XMU-MP-1

Catalog No.S8334 Batch:S833401

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Technical Data

Formula

C17H16N6O3S2
Molecular Weight 416.48 CAS No. 2061980-01-4
Solubility (25°C)* In vitro DMSO 83 mg/mL (199.28 mM)
Ethanol 2 mg/mL (4.8 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description XMU-MP-1 is an inhibitor of MST1/2 with IC50 values of 71.1±12.9 nM and 38.1±6.9 nM against MST1 and MST2, respectively.
Targets
MST2 [1]
(Cell-free assay)		 MST1 [1]
(Cell-free assay)
38.1 nM 71.1 nM
In vitro 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[1].
In vivo 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[1].

Protocol (from reference)

Cell Assay:[1]
  • Cell lines

    HepG2

  • Concentrations

    1 μM or 3 μM

  • Incubation Time

    6 h

  • Method

    Real-time quantitative polymerase chain reaction (RT-qPCR) analysis of the expression levels of CTGF and CYR61 in HepG2 cells after XMUMP- 1 treatment for 6 hours is conducted.

Animal Study:[1]
  • Animal Models

    FRG mice

  • Dosages

    1 mg/kg

  • Administration

    i.p.

Customer Product Validation

Data from [Data independently produced by , , FASEB J, 2019, 33(2):2514-2525]

Data from [Data independently produced by , , J Cell Physiol, 2019, 234(4):5117-5133]

Data from [Data independently produced by , , Phytother Res, 2018, 32(12):2456-2465]

Selleck's XMU-MP-1 has been cited by 47 publications

Targeting metastasis-initiating cancer stem cells in gastric cancer with leukaemia inhibitory factor [ Cell Death Discov, 2024, 10(1):120] PubMed: 38453889
ACADL-YAP axis activity in non-small cell lung cancer carcinogenicity [ Cancer Cell Int, 2024, 24(1):86] PubMed: 38402174
CircPOLA2 sensitizes non-small cell lung cancer cells to ferroptosis and suppresses tumorigenesis via the Merlin-YAP signaling pathway [ iScience, 2024, 27(9):110832] PubMed: 39310771
GPR137 inactivates Hippo signaling to promote gastric cancer cell malignancy [ Biol Direct, 2024, 19(1):3] PubMed: 38163861
Colonic crypt stem cell functions are controlled by tight junction protein claudin-7 through Notch/Hippo signaling [ Ann N Y Acad Sci, 2024, 10.1111/nyas.15137] PubMed: 38598500
WNT5a Signaling through ROR2 Activates the Hippo Pathway to Suppress YAP1 Activity and Tumor Growth [ Cancer Res, 2023, 83(7):1016-1030] PubMed: 36622276
Neutrophil Extracellular Traps Delay Diabetic Wound Healing by Inducing Endothelial-to-Mesenchymal Transition via the Hippo pathway [ Int J Biol Sci, 2023, 19(1):347-361] PubMed: 36594092
Neutrophil Extracellular Traps Delay Diabetic Wound Healing by Inducing Endothelial-to-Mesenchymal Transition via the Hippo pathway [ Int J Biol Sci, 2023, 19(1):347-361] PubMed: 36594092
Genetic and Pharmacological YAP Activation Induces Proliferation and Improves Survival in Human Induced Pluripotent Stem Cell-Derived Cardiomyocytes [ Cells, 2023, 12(17)2121] PubMed: 37681853
Genetic and Pharmacological YAP Activation Induces Proliferation and Improves Survival in Human Induced Pluripotent Stem Cell-Derived Cardiomyocytes [ Cells, 2023, 12(17)2121] PubMed: 37681853

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.