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XMU-MP-1

SKU: orb1303057
FeaturedFeatured Product

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

Images & Validation

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XMU-MP-1

Key Properties

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CAS Number2061980-01-4
MW416.5
Purity>98%
FormulaC17H16N6O3S2
SMILESCN1c2ccsc2C(=O)N(C)c2cnc(Nc3ccc(cc3)S(N)(=O)=O)nc12
TargetKinase
SolubilitySoluble in DMSO (up to 15 mg/ml)

Bioactivity

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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.
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.

Storage & Handling

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Storage-20°C
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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

Similar Products

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  • XMU-MP-1

    XMU-MP-1 [orb1225726]

    >98% (HPLC)

    2061980-01-4

    416.4773

    C17H16N6O3S2

    2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 200 mg, 500 mg, 1 g
Quality Guarantee

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Compound Identifiers

PubChem CID
121499143 ↗

Key Properties

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No computed properties available.

Protocol Information

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5 mg
$ 220.00
25 mg
$ 450.00
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