Bioactivity | MS023 trihydrochloride is a potent, selective, and cell-active inhibitor of human type I protein arginine methyltransferases (PRMTs) inhibitor, with IC50s of 30, 119, 83, 4 and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, respectively[1]. |
Invitro | MS023 dihydrochloride (1-1000 nM;48 小时) 抑制 MCF7 细胞中的 PRMT1 甲基转移酶活性[1]。 MS023 dihydrochloride (1-1000 nM;20 小时) 抑制 HEK293 细胞中的 PRMT6 甲基转移酶活性[1]。 Western Blot Analysis[1] Cell Line: |
In Vivo | MS023 dihydrochloride (160 mg/kg,ip) 与 PKC412 (100 mg/kg,ig) 联合给药,通过抑制功能性 MLL-r ALL 起始细胞的维持来阻断 MLL-r 急性淋巴细胞白血病 (ALL) 的传播[2]。 Animal Model: |
Name | MS023 trihydrochloride |
CAS | 2108631-19-0 |
Formula | C17H28Cl3N3O |
Molar Mass | 396.78 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Eram MS, et al. A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases. ACS Chem Biol. 2016 Mar 18;11(3):772-81. [2]. Yinghui Zhu, et al. Targeting PRMT1-mediated FLT3 methylation disrupts maintenance of MLL-rearranged acute lymphoblastic leukemia. Blood. 2019 Oct 10;134(15):1257-1268. |