G9a SPR Assay Service

Histone-lysine N-methyltransferase G9a assay with surface plasmon resonance (SPR) format

Target Overview

Target

G9a (AA 913-1193) in the absence and presence of methyl donor SAM

HGNC symbol

EHMT2

Synonyms

Histone-lysine N-methyltransferase EHMT2, Euchromatic histone-lysine N-methyltransferase 2, HLA-B-associated transcript 8, Histone H3-K9 methyltransferase 3 (H3-K9-HMTase 3), Lysine N-methyltransferase 1C

Scientific information

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

Screening location

Malvern, PA, USA

Further information

More information can be found on our website SPR Assay Services for Drug Discovery

UNC0638 binding to G9a in the absence and presence of SAM

UNC0638 Binding to G9a

 

The binding of UNC0638 to G9a was measured in the absence and presence of SAM using a Biacore 8K. Including SAM alters the binding kinetics of UNC0638 resulting in an approximately 10-fold slower off-rate and, as a result, an approximately 10-fold tighter KD. Due to the slower off-rate, single-cycle kinetics were used to measure the binding of UNC0638 in the presence of SAM instead of the multi-cycle kinetics used for the measurement in the absence of SAM. For both measurements a 1:1 kinetic binding model was used to fit the data.