GSK591

GSK591 : protein substrate competitive inhibitor, SAM uncompetitive inhibitor of PRMT5

Structure

Information

Protein target names: PRMT5

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

Recommended in-cell concentration:
10 nM - 1 uM

In Vitro Validations

Uniprot ID: O14744
Target Class: Epigenetic
Target SubClass: Protein methyltransferase
Potency: IC50
Potency Value: 4 nM
Potency Assay: Homogeneous time-resolved fluorescence (HTRF) assay under balanced conditions to monitor the monomethylation of H4R3 on a histone H4 peptide by PRMT5:MEP50.
PDB ID for probe-target interaction (3D structure): --
Structure-activity relationship: Yes. Early SAR exploration around the THIQ motif confirmed the contribution of the cation−π interaction with cofactor SAM and was thus retained within the series as a key binding interaction.
Target aliases:
Protein arginine N-methyltransferase 5, SKB1, JBP1 ...

In Cell Validations

In Vivo Data

No in Vivo Validations

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SERP ratings and comments


SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 18 May 2016 )

SERP Ratings

In Cell Rating

(last updated: 30 May 2016 )

SERP Ratings

In Cell Rating

Comments:

GSK591 is an excellent probe to investigate PRMT5 function in cells. For in vivo work, EPZ015666 is a more suitable compound.

(last updated: 4 Jun 2016 )