IHMT-MST1-58
Based on 1 Customer Validation
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.
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- Purity: 99.05%
- CAS No.: 2414484-25-4
- 화학식: C21H22N6O3S
- 분자량:438.50
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Anti-Liver Cancer Compound Library
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Anti-Colorectal Cancer Compound Library
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Heterocyclic Compound Library
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Highly Selective Inhibitors Library
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Bioactive Compound Library Max
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Anti-Aging Compound Library Mini
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MCE Bioactive Compound Library
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Bioactive Compound Library
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Protein Kinase Compound Library
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High-Throughput Bioactive Compound Library
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Biological Activity
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MST1 23 nM (IC50) |
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.
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Cell Line:HepG2 liver cells, RAW264.7, RPE1 and HL7702 cells; INS-1 and RIN-m5F cell lines
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Concentration:0-10 μM
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Incubation Time:2 h (HepG2 liver cells, RAW264.7, RPE1, and HL7702 cells)
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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.
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.
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Animal Model:mice[1]
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Dosage:50 mg/kg
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Administration:oral, single
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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
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Animal Model:T1D mouse models and T2D mouse models[1]
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Dosage:50 mg/kg
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Administration:p.o, 50 mg/kg/day, QD
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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.
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Animal Model:mice, Sprague Dawley rats, and beagle dogs[1]
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Dosage:1 mg/kg, 5 mg/kg and 10 mg/kg
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Administration:intravenous injection and oral administration
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Result:Displayed acceptable pharmacokinetic properties in different species.
Chemical Information
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CAS No. 2414484-25-4
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Appearance Solid
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분자량 438.50
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화학식 C21H22N6O3S
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Color Off-white to light yellow
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SMILES
O=S(C1=CC=C(NC(N=C2N(C)C3C4=CC=CC=C4C)=NC=C2N(C)C3=O)C=C1)(N)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
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Data Sheet (279 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
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 |
IHMT-MST1-58 Related Classifications
HY-151257 Related Classifications
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