM ...

DOI Reference: 10.1021/ml400496h

In Cell Validations

In Vivo Data

No in Vivo Validations

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SERP ratings and comments


SERP Ratings

In Cell Rating

(last updated: 17 May 2016 )

SERP Ratings

In Cell Rating
In Model Organisms

Comments:

Allow 3 days for effect: reduction of H3K9me2 in PC3 cells (IC50 = 100 nM). Use A-366 in parallel with UNC0642 (as an orthogonal control).

(last updated: 18 May 2016 )

SERP Ratings

In Cell Rating
In Model Organisms

Comments:

A-366 is a cell active and selective probe that has fewer off target effects than UNC638.

(last updated: 30 May 2016 )