MST3-IN-1
MST3-IN-1 is a selective and orally active MST3 inhibitor, with an IC50 of 122.4 nM. MST3-IN-1 shows antiproliferative activity against HepG2 cell. MST3-IN-1 effectively induces apoptosis in HepG2 cells, and halts the cell cycle at the G2/M transition. MST3-IN-1 significantly suppressed tumor growth in HepG2 xenograft mice. MST3-IN-1 can be used for the study of liver cancer.
For research use only. We do not sell to patients.
- CAS No.: 3095435-97-2
- Formula: C25H21F4N5O3S
- Molecular Weight:547.52
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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Biological Activity
MST3-IN-1 (Compound LD-1) exhibits antiproliferative activities to cancer cell lines with GI50s of 0.68 μM (HepG2 cells), 0.77 μM (HCT116 cells) and 0.83 μM (H226 cells) and inhibits HK2 cells are all greater than 30 μM, showing good selectivity[1]. MST3-IN-1 (1 μM) shows an inhibition rate of 95.49 % against MST3, and the inhibition rate against the secondranked kinase, AKT2, is only 66.51 %[1]. MST3-IN-1 (0.25-2 μM, 24 h) induces apoptosis in HepG2 cells and may inhibit HepG2 cells proliferation by prolonging the G2/M phase[1]. MST3-IN-1 (0.25-2 μM, 24 h) reduces the expression level of p-MST3 in a concentration-dependent manner and does not affect the expression level of MST3[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 cells
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Concentration:0.5, 1, 2 μM
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Incubation Time:24 h
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Result:Induced apoptosis in HepG2 cells.
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Cell Line:HepG2 cells
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Concentration:0.5, 1, 2 μM
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Incubation Time:48 h
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Result:Revealed distinct morphological characteristics of apoptosis, including chromatin condensation and nuclear fragmentation.
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Cell Line:HepG2 cells
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Concentration:0.25, 0.5, 1 μM
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Incubation Time:24 h
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Result:Increased the proportion of cells at the G2/M phase.
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Cell Line:HepG2 cells
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Concentration:0.33, 1, 3 μM
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Incubation Time:24 h
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Result:Reduced the expression level of p-MST3.
Increased the expression level of cleaved caspase-3.
Reduced the expression levels of caspase-3 and Bcl-2.
Did not affect the expression level of MST3.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:HepG2 cells (5 × 106) were injected subcutaneously into the right armpit of the mice[1]
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Dosage:40 mg/kg
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Administration:i.g. daily for 15 days
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Result:Exhibited a significant tumor growth inhibition (TGI) rate of 47.64%, outperforming the current first-line treatment agent Sorafenib (HY-10201) (TGI = 32.52%). Showed no mouse mortality or significant body weight loss was observed across all dosage groups.
Chemical Information
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CAS No. 3095435-97-2
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Molecular Weight 547.52
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Formula C25H21F4N5O3S
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SMILES
O=C(C1=CN(C2CC2)C3=CC(N4CCNCC4)=C(C=C3C1=O)F)NC5=NC6=C(S5)C=C(OC(F)(F)F)C=C6
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MST3-IN-1 Related Classifications
HY-175208 Related Classifications
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