A-366

A-366 : protein substrate competitive, SAM uncompetitive inhibitor of EHMT2 and EHMT1

Structure

SERP Rating

In Cells

(3 ratings)

In Model Organisms

(2 ratings)

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.

Information

EHMT2
EHMT1

protein substrate competitive inhibitor, SAM uncompetitive inhibitor

300 nM - 5 uM

DOI - 10.1021/ml400496h

Probe Availability:

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

Off-Target Selectivity Assesments

Potency assay (off target): A-366 had no significant activity against 21 protein methyltransferases in a scintillation proximity assay. A-366 is 10-fold selective for EHMT1>EHMT2.

Probe Selectivity in Vitro:

A-366 had no significant activity against 21 protein methyltransferases in a scintillation proximity assay. A-366 is 10-fold selective for EHMT1>EHMT2.

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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

SERP 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

SERP Comments:

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

(last updated: 30 May 2016 )