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)
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]-
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
沸点
437.8±45.0 °C(Predicted)
密度
1.075±0.06 g/cm3(Predicted)
储存条件
-20°C
形态
powder
酸度系数(pKa)
17.44±0.50(Predicted)
颜色
white to light brown
生物活性
MS023 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。
靶点
IC50: 30 nM (PRMT1), 119 nM (PRMT3), 83 nM (PRMT4), 4 nM (PRMT6), 5 nM (PRMT8)
体外研究
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).
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).
体内研究
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.
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.
