Fig. 1 | Signal Transduction and Targeted Therapy

Fig. 1

From: Discovery of IHMT-337 as a potent irreversible EZH2 inhibitor targeting CDK4 transcription for malignancies

Fig. 1

Characterization of IHMT-337 as a highly selective EZH2 inhibitor. a Chemical structure of IHMT-337. b EZH2 signaling studies: Target effects of IHMT-337 on EZH2 signaling in Pfeiffer and Karpas422 cell lines. EPZ6438 (the FDA-approved EZH2 inhibitor) was set as control. c Proliferation studies: Effects of 6-day IHMT-337 treatment of Pfeiffer,Karpas422 and SU-DHL6 cell lines. EPZ6438 was set as control. d The GI50 values (the concentrations that cause 50% growth inhibition) of IHMT-337 and EZP6438 to DLBCL cell lines were shown. e Biochemical assays: the effects of IHMT-337 on EZH2 methyltransferase activity on PRC2/EZH2 complex. f Methyltransferase selectivity profiling of IHMT-337 generated from the Hotpot approach. Data shown were representative of at least 2 independent experiments

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