产品
编 号:F225318
分子式:C26H34ClN3O4
分子量:488.02
产品类型
结构图
CAS No: 1809336-39-7
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产品详情
生物活性:
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.
体内研究:
Valemetostat (0.01 mg/g; i.p.; once) prevents the changes of H3K27me3 after exercise training.Animal Model:Male C57BL/6J mice with chronic and acute running exercise or without exercise
Dosage:0.01 mg/g
Administration:Intraperitoneal injection; 0.01 mg/g; 30 min before the start of running exercise
Result:Significantly increased the level of H3K27me3 , slightly decresed EZH1 level , upregulated the EZH2 level and increased the level of phosphorylated AMPK after exercise. Repressed myonuclear H3K27me3 accumulation during training and caused a failure of adaptive changes.
体外研究:
Valemetostat (1-1000 nM) strongly and specifically inhibits EZH1 and EZH2 with IC50 values <10 nM.Valemetostat (100 nM; 7 d) effectively removes H3K27me3 and also prevents unexpected gain of H3K27me3.Valemetostat (0.1-100 nM; 7 d) potently inhibits H3K27me3 by low-dose treatmentin the sensitive lymphoma types.