MS023 二盐酸盐
| 中文名称 | MS023 二盐酸盐 |
|---|---|
| 中文同义词 | MS-023 HCL(新增分子);化合物 MS023 DIHYDROCHLORIDE |
| 英文名称 | MS023 dihydrochloride |
| 英文同义词 | MS023 dihydrochloride;N1-[4-(4-Isopropoxy-phenyl)-1H-pyrrol-3-ylmethyl]-N1-methyl-ethane-1,2-diamine dihydrochloride;MS-023 2HCl |
| CAS号 | 1992047-64-9 |
| 分子式 | C17H26ClN3O |
| 分子量 | 323.87 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 1992047-64-9.mol |
| 结构式 |  |
MS023 二盐酸盐 性质
| 储存条件 | Store at -20°C |
|---|---|
| 溶解度 | 二甲基亚砜：≥ 150 mg/mL（416.30 mM） |
MS023 dihydrochloride 是一种有效选择性的，具有细胞活性的人 I 型蛋白精氨酸甲基转移酶 (PRMTs) 抑制剂，对 PRMT1，PRMT3，PRMT4，PRMT6 和 PRMT8 的 IC50 分别为 30，119，83，4 和 5 nM。
IC50: 30 nM (PRMT1), 119 nM (PRMT3), 83 nM (PRMT4), 4 nM (PRMT6), 5 nM (PRMT8)
MS023 (1-1000 nM; 48 hours) inhibits PRMT1 methyltransferase activity in MCF7 cells.
MS023(1-1000 nM; 20 hours) inhibits PRMT6 methyltransferase activity in HEK293 cells.
Western Blot Analysis
| Cell Line: | MCF7 and HEK293 cells |
| Concentration: | 1.4, 4, 12, 37, 111, 333, and 1000 nM |
| Incubation Time: | 48 hours for MCF7 cells; 20 hours for HEK293 cells |
| Result: |
Treatment potently and concentration-dependently reduced cellular levels of H4R3me2a (IC
50
=9±0.2 nM).
Treatment concentration-dependently reduced the H3R2me2a mark (IC 50 =56±7 nM). |
Administration of MS023 (160 mg/kg, i.p) in combination with PKC412 (100 mg/kg, i.g.) blocks MLL-r acute lymphoblastic leukemia (ALL) propagation by inhibiting maintenance of functional MLL-r ALL-initiating cells.
| Animal Model: | NOD-scid IL2Rgnull (NSG) mice bearing primary MLL-r ALL cells |
| Dosage: | 160 mg/kg |
| Administration: | Intraperitoneal injection; PKC412 (100 mg/kg, i.g.), MS023 (160 mg/kg, i.p), or a combination for 4 weeks |
| Result: | Combinatorial treatment extended survival of leukemic mice relative to single treatments. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-19615B | MS023 DIHYDROCHLORIDE MS023 dihydrochloride | 1992047-64-9 | 2mg | 760元 |
| 2024/04/30 | HY-19615B | MS023 DIHYDROCHLORIDE MS023 dihydrochloride | 1992047-64-9 | 10mM * 1mLin DMSO | 793元 |