Art. -Nr.: HY-164595

IHMT-MST1-39

Kundenbewertung

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).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.68%
CAS. Nr.: 2414484-01-6
Formel: C₂₀H₁₈F₂N₆O₃S
Molecular Weight:460.46

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

IHMT-MST1-39 Chemical Structure

CAS. Nr.: 2414484-01-6

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

MST1

42 nM (IC₅₀)

MST2

109 nM (IC₅₀)

MST3

289 nM (IC₅₀)

MST4

159 nM (IC₅₀)

Alle Hippo (MST) Isoform-spezifische Produkte anzeigen :

Alle AMPK Isoform-spezifische Produkte anzeigen :

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.

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

Species	Dose	Route	T_1/2	T_max	C_max	AUC_0-t	AUC_0-∞	V_z	CL	MRT_0-t	MRT_0-∞	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 %

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 Lepr^db 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.

Chemical Information

CAS. Nr. 2414484-01-6
Appearance Solid
Molecular Weight 460.46
Formel C₂₀H₁₈F₂N₆O₃S
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1717 mL

10.8587 mL

21.7174 mL

5 mM

0.4343 mL

2.1717 mL

4.3435 mL

10 mM

0.2172 mL

1.0859 mL

2.1717 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Wang J, et al. Discovery of IHMT-MST1-39 as a novel MST1 kinase inhibitor and AMPK activator for the treatment of diabetes mellitus. Signal Transduct Target Ther. 2023 Apr 5;8(1):143. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

IHMT-MST1-39

Bioactive Compound Library Max

Bioactive Compound Library

Apoptosis Compound Library

Epigenetics Compound Library

PI3K/Akt/mTOR Compound Library

Stem Cell Signaling Compound Library

Anti-Aging Compound Library

Antioxidant Compound Library

Anti-diabetic Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Lipid Metabolism Compound Library

Glucose Metabolism Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Pain-Related Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Multi-Target Compound Library

Radioprotector Library

Anti-Aging Compound Library Mini

MCE Bioactive Compound Library

Anti-Fibrosis Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Lactic Acid Metabolic Compound Library

High-Throughput Bioactive Compound Library

Alle Hippo (MST) Isoform-spezifische Produkte anzeigen

Alle AMPK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

IHMT-MST1-39 Related Classifications

HY-164595 Related Classifications