| Identification | Back Directory | [Name]
DS-3201 | [CAS]
1809336-39-7 | [Synonyms]
DS-3201
Valemetostat
1,3-Benzodioxole-5-carboxamide, 7-chloro-N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-2-[trans-4-(dimethylamino)cyclohexyl]-2,4-dimethyl-, (2R)-
(R)-7-chloro-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-((1r,4R)-4-(dimethylamino)cyclohexyl)-2,4-dimethylbenzo[d][1,3]dioxole-5-carboxamide | [Molecular Formula]
C26H34ClN3O4 | [MDL Number]
MFCD31692361 | [MOL File]
1809336-39-7.mol | [Molecular Weight]
488.02 |
| Chemical Properties | Back Directory | [Boiling point ]
610.0±55.0 °C(Predicted) | [density ]
1.26±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: soluble | [form ]
A crystalline solid | [pka]
11.87±0.10(Predicted) | [color ]
White to off-white | [InChIKey]
SSDRNUPMYCFXGM-UYPAYLBCSA-N | [SMILES]
O1C2=C(Cl)C=C(C(NCC3=C(C)C=C(C)NC3=O)=O)C(C)=C2O[C@]1([C@@H]1CC[C@@H](N(C)C)CC1)C |
| Hazard Information | Back Directory | [Uses]
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[1][2][3]. | [in vivo]
Valemetostat (0.01 mg/g; i.p.; once) prevents the changes of H3K27me3 after exercise training[2]. | Animal Model: | Male C57BL/6J mice with chronic and acute running exercise or without exercise[1] | | 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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| [IC 50]
EZH1 | [storage]
Store at -20°C | [References]
[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. DOI:10.1113/JP282917
[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. DOI:10.1016/j.celrep.2019.10.083 |
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