1. PI3K/Akt/mTOR Cell Cycle/DNA Damage Apoptosis
  2. PI3K CDK Apoptosis
  3. FOXM1-IN-3

FOXM1-IN-3 is a potent FOXM1 inhibitor. FOXM1-IN-3 downregulates FOXM1 expression at protein and mRNA levels, suppressing downstream effectors CCNB1 and CDC25. FOXM1-IN-3 induces G2/M cell cycle arrest and apoptosis in colorectal cancer cells. FOXM1-IN-3 inhibits colony formation and cell migration in colorectal cancer cells. FOXM1-IN-3 targets the cancer stem cell phenotype in colorectal cancer cells, reducing cancer stem cell marker expression. FOXM1-IN-3 reduces tumor growth in a zebrafish xenograft model. FOXM1-IN-3 can be used for the research of colorectal cancer.

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FOXM1-IN-3

FOXM1-IN-3 Chemical Structure

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Description

FOXM1-IN-3 is a potent FOXM1 inhibitor. FOXM1-IN-3 downregulates FOXM1 expression at protein and mRNA levels, suppressing downstream effectors CCNB1 and CDC25. FOXM1-IN-3 induces G2/M cell cycle arrest and apoptosis in colorectal cancer cells. FOXM1-IN-3 inhibits colony formation and cell migration in colorectal cancer cells. FOXM1-IN-3 targets the cancer stem cell phenotype in colorectal cancer cells, reducing cancer stem cell marker expression. FOXM1-IN-3 reduces tumor growth in a zebrafish xenograft model. FOXM1-IN-3 can be used for the research of colorectal cancer[1].

IC50 & Target

FOXM1

 

PI3Kγ

3.5 μM (IC50)

In Vitro

FOXM1-IN-3 (compound 14) (6.25-100 μM; 24 h) potently inhibits proliferation in SW620 and SW480 colorectal cancer cells with IC50 values of 14.9 μM and 17.5 μM, respectively, and shows favorable selectivity over normal CCD841 cells (IC50 of 36.65 μM)[1].
FOXM1-IN-3 (0.75-3 μM; 7 days) almost completely inhibits colony formation in SW480 and SW620 cells at 3 μM, reflecting long-term antiproliferative effects[1].
FOXM1-IN-3 (6.25-25 μM; 48 h) suppresses cell migration in SW480 cells at 6.25 μM and in SW620 cells at 12.5 μM over 48 h[1].
FOXM1-IN-3 shows measurable inhibition of PI3Kβ, γ, and δ[1].
FOXM1-IN-3 (6.25-25 μM; 24 h) downregulates FOXM1 and its downstream effectors CCNB1 and CDC25 in SW480 and SW620 cells at concentrations as low as 6.25 μM[1].
FOXM1-IN-3 (6.25-25 μM; 24 h) causes G2/M phase arrest in SW480 and SW620 cells, correlating with FOXM1 downregulation[1].
FOXM1-IN-3 (6.25-25 μM; 24 h) induces apoptosis in SW480 and SW620 cells at 12.5 μM and 25 μM[1].
FOXM1-IN-3 (10 μM; 24 h, 48 h) selectively targets cancer stem cell (CSC) phenotypes in SW480 and SW620 cells at 10 μM, with mild and reversible effects on normal CCD841 cells[1].
FOXM1-IN-3 has high passive permeability, low CYP interference, notable hepatotoxicity (IC50 ~5.6 μM in HepG2), and lower neurotoxicity (IC50 ~17 μM in SH-SY5Y)[1].

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

Cell Viability Assay[1]

Cell Line: SW620, SW480, CCD841
Concentration: 100 μM, 50 μM, 25 μM, 12.5 μM, 6.25 μM
Incubation Time: 24 h
Result: Demonstrated antiproliferative effects with IC₅₀ values of 14.9 μM (SW620), 17.5 μM (SW480), and 36.7 μM (CCD841), yielding selectivity indices of 2.1-2.5.

Cell Migration Assay[1]

Cell Line: SW480, SW620
Concentration: 25 μM, 12.5 μM, 6.25 μM
Incubation Time: 48 h
Result: Significantly impaired migration ability, with inhibition observed at 6.25 μM in SW480 cells and at 12.5 μM in SW620 cells.

Cell Cycle Analysis[1]

Cell Line: SW480, SW620
Concentration: 25 μM, 12.5 μM, 6.25 μM
Incubation Time: 24 h
Result: Induced a dose-dependent accumulation of cells in the G2/M phase along with a significant reduction in the S phase population in both cell lines.

Apoptosis Analysis[1]

Cell Line: SW480, SW620
Concentration: 25 μM, 12.5 μM, 6.25 μM
Incubation Time: 24 h
Result: Increased levels of both early and late apoptotic cells in a dose-dependent manner, particularly at 12.5 μM and 25 μM.
In Vivo

FOXM1-IN-3 (compound 14) (5-10 μM; immersion; 72 hours) inhibits tumor growth in a zebrafish xenograft model, with the most pronounced effect in the SW620 line (80.95% tumor growth at 10 μM relative to control)[1].

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

Animal Model: Zebrafish species Danio rerio (wild-type AB)[1]
Dosage: 5, 10 μM
Administration: immersion; 72 hours
Result: For SW620 xenografts, showed 85.06% tumor growth relative to control at 5 μM and 80.95% at 10 μM at 3 days post-injection (dpi).
For SW480 xenografts, showed 92.65% tumor growth relative to control at 5 μM and 90.05% at 10 μM at 3 dpi.
Molecular Weight

564.12

Formula

C29H38ClN9O

SMILES

C1(NCCC2=CNC3=C2C=CC=C3)=NC(NCCN4CCN(C5=CC=CC=C5)CC4)=NC(N6CCOCC6)=N1.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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    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.

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Product Name:
FOXM1-IN-3
Cat. No.:
HY-181076
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