2. Stem Cell/Wnt Apoptosis
  3. Hippo (MST) Caspase Bcl-2 Family Apoptosis
  4. 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.

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MST3-IN-1

MST3-IN-1 Chemical Structure

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MST3-IN-1 Related Antibodies

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Description

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[1].

In Vitro

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.

MST3-IN-1 Related Antibodies

Apoptosis Analysis[1]

Cell Line: HepG2 cells
Concentration: 0.5, 1, 2 μM
Incubation Time: 24 h
Result: Induced apoptosis in HepG2 cells.

Immunofluorescence[1]

Cell Line: HepG2 cells
Concentration: 0.5, 1, 2 μM
Incubation Time: 48 h
Result: Revealed distinct morphological characteristics of apoptosis, including chromatin condensation and nuclear fragmentation.

Cell Cycle Analysis[1]

Cell Line: HepG2 cells
Concentration: 0.25, 0.5, 1 μM
Incubation Time: 24 h
Result: Increased the proportion of cells at the G2/M phase.

Western Blot Analysis[1]

Cell Line: HepG2 cells
Concentration: 0.33, 1, 3 μM
Incubation Time: 24 h
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.
In Vivo

MST3-IN-1 (Compound LD-1) (40 mg/kg, i.g., daily for 15 days) demonstrates good efficacy in inhibiting the growth of hepatocellular carcinoma tumors in HepG2 xenograft mice[1].

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

Animal Model: HepG2 cells (5 × 106) were injected subcutaneously into the right armpit of the mice[1]
Dosage: 40 mg/kg
Administration: i.g. daily for 15 days
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.
Molecular Weight

547.52

Formula

C25H21F4N5O3S
SMILES

O=C(C1=CN(C2CC2)C3=C(C=C(F)C(N4CCNCC4)=C3)C1=O)NC5=NC6=CC=C(OC(F)(F)F)C=C6S5
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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MST3-IN-1 Related Classifications

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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:

MST3-IN-1Hippo (MST)CaspaseBcl-2 FamilyApoptosisMST3cancerHepG2 cellsInhibitorinhibitorinhibit

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