Name: XMU-MP-1
Price: 787.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    XMU-MP-1 is a reversible, potent and selective inhibitor of MST1/2 with IC50 values of 71.1 ± 12.9 nM and 38.1 ± 6.9 nM, respectively [1].
    The Sterile 20-like kinases MST1 and MST2 are key components of the Hippo signaling cascade that play an important role in tissue regeneration, stem cell self-renewal and organ size control [1].
    XMU-MP-1 is a potent, selective and ATP-competitive MST1/2 inhibitor. In ELISA-based high-throughput screening assay, XMU-MP-1 at 10 μM inhibited MST2 kinase activity by more than 50% and dose-dependently inhibited the phosphorylation of MOB1 mediated by MST2. In human liver carcinoma (HepG2) cells, XMU-MP-1 (0.1 to 10 μM) dose-dependently reduced the phosphorylation of endogenous MOB1, LATS1/2, and YAP. Also, in a variety of cell lines, including human osteosarcoma (U2OS), human colorectal adenocarcinoma (SW480) and human pleomorphic hepatocellular carcinoma (SNU-423), XMU-MP-1 inhibited H2O2-stimulated MOB1 phosphorylation and MST1/2 autophosphorylation [1].
    In wild-type mice, treatment with XMU-MP-1 once a day before a two-thirds partial hepatectomy followed by daily treatment for 7 days. XMU-MP-1 significantly reduced the phosphorylation levels of MOB1 and YAP. After partial hepatectomy, XMU-MP-1 substantially increased liver regeneration. In CCl4-induced liver chronic injury mice treatment with XMU-MP-1 (1 mg/kg) had a small amount of collagen deposition, suggesting XMU-MP-1 is capable of partially rescuing fibrosis [1].
- Properties
  - Alternative Name
    
    4-((5,10-dimethyl-6-oxo-6,10-dihydro-5H-pyrimido[5,4-b]thieno[3,2-e][1,4]diazepin-2-yl)amino)benzenesulfonamide
    
    CAS Number
    
    2061980-01-4
    
    Molecular Formula
    
    C17H16N6O3S2
    
    Molecular Weight
    
    416.48
    
    Appearance
    
    A solid
    
    Purity
    
    99.86%
    
    Solubility
    
    ≥41.6 mg/mL in DMSO with gentle warming; insoluble in H2O; insoluble in EtOH
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Yuan L, Liu X, et al. "Optimized HepaRG is a suitable cell source to generate the human liver chimeric mouse model for the chronic hepatitis B virus infection." Emerg Microbes Infect. 2018 Aug 10;7(1):144. PMID:30097574
    2. Yuan L, Liu X, et al. "A Chimeric Humanized Mouse Model by Engrafting the Human Induced Pluripotent Stem Cell-Derived Hepatocyte-Like Cell for the Chronic Hepatitis B Virus Infection." Front Microbiol. 2018 May 8;9:908. PMID:29867819

XMU-MP-1

XMU-MP-1

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