PRMT1-Deg-4

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

Structure

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.
I have extra information to add

SERP ratings and comments


No SERP comments found for PRMT1-Deg-4