MS-023

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

MS-023 是一种有效的、选择性的、具有细胞活性的 I 型 PRMT 抑制剂，对 PRMT1/3/4/6/8 的 IC50 值分别为 30/119/83/4/5 nM。

MS-023 is a potent, selective, and cell-active inhibitor of type I PRMTs with IC50s of 30/119/83/4/5 nM for PRMT1/3/4/6/8 respectively; doesn't inhibit PRMT5/9/7(>10 uM); inhibits H4R3me2a and H3R2me2a levels in MCF7 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 (IC50=9±0.2 nM). Treatment concentration-dependently reduced the H3R2me2a mark (IC50=56±7 nM).

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.

MS023 | MS 023

Chromatin/Epigenetic

HMTase

PRMT1|PRMT3|PRMT4|PRMT6|PRMT8

Other Indications

——

1831110-54-3

287.3999

C17H25N3O

>98% (HPLC)

DMSO: ≥ 30 mg/mL

CC(C)OC1=CC=C(C=C1)C2=CNC=C2CN(C)CCN

1,2-Ethanediamine, N1-methyl-N1-[[4-[4-(1-methylethoxy)phenyl]-1H-pyrrol-3-yl]methyl]-

(-20℃)

With Ice Pack

≥ 2 years