XMU-MP-1

Catalog No.S8334

XMU-MP-1 Chemical Structure

Molecular Weight(MW): 416.48

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.

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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

Cell Research:[1]
+ Expand
  • 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.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: FRG mice
  • Formulation: 20% Solutal
  • Dosages: 1 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 83 mg/mL (199.28 mM)
Ethanol 1 mg/mL (2.4 mM)
Water Insoluble
In vivo Add solvents individually and in order:
2% DMSO+30% PEG 300+2% Tween 80+ddH2O
5mg/mL

* 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.

Chemical Information

Molecular Weight 416.48
Formula

C17H16N6O3S2

CAS No.
Storage powder
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

  • Question 1:

    Does XMU-MP-1 form a clear solution in - 2% DMSO+30% PEG 300+2% Tween 80+ddH2O, at a concentration of 5 mg/ml? Is this the maximum solubility or is it possible to dissolve more drug to obtain a higher concentration?

  • Answer:

    XMU-MP-1 in 2% DMSO+30% PEG 300+2% Tween 80+ddH2O at 5mg/ml is a clear solution. It is the maximum concentration. If you want a higher concentration, the content of DMSO and PEG will also be increased

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID