YM1240 

YM1240 is an orally active dual EZH2/HDAC inhibitor with human EZH2 IC₅₀ 0.342 μM and human HDAC IC₅₀ 0.12 μM. YM1240 inhibits EZH2 pathway to reduce H3K27me3 levels, inhibits HDAC pathway to increase H3K9ac and H4ac levels. YM1240 suppresses proliferation, induces apoptosis, induces cell cycle arrest in lymphoma cells. YM1240 exhibits antitumor efficacy in lymphoma xenograft models. YM1240 can be used for the research of lymphoma^[1].

YM1240 (compound D19) (0.3-0.6 μM; 60 min) potently inhibits the activity of purified EZH2 enzyme, with an IC₅₀ of 0.342 μM; it also potently inhibits HDAC enzyme activity in HeLa nuclear extracts, with an IC₅₀ of 0.12 μM^[1].
YM1240 (60 min) is a potent and selective inhibitor of HDAC1 and HDAC6, with IC₅₀ values of 0.066 μM and 0.01 μM, respectively. It exhibits negligible activity against HDAC4 and only weak activity against HDAC8^[1].
YM1240 (0.01-10 μM; 6 days) potently inhibits the proliferation of Jeko-1, NAMALWA, RAJI, DAUDI, JVM-2 and Mino lymphoma cell lines, with GC₅₀ values ranging from 0.20 μM to 0.92 μM; it also potently inhibits the proliferation of SU-DHL-2 lymphoma cells, with a GC₅₀ of 0.26 μM^[1].
YM1240 (1-4 μM; 24 h) inhibits EZH2 activity (reduces H3K27me3 levels) and HDAC activity (increases H3K9ac and H4ac levels) in Jeko-1 and SU-DHL-2 lymphoma cells in a dose-dependent manner^[1].
YM1240 (1-2 μM; 72 h) induces apoptosis in Jeko-1 and SU-DHL-2 lymphoma cells in a dose-dependent manner, as evidenced by increased Annexin V-positive cells and elevated levels of activated caspase 3/7 and activated PARP^[1].
YM1240 (1-2 μM; 48 h) induces G0/G1 cell cycle arrest in Jeko-1 and SU-DHL-2 lymphoma cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

YM1240 (compound D19) (100 mg/kg; i.p.; daily; 21 days) demonstrates potent in vivo antitumor efficacy in a Jeko-1 lymphoma xenograft model, with a 70.7% tumor growth inhibition rate, while inhibiting both EZH2 and HDAC pathways without causing significant body weight loss^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

498.57

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• [1]. Sun Y, et al.. Design, synthesis and biological evaluation of EZH2/HDAC dual inhibitors for the treatment of lymphomas. European journal of medicinal chemistry. 2026 May 28;316:119006.