IHMT-MST1-39
Based on 1 Customer Validation
IHMT-MST1-39 is an orally active inhibitor for MST kinase, with IC50 of 42, 109, 286, 159 nM for MST1, MST2, MST3, MST4. IHMT-MST1-39 activates the AMPK signaling pathway in liver cells, reduces apoptosis of pancreatic β-cells. IHMT-MST1-39 can be used for the studies of type 1 diabetes (T1D) and type 2 diabetes (T2D).
For research use only. We do not sell to patients.
- Purity: 99.68%
- CAS No.: 2414484-01-6
- Formula: C20H18F2N6O3S
- Molecular Weight:460.46
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
All AMPK Isoforms
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Biological Activity
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MST1 42 nM (IC50) |
MST2 109 nM (IC50) |
MST3 289 nM (IC50) |
MST4 159 nM (IC50) |
IHMT-MST1-39 (0.3-3 μM, 72 h) blocks pancreatic β cell apoptosis through MST1 inhibition and improves pancreatic β cell function and survival under diabetogenic conditions[1].
IHMT-MST1-39 (0-100 μM, 24 h) activates AMPK signaling in an MST1-independent manner in HepG2 and HL7702 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Pancreatic β cells
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Concentration:1 μM
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Incubation Time:72 h
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Result:Significantly reduced the rate of cell apoptosis induced by high glucose.
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Cell Line:Pancreatic β cells
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Concentration:0.1, 1 and 3 μM
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Incubation Time:72 h
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Result:Dose-dependently reduced p-MST1 and p-H2B levels.
Reduced caspase 9/7/3 and PARP cleavage.
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Cell Line:HepG2 and HL7702 cells
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Concentration:0, 10, 20, 30, 40, 50, 60, 70, 80, 90, 100 μM
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Incubation Time:24 h
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Result:Increased AMPKα phosphorylation at Thr172 (p-AMPKα).
Decreased ribosomal protein S6 (RPS6) phosphorylation at Ser235/236 and Ser240/244.
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUC0-t | AUC0-∞ | Vz | CL | MRT0-t | MRT0-∞ | F |
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Dog[1] | 50 mg/kg | p.o. | 4.86 h | 0.5 h | 1096 ng/mL | 9296 ng·h/mL | 9597 ng·h/mL | 3739 mL/kg | 533 mL/h/kg | 6.68 h | 7.46 h | 151 % |
| Mice[1] | 50 mg/kg | p.o. | 2.96 h | 1 h | 1619 ng/mL | 7615 ng·h/mL | 8282 ng·h/mL | 5164 mL/kg | 1207 mL/h/kg | 4.27 h | 5.23 h | 129.6 % |
| Rat[1] | 50 mg/kg | p.o. | 2.22 h | 0.667 h | 1006 ng/mL | 2716 ng·h/mL | 2788 ng·h/mL | 12951 mL/kg | 3794 mL/h/kg | 2.60 h | 2.98 h | 52.6 % |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:STZ induced T1D model established in wild-type C57BL6/J mice[1]
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Dosage:50 and 250 mg/kg
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Administration:Oral gavage (i.g.), once daily for 12 weeks
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Result:Significantly reduced fasting blood glucose. Improved glucose tolerance. Reduced HbA1c levels. Protected pancreatic islet structure and beta cell mass.
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Animal Model:Spontaneous T2D established in diabetic Leprdb mice (db/db mice) and HFD/STZ-induced T2D model established in wild-type C57BL6/J mice and [1]
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Dosage:50 and 250 mg/kg
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Administration:Oral gavage (i.g.), once daily for 10-12 weeks
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Result:Significantly improved glycemic control in monotherapy.
Demonstrated synergistic effects in combination with Metformin (HY-B0627).
Significantly improved insulin resistance.
Chemical Information
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CAS No. 2414484-01-6
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Appearance Solid
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Molecular Weight 460.46
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Formula C20H18F2N6O3S
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Color White to off-white
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SMILES
O=C1N(C)C2=CN=C(NC3=CC=C(S(=O)(N)=O)C=C3)N=C2N(C1C4=C(F)C=CC=C4F)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 50 mg/mL (108.59 mM; Need ultrasonic; 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)
Purity & Documentation
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Data Sheet (277 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 | 2.1717 mL | 10.8587 mL | 21.7174 mL | 54.2935 mL |
| 5 mM | 0.4343 mL | 2.1717 mL | 4.3435 mL | 10.8587 mL | |
| 10 mM | 0.2172 mL | 1.0859 mL | 2.1717 mL | 5.4294 mL | |
| 15 mM | 0.1448 mL | 0.7239 mL | 1.4478 mL | 3.6196 mL | |
| 20 mM | 0.1086 mL | 0.5429 mL | 1.0859 mL | 2.7147 mL | |
| 25 mM | 0.0869 mL | 0.4343 mL | 0.8687 mL | 2.1717 mL | |
| 30 mM | 0.0724 mL | 0.3620 mL | 0.7239 mL | 1.8098 mL | |
| 40 mM | 0.0543 mL | 0.2715 mL | 0.5429 mL | 1.3573 mL | |
| 50 mM | 0.0434 mL | 0.2172 mL | 0.4343 mL | 1.0859 mL | |
| 60 mM | 0.0362 mL | 0.1810 mL | 0.3620 mL | 0.9049 mL | |
| 80 mM | 0.0271 mL | 0.1357 mL | 0.2715 mL | 0.6787 mL | |
| 100 mM | 0.0217 mL | 0.1086 mL | 0.2172 mL | 0.5429 mL |