XMU-MP-1

SKU: orb1303057

Description

XMU-MP-1 is a potent, reversible, and selective inhibitor of the kinases MST1 and MST2, with IC50 values of 71.1 nM and 38.1 nM, respectively. This small molecule is a valuable research tool for studying the Hippo signaling pathway in both cellular and in vivo models of tissue regeneration and cancer.

Research Area

Neuroscience, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 2061980-01-4
• MW: 416.5
• Purity: >98%
• Formula: C₁₇H₁₆N₆O₃S₂
• SMILES: CN1c2ccsc2C(=O)N(C)c2cnc(Nc3ccc(cc3)S(N)(=O)=O)nc12
• Target: Kinase
• Solubility: Soluble in DMSO (up to 15 mg/ml)

Bioactivity

• Target IC50:
  MST4:27.3 nM|MST1:71.1 nM|MST2:38.1 nM|MST2:18.2 nM|MST3:44.8 nM
• In Vivo:
  METHODS: To study the effect of XMU-MP-1 on cardiac function, C57Bl/6 mice underwent transverse aortic cotation (TAC) surgery to induce cardiac hypertrophy and dysfunction. XMU-MP-1 (1 mg/kg) or solvent (DMSO) treatment was administered 3 weeks after the operation, once every 2 days for 10 consecutive days. RESULTS: The cardiac systolic function of mice treated with XMU-MP-1 was significantly improved, manifested as an increase in ejection fraction. The cross-sectional area of myocardial cells in mice treated with XMU-MP-1 decreased, and the expression of the hypertrophy marker brain natriuretic peptide (BNP) decreased. The number of TunEL-positive cardiomyocytes in the hearts of mice treated with XMU-MP-1 decreased, and the degree of fibrosis was reduced, indicating that this drug inhibited cardiomyocyte apoptosis and fibrosis. METHODS: To study the ability of XMU-MP-1 in liver injury repair, XMU-MP-1 (1-3 mg/kg) was intraperitoneally injected into mouse models of acute/chronic liver injury. RESULTS: XMU-MP-1 has good pharmacokinetic characteristics in vivo and can improve the repair and regeneration ability of the intestinal tract and liver of mice. METHODS: To study the anti-tumor activity of XMU-MP-1, XMU-MP-1 was injected daily into NSG mice supplemented with estrogen. RESULTS: XMU-MP-1 significantly inhibited tumor growth in MCF-7 xenografts, and the treated xenografts showed increased nuclear localization of YAP and expression of target genes. METHODS: To study the effect of XMU-MP-1 on osteoarthritis, XMU-MP-1 (1 mg/kg) was intraperitoneally injected into a mouse model of osteoarthritis for two consecutive weeks. RESULTS: XMU-MP-1 can inhibit the erosion of the articular cartilage surface and the thickening of the synovial membrane, and alleviate the symptoms of osteoarthritis.
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• In Vitro:
  METHODS: HepG2 cells, mouse macrophage-like cells, human osteosarcoma, and human colorectal adenocarcinoma cells were treated with XMU-MP-1 (0-3 μM) for 15 minutes, and the phosphorylation levels were detected by western blot. RESULTS: XMU-MP-1 reduces the phosphorylation of endogenous MOB1, LATS1/2 and YAP in HepG2 cells in a dose-dependent manner. XMU-MP-1 inhibits hydrogen peroxide-stimulated phosphorylation of MOB1 and autophosphorylation of MST1/2 in mouse macrophagocyte-like cells, human osteosarcoma, and human colorectal adenocarcinoma cells.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

MST2, MST1, inhibit, Inhibitor, Hippopathway, Hippo (MST), Hippo pathway, XMU MP 1, XMUMP1, XMU-MP-1

Compound Identifiers

PubChem CID

121499143