EZH2 Methyltransferase Assay Service

Activity-based EZH2 Methyltransferase Assay for compound screening and profiling via radiometric HotSpotTM methyltranferase assay.
Target Overview
CAT#
EZH2
Enzyme
Human EZH2; 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/mlSAM, 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
CompoundsIC50 (nM)
SAH9,800
Sinefungin158,000
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, USA
Reference compound IC50 for EZH2
Reference compound IC50 for EZH2