1. GPCR/G Protein Neuronal Signaling Cell Cycle/DNA Damage
  2. 5-HT Receptor DNA/RNA Synthesis
  3. FOXM1-IN-4

FOXM1-IN-4 is a selective 5-HT7 receptor inhibitor with a Ki of 92 nM. FOXM1-IN-4 blocks 5-HT7 receptor signaling to reduce FOXM1, p-FOXM1, cyclin B1, and cdc25B levels. FOXM1-IN-4 acts as an antiproliferative, clonogenic inhibitor, and cell cycle inhibitor that induces G2/M arrest, reduces G0/G1 population. FOXM1-IN-4 can be used for the research of triple-negative breast cancer.

For research use only. We do not sell to patients.

FOXM1-IN-4

FOXM1-IN-4 Chemical Structure

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Description

FOXM1-IN-4 is a selective 5-HT7 receptor inhibitor with a Ki of 92 nM. FOXM1-IN-4 blocks 5-HT7 receptor signaling to reduce FOXM1, p-FOXM1, cyclin B1, and cdc25B levels. FOXM1-IN-4 acts as an antiproliferative, clonogenic inhibitor, and cell cycle inhibitor that induces G2/M arrest, reduces G0/G1 population. FOXM1-IN-4 can be used for the research of triple-negative breast cancer[1].

IC50 & Target[1]

5-HT7 Receptor

92 nM (Ki)

5-HT7 Receptor

11 nM (Kb)

In Vitro

FOXM1-IN-4 (Compound 36) binds strongly to the 5-HT7 receptor expressed in HEK293 cells, with a Ki of 92 nM and a Kb of 11 nM[1].
FOXM1-IN-4 (0.1-315.5 μM; 24 h) potently inhibits proliferation of MDA-MB-468, MDA-MB-231, and Hs578T TNBC cells with IC50 values of 7.1 μM, 11.3 μM, and 6.7 μM respectively, and shows limited cytotoxicity against NHDF cells with an IC50 of 12.2 μM[1].
FOXM1-IN-4 (0.7-6.7 μM); 7 days) dose-dependently suppresses long-term clonogenic growth of MDA-MB-231 and Hs578T TNBC cells[1].
FOXM1-IN-4 (1.5 × IC50; 24 h) induces G2/M phase cell cycle arrest in MDA-MB-231 TNBC cells[1].
FOXM1-IN-4 (16.95 μM; 24 h) suppresses FOXM1 activation and downstream G2/M regulator expression (cyclin B1, cdc25B) in MDA-MB-231 TNBC cells after 24 h of treatment at 1.5 × IC50[1].
FOXM1-IN-4 (5.63-22.6 μM; 24 h) exhibits enhanced antiproliferative activity in MDA-MB-231 TNBC cells pretreated with serotonin (10-20 μM; 48 h), with the strongest effect observed with 20 μM serotonin pretreatment[1].

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

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231, Hs578T (TNBC cell lines)
Concentration: 0.7 μM; 1.4 μM; 2.8 μM; 5.7 μM; 0.8 μM; 1.7 μM; 3.4 μM; 6.7 μM
Incubation Time: 7 days
Result: Significantly and dose-dependently reduced colony formation in both cell lines.
In MDA-MB-231 cells, the highest tested concentration (5.7 μM) caused the strongest reduction in colony numbers, with weaker effects at lower doses.
In Hs578T cells, reduced clonogenic growth at higher concentrations, with statistically significant inhibitory effects observed.

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231, Hs578T (TNBC cell lines)
Concentration: 16.95 μM
Incubation Time: 24 h
Result: In MDA-MB-231 cells, caused a marked decrease in the proportion of cells in the G0/G1 phase and a modest increase in the G2/M phase population, inducing cell cycle arrest.

Western Blot Analysis[1]

Cell Line: MDA-MB-231, Hs578T (TNBC cell lines)
Concentration: 16.95 μM
Incubation Time: 24 h
Result: In MDA-MB-231 cells, reduced total FOXM1 expression by over 2.6-fold and reduced p-FOXM1 levels by approximately 2.7-fold.
Caused a reduction in cyclin B1 and cdc25B protein levels in MDA-MB-231 cells.
Molecular Weight

456.59

Formula

C26H32N8

SMILES

NC1=NC(NCCN2CCN(C3=CC=CC=C3)CC2)=CC(NCCC4=CNC5=C4C=CC=C5)=N1

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-4
Cat. No.:
HY-182285
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