Valemetostat

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Valemetostat 是 zeste 同源物 1 (EZH1) 和 EZH2.1 增强子的双重抑制剂，它在无细胞测定中抑制含有 EZH1 或 EZH2 作为催化亚基的多梳抑制复合物 2 (PRC2)（IC50 分别 = 8.4 和 2.5 nM） 。

Valemetostat is a dual inhibitor of enhancer of zeste homolog 1 (EZH1) and EZH2.1 It inhibits polycomb repressive complex 2 (PRC2) containing EZH1 or EZH2 as the catalytic subunit in cell-free assays (IC50s = 8.4 and 2.5 nM, respectively). Valemetostat inhibits trimethylation of histone H3 lysine 27 in HCT116 cells (IC50 = 0.44 nM). It inhibits the growth of Karpas-422 diffuse large B cell lymphoma (DLBCL) cells (GI50 = 4.8 nM).(In Vitro):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 treatment in the sensitive lymphoma types.(In Vivo):Valemetostat (0.01 mg/g; i.p.; once) prevents the changes of H3K27me3 after exercise training.

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.

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.

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Others

Other Targets

EZH1/2

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1809336-39-7

488.02

C26H34ClN3O4

>98% (HPLC)

In Vitro:?DMSO : 70 mg/mL (143.44 mM)

CC1=CC(=C(C(=O)N1)CNC(=O)C2=CC(=C3C(=C2C)OC(O3)(C)C4CCC(CC4)N(C)C)Cl)C

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(-20℃)

With Ice Pack

≥ 2 years