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抑制剂描述:

产品名称:XMU-MP-1

产品别名:见爱必信官网

英文别名:XMU-MP-1

靶点:MST

CAS:2061980-01-4

纯度:98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

 XMU-MP-1 is a reversible and selective MST1/2 inhibitor with IC50 values of 71.1 and 38.1 nM against MST1 and MST2.

溶解性:DMSO : ≥ 30 mg/mL (72.03 mM)

体外研究:

XMU-MP-1 blocks MST1/2 kinase activities, thereby activating the downstream effector Yes-associated protein and promoting cell growth. XMU-MP-1 inhibits phosphorylation of MOB1 in a dose-dependent manner. Furthermore, with increasing ATP concentration, XMU-MP-1 exhibits a proportional increase in IC50 against MST1/2, as well as an attenuated inhibition of the MST2-mediated phosphorylation of MOB1. At concentrations ranging from 0.1 to 10 μM, XMU-MP-1 reduces the phosphorylation of endogenous MOB1, LATS1/2, and YAP in human liver carcinoma (HepG2) cells in a dose-dependent manner. Similarly, XMU-MP-1 treatment inhibits hydrogen peroxide (H2O2)-stimulated MOB1 phosphorylation and MST1/2 autophosphorylation in a variety of cell lines, including mouse macrophage-like cells (RAW264.7), human osteosarcoma (U2OS), human colorectal adenocarcinoma (SW480), immortalized human retinal pigment epithelial cells (RPE1), human pleomorphic hepatocellular carcinoma (SNU-423), and HepG2, as well as primary mouse hepatocytes, without affecting the phosphorylation of JNK (c-Jun N-terminal kinase), which is a positive control for H2O2 stimulation. XMU-MP-1 treatment increases YAP nuclear translocation.

体内研究:XMU-MP-1 displays excellent in vivo pharmacokinetics and is able to augment mouse intestinal repair, as well as liver repair and regeneration, in both acute and chronic liver injury mouse models at a dose of 1 to 3 mg/kg via intraperitoneal injection. XMU-MP-1 exhibits favorable pharmacokinetics in rats with a half-life of 1.2 hours and a bioavailability of 39.5%. The maximal phosphorylation inhibition of MOB1 and YAP is achieved between 1.5 and 6 hours after intraperitoneal dosing with XMU-MP-1 (1 mg/kg). XMU-MP-1 protects mice from DSS-induced colitis and ameliorates chronic liver injury.

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