N1-甲基-N1-[[4-[4-(异丙氧基)苯基]-1H-吡咯-3-基]甲基]-1,2-乙二胺
中文名称 | N1-甲基-N1-[[4-[4-(异丙氧基)苯基]-1H-吡咯-3-基]甲基]-1,2-乙二胺 |
---|---|
中文同义词 | N1-甲基-N1-[[4-[4-(异丙氧基)苯基]-1H-吡咯-3-基]甲基]-1,2-乙二胺;人I型PRMTS抑制剂(MS023);N1-((4-(4-异丙氧基苯基)-1H-吡咯-3-基)甲基)-N1-甲基乙烷-1,2-二胺;MS023,细胞活性PRMT抑制剂 |
英文名称 | MS023 |
英文同义词 | MS023;N1-Methyl-N1-[[4-[4-(1-methylethoxy)phenyl]-1H-pyrrol-3-yl]methyl]-1,2-ethanediamine;(2-aminoethyl)(methyl)({4-[4-(propan-2-yloxy)phenyl]-1H-pyrrol-3-yl}methyl)amine;CS-2284;MS023 (MS-023;1,2-Ethanediamine, N1-methyl-N1-[[4-[4-(1-methylethoxy)phenyl]-1H-pyrrol-3-yl]methyl]-;Inhibitor,MS 023,MS-023,MS023,inhibit,Histone Methyltransferase |
CAS号 | 1831110-54-3 |
分子式 | C17H25N3O |
分子量 | 287.4 |
EINECS号 | |
相关类别 | 细胞生物学试剂 |
Mol文件 | 1831110-54-3.mol |
结构式 |
N1-甲基-N1-[[4-[4-(异丙氧基)苯基]-1H-吡咯-3-基]甲基]-1,2-乙二胺 性质
沸点 | 437.8±45.0 °C(Predicted) |
---|---|
密度 | 1.075±0.06 g/cm3(Predicted) |
储存条件 | -20°C |
溶解度 | DMSO 中≥28.7 mg/mL;乙醇中≥13.7 mg/mL;水中≥23.3 mg/mL |
形态 | 粉末 |
酸度系数(pKa) | 17.44±0.50(Predicted) |
颜色 | 白色至浅棕色 |
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 |
---|---|---|---|---|---|
2024/01/25 | HY-19615 | N1-甲基-N1-[[4-[4-(异丙氧基)苯基]-1H-吡咯-3-基]甲基]-1,2-乙二胺 MS023 | 1831110-54-3 | 2mg | 760元 |
2024/01/25 | HY-19615 | N1-甲基-N1-[[4-[4-(异丙氧基)苯基]-1H-吡咯-3-基]甲基]-1,2-乙二胺 MS023 | 1831110-54-3 | 5mg | 1000元 |