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

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

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

FOXM1-IN-4 hydrochloride

FOXM1-IN-4 hydrochloride Chemical Structure

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FOXM1-IN-4 hydrochloride Related Antibodies

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Description

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

In Vitro

FOXM1-IN-4 (Compound 36) hydrochloride 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) hydrochloride 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) hydrochloride dose-dependently suppresses long-term clonogenic growth of MDA-MB-231 and Hs578T TNBC cells[1].
FOXM1-IN-4 (1.5 × IC50; 24 h) hydrochloride induces G2/M phase cell cycle arrest in MDA-MB-231 TNBC cells[1].
FOXM1-IN-4 (16.95 μM; 24 h) hydrochloride 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) hydrochloride 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.

FOXM1-IN-4 hydrochloride Related Antibodies

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231, Hs578T (triple-negative breast cancer cells)
Concentration: 0.7-5.7 μM (MDA-MB-231 cells); 0.8-6.7 μM (Hs578T cells)
Incubation Time: 7 days
Result: Significantly reduced colony numbers in MDA-MB-231 cells in a dose-dependent manner, with the strongest inhibition at 5.7 μM.
Significantly reduced colony numbers in Hs578T cells in a dose-dependent manner, with the strongest inhibition at 6.7 μM (equivalent to 0.5x IC50).

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231, Hs578T (triple-negative breast cancer cells)
Concentration: 1.5x IC50
Incubation Time: 24 h
Result: Caused a modest increase in the proportion of MDA-MB-231 cells in the G2/M phase and a marked decrease in the G0/G1 phase population.
Did not induce significant cell cycle arrest in Hs578T cells.

Western Blot Analysis[1]

Cell Line: MDA-MB-231, Hs578T (triple-negative breast cancer cells)
Concentration: 1.5x IC50
Incubation Time: 24 h
Result: Reduced total FOXM1 levels by over 2.6-fold, reduced p-FOXM1 levels by approximately 2.7-fold, and reduced cyclin B1 expression in MDA-MB-231 cells; no significant reduction of cdc25B levels was observed relative to other compounds.
Increased FOXM1, p-FOXM1, cyclin B1, and cdc25B protein levels by >1.5-fold in Hs578T cells.

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231 (triple-negative breast cancer cells, serotonin-pretreated)
Concentration: 0.5x IC50-2x IC50 (compound); 10-20 μM (serotonin pretreatment)
Incubation Time: 24 h (compound treatment); 48 h (serotonin pretreatment)
Result: Inhibited cell proliferation in a concentration-dependent manner, with enhanced antiproliferative efficacy following pretreatment with 10 μM or 20 μM serotonin; the maximum effect was observed with 20 μM serotonin pretreatment.
Molecular Weight

493.05

Formula

C26H33ClN8
SMILES

NC1=NC(NCCN2CCN(C3=CC=CC=C3)CC2)=CC(NCCC4=CNC5=C4C=CC=C5)=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
References
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FOXM1-IN-4 hydrochloride 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:

FOXM1-IN-45-HT ReceptorDNA/RNA SynthesisSerotonin Receptor5-hydroxytryptamine Receptor5-HT7 receptornormal human dermal fibroblastscyclin B1cdc25BFOXM1HEK293 cells5-HT2A5-HT1A5-HT6 receptorstriple-negative breast cancer cell linesInhibitorinhibitorinhibit

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