EZH2 (Y641F) Methyltransferase Assay Service

Activity-based EZH2 (Y641F) Methyltransferase Assay for compound screening and profiling via radiometric HotSpotTM methyltranferase assay.

Target Overview

CAT#

EZH2 (Y641F)

Enzyme

Human EZH2 (Y641F); 5 component complex

Synonym

EZH2: Polycomb protein EZH2, Enhancer of zeste homolog 2, ENX-1, KMT6
EED: WD protein associating with integrin cytoplasmic tails 1
SUZ12: Suppressor of zeste 12 protein homolog
RBAP48: Histone-binding protein RBBP4
AEBP2: Zinc finger protein AEBP2

Substrates

Core Histone, 0.05 mg/ml
SAM, 1 µM

Assay Properties

Reaction

S-adenosyl-L-[methyl-³H]methionine + histone L-lysine = S-adenosyl-L-homocysteine + histone N⁶-[methyl-³H]-L-lysine

Readout

Enzymatic activity

Reference Compound IC50s
Compounds IC50 (nM)
SAH 26,000
Sinefungin >200,000
BIX01294 >200,000
Chaetocin >200,000

Scientific Information

EZH2 Q15910 (http://www.uniprot.org/uniprot/Q15910)
EED O75530 (http://www.uniprot.org/uniprot/O75530)
SUZ12 Q15022 (http://www.uniprot.org/uniprot/Q15022)
RBBP4 Q09028 (http://www.uniprot.org/uniprot/Q09028)
AEBP2 Q6ZN18 (http://www.uniprot.org/uniprot/Q6ZN18)

Screening Location

Malvern, PA, USA

Further Information

More information can be found on our website Methyltransferase Assays.

Reference compound IC50 for EZH2 (Y641F)

Reference compound IC50 for EZH2 (Y641F)

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