MS023 dihydrochloride

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

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。

MS023 dihydrochloride 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.

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.

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Others

Other Targets

Histone Methyltransferase

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1992047-64-9

360.32

C17H27Cl2N3O

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : ≥ 150 mg/mL (416.30 mM ) H2O 中的溶解度 : 33.33 mg/mL (92.50 mM; 超声助溶)

Cl.Cl.CC(C)Oc1ccc(cc1)-c1c[nH]cc1CN(C)CCN

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(-20℃)

With Ice Pack

≥ 2 years