2. Stem Cell/Wnt Apoptosis PI3K/Akt/mTOR Epigenetics
  3. Hippo (MST) Apoptosis AMPK
  4. IHMT-MST1-39

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).

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IHMT-MST1-39

IHMT-MST1-39 Chemical Structure

CAS No. : 2414484-01-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

IHMT-MST1-39 Related Antibodies

Top Publications Citing Use of Products

View All Hippo (MST) Isoform Specific Products:

View All Isoforms
MST1 MST2 MST3 MST4

View All AMPK Isoform Specific Products:

View All Isoforms
NUAK1 NUAK2 AMPK AMPK α1β1γ1 AMPK α2β1γ1 AMPK α1β2γ1 AMPK α2β2γ1 BRSK1 BRSK2 HUNK AMPKα

  • Biological Activity

  • Purity & Documentation

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  • Customer Review

Description

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)[1].

IC50 & Target[1]

MST1

42 nM (IC50)

MST2

109 nM (IC50)

MST3

289 nM (IC50)

MST4

159 nM (IC50)

In Vitro

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.

IHMT-MST1-39 Related Antibodies

Apoptosis Analysis[1]

Cell Line: Pancreatic β cells
Concentration: 1 μM
Incubation Time: 72 h
Result: Significantly reduced the rate of cell apoptosis induced by high glucose.

Western Blot Analysis[1]

Cell Line: Pancreatic β cells
Concentration: 0.1, 1 and 3 μM
Incubation Time: 72 h
Result: Dose-dependently reduced p-MST1 and p-H2B levels.
Reduced caspase 9/7/3 and PARP cleavage.

Western Blot Analysis[1]

Cell Line: HepG2 and HL7702 cells
Concentration: 0, 10, 20, 30, 40, 50, 60, 70, 80, 90, 100 μM
Incubation Time: 24 h
Result: Increased AMPKα phosphorylation at Thr172 (p-AMPKα).
Decreased ribosomal protein S6 (RPS6) phosphorylation at Ser235/236 and Ser240/244.
Parmacokinetics[1]
Species Dose Route Indicator value
Dog 50 mg/kg p.o. T1/2 4.86 h
Mice 50 mg/kg p.o. T1/2 2.96 h
Rat 50 mg/kg p.o. T1/2 2.22 h
Dog 50 mg/kg p.o. Tmax 0.5 h
Mice 50 mg/kg p.o. Tmax 1 h
Rat 50 mg/kg p.o. Tmax 0.667 h
Dog 50 mg/kg p.o. Cmax 1096 ng/mL
Mice 50 mg/kg p.o. Cmax 1619 ng/mL
Rat 50 mg/kg p.o. Cmax 1006 ng/mL
Dog 50 mg/kg p.o. AUC0-t 9296 ng·h/mL
Mice 50 mg/kg p.o. AUC0-t 7615 ng·h/mL
Rat 50 mg/kg p.o. AUC0-t 2716 ng·h/mL
Dog 50 mg/kg p.o. AUC0-∞ 9597 ng·h/mL
Mice 50 mg/kg p.o. AUC0-∞ 8282 ng·h/mL
Rat 50 mg/kg p.o. AUC0-∞ 2788 ng·h/mL
Dog 50 mg/kg p.o. Vz 3739 mL/kg
Mice 50 mg/kg p.o. Vz 5164 mL/kg
Rat 50 mg/kg p.o. Vz 12951 mL/kg
Dog 50 mg/kg p.o. CL 533 mL/h/kg
Mice 50 mg/kg p.o. CL 1207 mL/h/kg
Rat 50 mg/kg p.o. CL 3794 mL/h/kg
Dog 50 mg/kg p.o. MRT0-t 6.68 h
Mice 50 mg/kg p.o. MRT0-t 4.27 h
Rat 50 mg/kg p.o. MRT0-t 2.60 h
Dog 50 mg/kg p.o. MRT0-∞ 7.46 h
Mice 50 mg/kg p.o. MRT0-∞ 5.23 h
Rat 50 mg/kg p.o. MRT0-∞ 2.98 h
Dog 50 mg/kg p.o. F 151 %
Mice 50 mg/kg p.o. F 129.6 %
Rat 50 mg/kg p.o. F 52.6 %
In Vivo

IHMT-MST1-39 (50-250 mg/kg, i.g., once daily for 10-12 weeks) reverses diabetic symptoms in the Streptozotocin (STZ) (HY-13753)-induced T1D mouse model and prevents diabetic hyperglycemia in T2D mouse models[1].

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

Animal Model: STZ induced T1D model established in wild-type C57BL6/J mice[1]
Dosage: 50 and 250 mg/kg
Administration: Oral gavage (i.g.), once daily for 12 weeks
Result: Significantly reduced fasting blood glucose.
Improved glucose tolerance.
Reduced HbA1c levels.
Protected pancreatic islet structure and beta cell mass.
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]
Dosage: 50 and 250 mg/kg
Administration: Oral gavage (i.g.), once daily for 10-12 weeks
Result: Significantly improved glycemic control in monotherapy.
Demonstrated synergistic effects in combination with Metformin (HY-B0627).
Significantly improved insulin resistance.
Molecular Weight

460.46

Formula

C20H18F2N6O3S
CAS No.
Appearance

Solid

Color

White to off-white

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
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 : 50 mg/mL (108.59 mM; Need ultrasonic; 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 2.1717 mL 10.8587 mL 21.7174 mL
5 mM 0.4343 mL 2.1717 mL 4.3435 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.

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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.
Calculation results:
Working solution concentration: mg/mL
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 2.1717 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
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IHMT-MST1-39 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-MST1-392414484-01-6Hippo (MST)ApoptosisAMPKAMP-activated protein kinasetype 1 diabetesT1DC57BL/6?J mouseICR mousedb/db mouseorally activeInhibitorinhibitorinhibit

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