UNC0321 tri (trifluoroacetate salt)

UNC0321 is an inhibitor of G9a histone methyltransferase (HMTase) with picomolar potency. It is a quinazoline analogue with a Morrison Ki of 63 pM. It inhibits G9a with an IC₅₀ of 6 nM and 9 nM in chemiluminescence-based oxygen tunneling (CLOT) assays and enzyme-coupled SAH detection assays (ECSD). It inhibits GLP (G9a like protein) with an IC₅₀ of 15 nM and 23 nM in these assays. It is inactive against SET7/9, SET8/PreSET7 and PRMT3 in ECSD assays.