产品说明书

XMU-MP-1

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Chemical Structure| 2061980-01-4 同义名 : -
CAS号 : 2061980-01-4
货号 : A397171
分子式 : C17H16N6O3S2
纯度 : 99%+
分子量 : 416.477
MDL号 : MFCD30377214
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 6 mg/mL(14.41 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

IP 2% DMSO+2% Tween80+30% PEG300+water 4 mg/mL clear

PO 0.5% CMC-Na 60 mg/mL suspension

生物活性
描述 The mammalian ste20-like kinases 1/2 (MST1/2) which is a core component in the Hippo pathway in mammals, is related in cell growth, controlling organ size and maintaining organ homeostasis[1]. XMU-MP-1 is a potent and selective inhibitor of MST1/2 with IC50 value of 71.1 nM and 38.1 nM against MST1 and MST2, respectively[2].
XUM-MP-1 was added to a variety of cell lines including RAW264.7, USOS, SW480, SNU-423, RPE1 and HepG2, and the inhibition of hydrogen peroxide (H2O2)–stimulated MOB1 phosphorylation and MST1/2 autophosphorylation started at concentration of 1 and 3 μM for all cell lines measured by immunoblotting assay after incubating with XMU-MP-1 for 3 hours.
In Sprague-Dawley rats, after intraperitoneal administration of 1 mg/kg XMU-MP-1, the maximal phosphorylation inhibition of MOB1 and YAP was achieved between 1.5 and 6 hours in the liver tissue. The wild-type mice were treated with XMU-MP-1 once a day before a two-thirds partial hepatectomy followed by daily treatment for 7 days. The treatment of XMU-MP-1 could enhance liver regeneration and increase the amounts of Ki67-positive cells and YAP-positive cells in the liver, as well as liver/body weight ratio compared with the control group.
作用机制 XMUMP-1 target the ATP-binding site of the kinases MST1/2.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.40mL

0.48mL

0.24mL

12.01mL

2.40mL

1.20mL

24.01mL

4.80mL

2.40mL
参考文献

[1]Pfleger CM. The Hippo Pathway: A Master Regulatory Network Important in Development and Dysregulated in Disease. Curr Top Dev Biol. 2017.

[2]Fan F, He Z, et al. Pharmacological targeting of kinases MST1 and MST2 augments tissue repair and regeneration. Sci Transl Med. 2016;8(352):352ra108.