Home Hippo MST inhibitor XMU-MP-1

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XMU-MP-1 MST1/2 Inhibitor

Cat.No.S8334

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.
XMU-MP-1 MST inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 416.48

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability

Quality Control

Batch: S833401 DMSO]83 mg/mL]false]Ethanol]2 mg/mL]false]Water]Insoluble]false Purity: 99.88%
99.88

Chemical Information, Storage & Stability

Molecular Weight 416.48 Formula

C17H16N6O3S2

 Storage (From the date of receipt)
CAS No. 2061980-01-4 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CN1C2=C(C(=O)N(C3=CN=C(N=C31)NC4=CC=C(C=C4)S(=O)(=O)N)C)SC=C2

Solubility

In vitro
Batch:

DMSO : 83 mg/mL (199.28 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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% DMSO
%
% Tween 80
% ddH2O
% DMSO
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Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
MST2 [1]
(Cell-free assay)
38.1 nM
MST1 [1]
(Cell-free assay)
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. This compound inhibits phosphorylation of MOB1 in a dose-dependent manner. Furthermore, with increasing ATP concentration, it 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, this chemical reduces the phosphorylation of endogenous MOB1, LATS1/2, and YAP in human liver carcinoma (HepG2) cells in a dose-dependent manner. Similarly, its 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. This 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. This compound 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 this chemical (1 mg/kg). It protects mice from DSS-induced colitis and ameliorates chronic liver injury[1].
References

Applications

Methods Biomarkers Images PMID
Western blot p-YAP / YAP / p-MST1/2 / MST1 / p-MOB1 / MOB1 S8334-WB1 29262338

Tech Support

Handling Instructions

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Frequently Asked Questions

Question 1:
Does it 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 of this compound to obtain a higher concentration?

Answer:
In 2% DMSO+30% PEG 300+2% Tween 80+ddH2O at 5mg/ml, it is a clear solution. This is the maximum concentration. If you want a higher concentration, the content of DMSO and PEG will also be increased.