Valemetostat

SKU: orb1220173

Description

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.

Key Properties

• CAS Number: 1809336-39-7
• MW: 488.02
• Purity: >98% (HPLC)
• Formula: C₂₆H₃₄ClN₃O₄
• SMILES: CC1=CC(=C(C(=O)N1)CNC(=O)C2=CC(=C3C(=C2C)OC(O3)(C)C4CCC(CC4)N(C)C)Cl)C
• Target: EZH1/2
• Solubility: In Vitro: DMSO : 70 mg/mL (143.44 mM)

Bioactivity

• In Vivo:
  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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• 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 treatmentin the sensitive lymphoma types.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

EZH1/2