SGC6870

SGC6870, an allosteric inhibitor of PRMT6

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(0 ratings)

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Probe SGC6870 is in the process of SERP review.

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Information

PRMT6

Allosteric

~~up to 5 uM~~
Reviewer recommended concentration: 3 µM

Additional Data

SGC Chemical Probe Collection

In Vitro Validations

Uniprot ID: Q96LA8

Target Class: Epigenetic

Target SubClass: Methyltransferase

Potency: IC50

Potency Value: 77 nM

Potency Assay: Biochemical assay (radiometric method)

PDB ID for probe-target interaction (3D structure): 6W6D

Target aliases:

Protein arginine N-methyltransferase 6, HRMT1L6, P ...

DOI Reference: 10.1021/acs.jmedchem.0c02160

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): Selectivity within target family: (R)-2 and (S)-2 were against a total of 33 methyltransferases, including 8 PRMTs, 21 protein lysine methyltransferases (PKMTs), 3 DNA methyltransferases (DNMTs), and 1 RNA methyltransferase. (R)-2 at both 1 and 10 μM potently inhibited PRMT6, but did not significantly inhibit the other 32 methyltransferases. (S)-2 did not significantly inhibit any of the 33 methyltransferases, including PRMT6, at 1 or 10 μM. Selectivity outside target family: (R)-2 was remarkably selective for PRMT6 over a broad range of nonepigenetic targets, including G protein-coupled receptors (GPCRs), ion channels, transporters, and other enzymes at 1 μM.

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SERP ratings and comments

SERP Ratings

In Cell Rating

(last updated: 16 Feb 2023 )

SERP+ Ratings

In Cell Rating

SERP+ Comments:

This probe has an excellent selectivity, no apparent off-targets or cytotoxicity, good negative control and orthogonal probes do exist. Although selectivity against off-targets for the panel of proteins was performed at 1 uM, use at up to 5 uM should be fine.

(last updated: 22 Mar 2023 )