MS023

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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。

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PRMT1，PRMT3，PRMT4，PRMT6和PRMT8的IC₅₀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°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 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 mg

5 mg

10 mg

1 mM	3.4795 mL	17.3974 mL	34.7947 mL
5 mM	0.6959 mL	3.4795 mL	6.9589 mL
10 mM	0.3479 mL	1.7397 mL	3.4795 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。