PRMT5 (C449S)/MEP50 Methyltransferase Assay Service

Activity-based PRMT5 (C449S)/MEP50 Methyltransferase Assay for compound screening and profiling via radiometric HotSpotTM and FlashPlate methyltranferase assay.

Target Overview
CAT#

PRMT5 (C449S)/MEP50

Enzyme

Human PRMT5 (C449S)/MEP50

Synonym

PRMT5: Protein arginine N-methyltransferase 5, Shk1 kinase-binding protein 1 homolog, Jak-binding protein 1, 72 kDa ICln-binding protein, HRMT1L5, IBP72, JBP1, SKB1, ANM5 MEP50: Methylosome protein 50, Androgen receptor cofactor p44 WD repeat-containing protein 77, p44/Mep50, WDR77, HKMT1069

Substrates HotSpotTM assay:

Histone H2A, 5 µMSAM, 1 µM

Substrates FlashPlate assay:

H4 (1-15)-Biotin, 40 nMSAM, 1 µM

Assay Properties
Reaction

S-adenosyl-L-[methyl-³H]methionine + histone L-arginine = S-adenosyl-L-homocysteine + histone [methyl-³H]-L- arginine

Readout

Enzymatic activity

Reference Compound IC50s HotSpotTM assay
Compounds IC50 (nM)
SAH 1,000
Sinefugin 640
MTA 87
EPZ015666 2,600
Reference Compound IC50s FlashPlate Assay
Compounds IC50 (nM)
SAH 1,100
Sinefugin 440
MTA 1,400
EPZ015666 14
Scientific Information

PRMT5; O14744 (http://www.uniprot.org/uniprot/O14744)MEP50; Q9BQA1 (http://www.uniprot.org/uniprot/Q9BQA1)

Screening Location

Malvern, USA

Reference compound IC50 for PRMT5(C449S)/MEP50 - HotSpot

Reference compound IC50 for PRMT5(C449S)/MEP50 - HotSpot


 

Reference compound IC50 for PRMT5(C449S)/MEP50 - FlashPlate

Reference compound IC50 for PRMT5(C449S)/MEP50 - FlashPlate