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MS023
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MS023图片
CAS NO:1831110-54-3
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
2mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
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PRMT1PRMT3PRMT4PRMT6PRMT8IC50分别为 30,119,83,4 和 5 nM。
生物活性

MS023 is a potent, selective, and cell-active inhibitor of humantype I protein arginine methyltransferases (PRMTs)inhibitor, withIC50s of 30, 119, 83, 4 and 5 nM forPRMT1,PRMT3,PRMT4,PRMT6, andPRMT8, respectively[1].

IC50& Target

IC50: 30 nM (PRMT1), 119 nM (PRMT3), 83 nM (PRMT4), 4 nM (PRMT6), 5 nM (PRMT8)[1]

体外研究
(In Vitro)

MS023 (1-1000 nM; 48 hours) inhibits PRMT1 methyltransferase activity in MCF7 cells[1].
MS023(1-1000 nM; 20 hours) inhibits PRMT6 methyltransferase activity in HEK293 cells[1].

Western Blot Analysis[1]

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).
体内研究
(In Vivo)

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[2].

Animal Model:NOD-scid IL2Rgnull (NSG) mice bearing primary MLL-r ALL cells[2]
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.
分子量

287.40

性状

Solid

Formula

C17H25N3O

CAS 号

1831110-54-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

H2O : 66.67 mg/mL(231.98 mM;Need ultrasonic)

DMSO : ≥ 30 mg/mL(104.38 mM)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM3.4795 mL17.3974 mL34.7947 mL
5 mM0.6959 mL3.4795 mL6.9589 mL
10 mM0.3479 mL1.7397 mL3.4795 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。