SGC3027

SGC3027 : Prodrug, SAM-competitive of PRMT7

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(0 ratings)

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Probe SGC3027 is in the process of SERP review.

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Information

PRMT7

Prodrug, SAM-competitive

up to 10 uM
Reviewer recommended concentration:

Additional Data

SGC Chemical Probe Collection

In Vitro Validations

Uniprot ID: Q9NVM4

Target Class: Epigenetic

Target SubClass: Methyltransferase

Potency: IC50

Potency Value: <2.4 nM

Potency Assay: Scintillation proximity assay (SPA) against PRMT7 using 3H-SAM and a histone H2B peptide (residues 23–37) as a substrate (testing SGC8158)

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

Target aliases:

Protein arginine N-methyltransferase 7, KIAA1933, ...

DOI Reference: 10.1038/s41467-020-16271-z

Uniprot ID: Q9NVM4

Target Class: Epigenetic

Target SubClass: Methyltransferase

Potency: Kd

Potency Value: 6.4 ± 1.2 nM

Potency Assay: SPR using SGC8158

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

Target aliases:

Protein arginine N-methyltransferase 7, KIAA1933, ...

DOI Reference: 10.1038/s41467-020-16271-z

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): Good selectivity over a panel of 35 methyltransferases including PRMTs and kinases. RIPK2: 81% inhibition at 1 µM.

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

SGC3027 is recommended as a selective inhibitor of PRMT7 for in vitro experiments including studies in cells. No information is known about the PK of SGC3027 so it is not recommended for in vivo studies. Note that SGC3027 is a prodrug of the active compound, SGC8158.

(last updated: 22 May 2023 )