Valemetostat (DS-3201) tosylate, a first-in-class EZH1/2 dual inhibitor with IC 50 values ＜10 nM. Valemetostat tosylate can be used for the research of relapsed/refractory peripheral T-cell lymphoma In Vitro Valemetostat tosylate (1-1000 nM) strongly and specifically inhibits EZH1 and EZH2 with IC 50 values ＜10 nM. Valemetostat tosylate (100 nM; 7 d) effectively removes H3K27me3 and also prevents unexpected gain of H3K27me3. Valemetostat tosylate (0.1-100 nM; 7 d) potently inhibits H3K27me3 by low-dose treatment in the sensitive lymphoma types. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo Valemetostat tosylate (0.01 mg/g; i.p.; once) prevents the changes of H3K27me3 after exercise training. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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. Form:Solid IC50& Target:EZH1
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Valemetostat tosylate
CAS number：1809336-93-3 molecular formula：C33H42ClN3O7S
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| Chinese alias | 伐美司他甲磺酸盐 | ||
| English alias | 1809336-93-3 (tosylate) | Valemetostat tosylate | AKOS040740514 | Valemetostat tosylayte | MS-31014 | DS-3201 tosylate | VALEMETOSTAT TOSILATE [JAN] | (2R)-7-chloro-2-[trans-4-(dimethylamino)cyclohexyl]-N-[(4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methy | ||
| CAS number | 1809336-93-3 | molecular formula | C33H42ClN3O7S |
| molecular weight | 660.22 g/mol | Exact mass | ≥98% |
| PSA | 143.000 Ų | logp | - |
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