2. Stem Cell/Wnt
  3. Hippo (MST)
  4. IHMT-MST1-58

IHMT-MST1-58 is a potent, selective mammalian and orally active STE20-like protein 1 kinase (MST1) inhibitor with IC50 value of 23 nM. IHMT-MST1-58 can be used for the research of Type 1/2 diabetes.

For research use only. We do not sell to patients.

IHMT-MST1-58 Chemical Structure

IHMT-MST1-58 Chemical Structure

CAS No. : 2414484-25-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 330 In-stock
Solution
10 mM * 1 mL in DMSO USD 330 In-stock
Solid
5 mg USD 300 In-stock
10 mg USD 480 In-stock
25 mg USD 850 In-stock
50 mg USD 1200 In-stock
100 mg USD 1700 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

IHMT-MST1-58 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

IHMT-MST1-58 is a potent, selective mammalian and orally active STE20-like protein 1 kinase (MST1) inhibitor with IC50 value of 23 nM. IHMT-MST1-58 can be used for the research of Type 1/2 diabetes[1].

IC50 & Target[1]

MST1

23 nM (IC50)

In Vitro

IHMT-MST1-58 (compound 19) shows good activity against MST1 with an IC50 value of 23 nM[1].
IHMT-MST1-58 (1 μM) displays strong inhibitory activity against MST1 (IC50 = 23 nM), weak activity against MST2 (IC50 = 652 nM), but no activity against NEK3 even at 10 μM (IC50 > 10 μM) [1].
IHMT-MST1-58 (1 μM) shows strong binding affinity to MST1 and weak binding affinity to MST2 with Kd values of 240 nM and 2.7 μM[1].
IHMT-MST1-58 (0.1-10 μM; 1-2 h) inhibits the phosphorylation of MST1 in vitro[1].
IHMT-MST1-58 (0.03, 0.1 and 0.3 μM; 48 h) exhibits a significant protective effect of β cells from the damage caused by inflammatory cytokines[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

IHMT-MST1-58 Related Antibodies

Western Blot Analysis[1]

Cell Line: HepG2 liver cells, RAW264.7, RPE1 and HL7702 cells; INS-1 and RIN-m5F cell lines
Concentration: 0-10 μM
Incubation Time: 2 h (HepG2 liver cells, RAW264.7, RPE1, and HL7702 cells)
Result: Inhibited the H2O2-stimulated MOB1 phosphorylation and MST1/2 autophosphorylation in a dose-dependent manner in all four cell lines.
Inhibited the phosphorylation of LATS1 (T1079) and YAP (S127) in HepG2 cells.
Showed strong inhibition of MST1 phosphorylation and its downstream MOB1 autophosphorylation in a dose-dependent manner in both cell lines.
In Vivo

IHMT-MST1-58 (compound 19) (p.o, 50 mg/kg/day, QD) combination with metformin led to the decline of fasting blood glucose, show protective effect of β cells and decrease the hemoglobin A1c level in the STZ-induced T1D/T2D mouse models[1].
Pharmacokinetic Parameters of IHMT-MST1-58 in different species (i.v. or p.o; 1 mg/kg, 5 mg/kg and 10 mg/kg)[1].

mice rats beagle dogs
parameter i.v.(1 mg/kg) p.o.(10 mg/kg) i.v.(1 mg/kg) p.o.(10 mg/kg) i.v.(1 mg/kg) p.o.(10 mg/kg)
AUC0-t(ng/mL*h) 501.1 5583 2553±155.1 4858±2648 764.5±82.9 4939±1067
t1/2(h) 1.7 1.81 3.51±0.34 3.03±0.2 6.47±0.71 5.79±1.09
Cmax/F (ng/mL) 1240 1922 944.0±219.1 1717±276 466.7±45.2 1113±417
F(%) - 110.8 - 73.3±40.1 - 106.5±20.9

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: mice[1]
Dosage: 50 mg/kg
Administration: oral, single
Result:
parameter plasma pancreas
Cmax(ng/mL) 3990±390 12216±1509
AUC0-t(ng/mL*h) 13621±2127 51394±10098
Cl(mL/h/kg) 3734±641 996±189
Animal Model: T1D mouse models and T2D mouse models[1]
Dosage: 50 mg/kg
Administration: p.o, 50 mg/kg/day, QD
Result: Decreased the FBG level, improved the food intake and water consumption, had low HbA1c and a good antidiabetic effect, improved the histological structure of the islet.
Animal Model: mice, Sprague Dawley rats, and beagle dogs[1]
Dosage: 1 mg/kg, 5 mg/kg and 10 mg/kg
Administration: intravenous injection and oral administration
Result: Displayed acceptable pharmacokinetic properties in different species.
Molecular Weight

438.50

Formula

C21H22N6O3S
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=S(C1=CC=C(NC(N=C2N(C)C3C4=CC=CC=C4C)=NC=C2N(C)C3=O)C=C1)(N)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (228.05 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2805 mL 11.4025 mL 22.8050 mL
5 mM 0.4561 mL 2.2805 mL 4.5610 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (5.70 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (5.70 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2805 mL 11.4025 mL 22.8050 mL 57.0125 mL
5 mM 0.4561 mL 2.2805 mL 4.5610 mL 11.4025 mL
10 mM 0.2281 mL 1.1403 mL 2.2805 mL 5.7013 mL
15 mM 0.1520 mL 0.7602 mL 1.5203 mL 3.8008 mL
20 mM 0.1140 mL 0.5701 mL 1.1403 mL 2.8506 mL
25 mM 0.0912 mL 0.4561 mL 0.9122 mL 2.2805 mL
30 mM 0.0760 mL 0.3801 mL 0.7602 mL 1.9004 mL
40 mM 0.0570 mL 0.2851 mL 0.5701 mL 1.4253 mL
50 mM 0.0456 mL 0.2281 mL 0.4561 mL 1.1403 mL
60 mM 0.0380 mL 0.1900 mL 0.3801 mL 0.9502 mL
80 mM 0.0285 mL 0.1425 mL 0.2851 mL 0.7127 mL
100 mM 0.0228 mL 0.1140 mL 0.2281 mL 0.5701 mL
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IHMT-MST1-58 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

IHMT-MST1-582414484-25-4Hippo (MST)oralSTE20-like protein 1 kinase (MST1)Type 1/2 diabetesHepG2 liver cellsRAW264.7RPE1HL7702 cellsINS-1RIN-m5F cell linesInhibitorinhibitorinhibit

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