货号	规格	价格	上海	北京	珠海	重庆	武汉
S89697-5mg买3赠1	99.40%	￥420.00 S89697-5mg ￥420.00 现货（买3赠1）	7 7	-	-	-	-
S89697-10mg买3赠1	99.40%	￥710.00 S89697-10mg ￥710.00 现货（买3赠1）	5 5	-	-	-	-
S89697-25mg买3赠1	99.40%	￥1390.00 S89697-25mg ￥1390.00 现货（买3赠1）	4 4	-	-	-	-
S89697-100mg	≥98%	￥4010.00 S89697-100mg ￥4010.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

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

靶点：

Histone Methyltransferase;HistoneMethyltransferase

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 treatment in the sensitive lymphoma types.

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.

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：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.049 ml	10.245 ml	20.491 ml
5 mM	0.41 ml	2.049 ml	4.098 ml
10 mM	0.205 ml	1.025 ml	2.049 ml
50 mM	0.041 ml	0.205 ml	0.41 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。

参考文献

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