| 产品描述： | Valemetostat (DS-3201) tosylate, a first-in-class EZH1/2 dual inhibitor with IC50 values ＜10 nM. Valemetostat tosylate can be used for the research of relapsed/refractory peripheral T-cell lymphoma |
| 靶点： |
EZH1 |
| 体外研究： |
Valemetostat tosylate (1-1000 nM) 强烈且特异地抑制 EZH1 和 EZH2，IC50 值 <10 nM。 Valemetostat tosylate (100 nM；7 d) 有效去除 H3K27me3 并防止 H3K27me3 意外增加。 Valemetostat tosylate (0.1-100 nM；7 d) 通过低剂量处理在敏感细胞中有效抑制 H3K27me3 淋巴瘤类型 |
| 体内研究： |
Valemetostat tosylate (0.01 mg/g; i.p.; once) 可防止运动训练后 H3K27me3 的变化。 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. |
| 参考文献： |
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. 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. |
| 溶解性： |
soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.515 ml |
7.573 ml |
15.146 ml |
| 5 mM |
0.303 ml |
1.515 ml |
3.029 ml |
| 10 mM |
0.151 ml |
0.757 ml |
1.515 ml |
| 50 mM |
0.03 ml |
0.151 ml |
0.303 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
