G9a Methyltransferase Assay Service

Activity-based G9a Methyltransferase Assay for compound screening and profiling via radiometric HotSpotTM methyltranferase assay.

Target Overview

CAT#

G9a

Enzyme

Human G9a

Synonym

Histone-lysine N-methyltransferase EHMT2, Histone H3-K9 methyltransferase 3, Euchromatic histone-lysine N-methyltransferase 2, HLA-B-associated transcript 8 Protein G9a, Lysine N-methyltransferase 1C, EHMT2, BAT8, C6orf30, G9A, KMT1C, NG36

Substrates

Histone H3, or H3 (1-21) peptide, 5 µM
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) With Histone H3 substrate
SAH 2,300
Sinefungin 94,000
BIX 01294 >200,000
Chaetocin 6,000
Compounds IC50 (nM) With H3 (1-21) peptide substrate
SAH 760
Sinefungin 8,300
BIX 01294 5,300
Chaetocin 8,000

Scientific Information

Q96KQ7 (http://www.uniprot.org/uniprot/Q96KQ7)

Screening Location

Malvern, PA, USA

Further Information

More information can be found on our website Methyltransferase Assays.

Reference compound IC50 for G9a/Histone H3

Reference compound IC50 for G9a/Histone H3

Reference Compound IC50 for G9a/H3 (1-21)

Reference Compound IC50 for G9a/H3 (1-21)