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Valemetostat (DS-3201), a first-in-class EZH1/2 dual inhibitor with IC50 values ＜10 nM. Valemetostat can be used for the research of relapsed/refractory peripheral T-cell lymphoma[1][2][3].

EZH1

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[1] Daiichi Sankyo’s EZH1/2 Dual Inhibitor Valemetostat (DS-3201) Receives SAKIGAKE Designation for Treatment of Patients with Relapsed/Refractory Peripheral T-Cell Lymphoma from Japan MHLW.
[2] Shimizu J, Kawano F. Exercise-induced histone H3 trimethylation at lysine 27 facilitates the adaptation of skeletal muscle to exercise in mice. J Physiol. 2022 Jul;600(14):3331-3353. DOI:10.1113/JP282917
[3] Yamagishi M, et al. Targeting Excessive EZH1 and EZH2 Activities for Abnormal Histone Methylation and Transcription Network in Malignant Lymphomas. Cell Rep. 2019 Nov 19;29(8):2321-2337.e7. DOI:10.1016/j.celrep.2019.10.083