1992047-64-9
中文名稱
MS023 二鹽酸鹽
英文名稱
MS023 dihydrochloride
CAS
1992047-64-9
分子式
C??H??Cl?N?O
更新日期
2024/11/08 11:28:10
分子量
323.87
MOL 文件
1992047-64-9.mol
1992047-64-9 結(jié)構(gòu)式
MS023 二鹽酸鹽價格(試劑級)
| 報價日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價格 |
| 2024/11/08 | HY-19615B | MS023 DIHYDROCHLORIDE MS023 dihydrochloride | 1992047-64-9 | 10mM * 1mLin DMSO | 793元 |
| 2024/11/08 | HY-19615B | MS023 DIHYDROCHLORIDE MS023 dihydrochloride | 1992047-64-9 | 5mg | 829元 |
| 2024/11/08 | HY-19615B | MS023 DIHYDROCHLORIDE MS023 dihydrochloride | 1992047-64-9 | 10mg | 1303元 |
常見問題列表
生物活性
MS023 dihydrochloride 是一種有效選擇性的，具有細(xì)胞活性的人 I 型蛋白精氨酸甲基轉(zhuǎn)移酶 (PRMTs) 抑制劑，對 PRMT1，PRMT3，PRMT4，PRMT6 和 PRMT8 的 IC50 分別為 30，119，83，4 和 5 nM。靶點
IC50: 30 nM (PRMT1), 119 nM (PRMT3), 83 nM (PRMT4), 4 nM (PRMT6), 5 nM (PRMT8)
體外研究
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). |
體內(nèi)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. |