PRMT1-Deg-4

PRMT1-Deg-4 : Degrader (PROTAC) of PRMT1

Structure

SERP Rating

Probe PRMT1-Deg-4 is in the process of SERP review.

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Information

PRMT1

Degrader (PROTAC)

up to 5 uM

In Vitro Validations

Uniprot ID: Q99873

Target Class: Epigenetic

Target SubClass: Methyltransferase

Potency: IC50

Potency Value: 185.7 nM

Potency Assay: Methyltransferase Inhibition Assay

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

Target aliases:

Protein arginine N-methyltransferase 1, IR1B4, HRM ...

DOI Reference: 10.1021/acs.jmedchem.5c03030

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Selectivity within family

Probe Selectivity in Vitro:

AlphaLISA enzymatic inhibition assays confrimed that Cpd 4 retained its potency as a pan inhibitor of type I PRMTs (PRMT3, -4, -6, and -8), with IC50 values ranging from 94.6 to 423.6 nM.

Potency assay, off target (cells): Selectivity within target family

Probe Selectivity in Cell:

Selectivity for type I PRMT degradation, other I type PRMT proteins levels, including PRMT3, -4, -6, and -8, after treatment with compound 4 were evaluated via Western blotting in MCF-7 cells. Only PRMT8 seemed affected after 96h.

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