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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. |
Dose | Mice: 1 mg/kg - 3 mg/kg[2] |
Administration | i.p. |
计算器 | ||||
存储液制备 | 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 |
CAS号 | 2061980-01-4 |
分子式 | C17H16N6O3S2 |
分子量 | 416.477 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
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 |