MS1943
规格
| Cas Number | 2225938-17-8 |
| 规格或纯度 | ≥98% |
| 纯度 | ≥98% |
| 包装 | 100mg 或 1mg 或 5mg 或 25mg |
产品信息
| 品牌 | 阿拉丁 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 100 mg/mL (139.09 mM); Ethanol: 100 mg/mL (139.09 mM); Water: Insoluble; |
| 简短描述 | 组蛋白甲基转移酶抑制剂 |
| 英文简短描述 | Histone Methyltransferase Inhibitors |
| 过滤标签 | 表观遗传学,组蛋白甲基转移酶 |
| 储存温度 | -20°C储存 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | MS1943 是一种可口服的 EZH2 选择性降解剂，能有效降低细胞中的 EZH2 水平，抑制 EZH2 甲基转移酶活性的 IC50 值为 120 nM。 |
| 英文描述 |
Information MS1943 MS1943 is an orally bioavailable EZH2 selective degrader with IC50 of 120 nM. Targets EZH2 (Cell-free assay) 120 nM In vitro MS1943 is a first-in-class EZH2 selective degrader that effectively reduces EZH2 levels in cells. MS1943 has a profound cytotoxic effect in multiple TNBC cells, while sparing normal cells. MS1943 mediates its cytotoxic effects through ER stress and UPR induction in cells that are dependent for their growth on EZH2. In vivo MS1943 is efficacious in vivo and well tolerated in mice at the efficacious dose, suggesting that pharmacologic degradation of EZH2 can be advantageous for treating the cancers that are dependent on EZH2. Cell Research(from reference) Cell lines：MDA-MB-468 cells, HCC70 cells, BT549, HCC70 and MDA-MB-231 TNBC cells, KARPAS-422 and SUDHL8 lymphoma cells and PNT2 non-cancerous prostate cells Concentrations：5 μM, 4 μM Incubation Time：24 h, 6 h |