MRK-990

MRK-990 : Inhibitor of PRMT9, PRMT5

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(0 ratings)

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Probe MRK-990 is in the process of SERP review.

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Information

PRMT9
PRMT5

Inhibitor

up to 10 uM

Additional Data

SGC Chemical Probe Collection

In Vitro Validations

Uniprot ID: Q6P2P2

Target Class: Epigenetic

Target SubClass: Methyltransferase

Potency: IC50

Potency Value: 10 nM

Potency Assay: Biochemical assay

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

Target aliases:

Protein arginine N-methyltransferase 9, PRMT10, PR ...

Other Reference: Peer reviewed at SGC

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): Selectivity was assessed against 8 PRMTs at 1 and 10uM: PRMT7 and PMRT4 remaining activity of 20 and 30% respectively. Selectivity assessed also against 44 additional Methyltransferases.

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

There are many tool compounds available to explore PRMT5 biology that modulate its activity selectively through a number of different binding modes. The value of MRK-990 comes from its PRMT9 cellular activity as demonstrated by reduced methylation of SAP145. Given that this compound is an S-adenosylmethionine (SAM) analogue, caution should be taken when interpreting cellular phenotypic data as there is the possibility of off-target activity at the many other methyl transferases that have not been assayed with this compound.

(last updated: 7 Jun 2023 )

SERP+ Ratings

In Cell Rating

(last updated: 23 Sept 2024 )