MS023 dihydrochloride

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CAS NO:

1992047-64-9

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。

生物活性

MS023 dihydrochloride 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

360.32

性状

Solid

Formula

C₁₇H₂₇Cl₂N₃O

CAS 号

1992047-64-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据

In Vitro:

DMSO : ≥ 150 mg/mL(416.30 mM)

H₂O : 33.33 mg/mL(92.50 mM;Need ultrasonic)

*"≥" 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	2.7753 mL	13.8766 mL	27.7531 mL
5 mM	0.5551 mL	2.7753 mL	5.5506 mL
10 mM	0.2775 mL	1.3877 mL	2.7753 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 (stored under nitrogen)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.
请依序添加每种溶剂： PBS
Solubility: 25 mg/mL (69.38 mM); Clear solution; Need ultrasonic and warming

*以上所有助溶剂都可在本网站选购。