EZH2-IN-1 is a selective inhibitor targeting EZH2 and EZH1 through a SAM-competitive mechanism. It demonstrates potent inhibition with IC50 values of 32 nM for wild-type EZH2, 197 nM for the EZH2 Y641N mutant, and 213 nM for EZH1. This compound effectively reduces levels of bulk H3K27me3 and H3K27me2, highlighting its potential utility in research related to diffuse large B cell lymphoma.
EZH2-IN-1 is a selective inhibitor targeting EZH2 and EZH1 through a SAM-competitive mechanism. It demonstrates potent inhibition with IC50 values of 32 nM for wild-type EZH2, 197 nM for the EZH2 Y641N mutant, and 213 nM for EZH1. This compound effectively reduces levels of bulk H3K27me3 and H3K27me2, highlighting its potential utility in research related to diffuse large B cell lymphoma.
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