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XMU-MP-1

Name: XMU-MP-1
Brand: TargetMol
SKU: T4212
Price: 48 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T4212Cas No. 2061980-01-4

XMU-MP-1 is a reversible and selective MST1/2 kinase inhibitor, and its IC50 values for MST1 and MST2 are 71.1 nM and 38.1 nM, respectively.

XMU-MP-1

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Purity: 99.97%

Catalog No. T4212Cas No. 2061980-01-4

XMU-MP-1 is a reversible and selective MST1/2 kinase inhibitor, and its IC50 values for MST1 and MST2 are 71.1 nM and 38.1 nM, respectively.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$48	In Stock	In Stock
2 mg	$72	In Stock	In Stock
5 mg	$98	In Stock	In Stock
10 mg	$155	In Stock	In Stock
25 mg	$322	In Stock	In Stock
50 mg	$538	In Stock	In Stock
100 mg	$698	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$96	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Purity:99.97%

Color:White

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Product Introduction

Bioactivity

Description	XMU-MP-1 is a reversible and selective MST1/2 kinase inhibitor, and its IC50 values for MST1 and MST2 are 71.1 nM and 38.1 nM, respectively.
Targets&IC50	MST2:38.1 nM, MST1:71.1 nM, MST3:44.8 nM, MST4:27.3 nM, MST2:18.2 nM
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. [1]
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. [2] 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. [3] 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.
Kinase Assay	XMU-MP-1 is dissolved in DMSO (stock concentration, 10 mM). For the in vitro kinase inhibition assays, recombinant GST-tagged MOB1a and various forms of recombinant His-tagged full-length MST1 or MST2 kinase are expressed and purified from Escherichia coli. The assays are performed with the various doses of XMU-MP-1 in the kinase assay buffer for 30 min at 30°C[1].

Chemical Properties

Molecular Weight	416.48
Formula	C₁₇H₁₆N₆O₃S₂
Cas No.	2061980-01-4
Smiles	CN1c2ccsc2C(=O)N(C)c2cnc(Nc3ccc(cc3)S(N)(=O)=O)nc12
Relative Density.	1.523 g/cm3 (Predicted)

Storage & Solubility Information

Storage

store at low temperature | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 12.5 mg/mL (30.01 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 0.5 mg/mL (1.2 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.4011 mL	12.0054 mL	24.0108 mL	120.0538 mL
5 mM	0.4802 mL	2.4011 mL	4.8022 mL	24.0108 mL
10 mM	0.2401 mL	1.2005 mL	2.4011 mL	12.0054 mL
20 mM	0.1201 mL	0.6003 mL	1.2005 mL	6.0027 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc