5-HT7 modulator-1
5-HT7 modulator-1 is a selective 5-HT7 receptor antagonist with a Ki of 92 nM. 5-HT7 modulator-1 blocks 5-HT7 receptor signaling to reduce FOXM1, phosphorylated FOXM1, cyclin B1, and cdc25B levels. 5-HT7 modulator-1 acts as an antiproliferative, clonogenic inhibitor, and cell cycle inhibitor that induces G2/M arrest, reduces G0/G1 population. 5-HT7 modulator-1 can be used for the research of triple-negative breast cancer.
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- CAS. Nr.: 3122097-27-9
- Formel: C26H32N8
- Molecular Weight:456.59
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
5-HT7 Receptor 92 nM (Ki) |
5-HT7 Receptor 11 nM (Kb) |
In Vitro
5-HT7 modulator-1 (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].
5-HT7 modulator-1 (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].
5-HT7 modulator-1 (0.7-5.7 μM (MDA-MB-231); 0.8-6.7 μM (Hs578T); 7 days) dose-dependently suppresses long-term clonogenic growth of MDA-MB-231 and Hs578T TNBC cells[1].
5-HT7 modulator-1 (1.5 × IC50; 24 h) induces G2/M phase cell cycle arrest in MDA-MB-231 TNBC cells[1].
5-HT7 modulator-1 (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].
5-HT7 modulator-1 (0.5 × IC50-2 × IC50; 24 h) exhibits enhanced antiproliferative activity in MDA-MB-231 TNBC cells pretreated with Serotonin (HY-B1473A)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:MDA-MB-231, Hs578T (TNBC cell lines)
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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
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Incubation Time:7 days
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Result:Significantly and dose-dependently reduced colony formation in both cell lines.
In MDA-MB-231 cells, 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.
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Cell Line:MDA-MB-231, Hs578T (TNBC cell lines)
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Concentration:16.95 μM
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Incubation Time:24 h
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Result: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 in MDA-MB-231 cells.
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Cell Line:MDA-MB-231, Hs578T (TNBC cell lines)
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Concentration:16.95 μM
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Incubation Time:24 h
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Result:Reduced total FOXM1 expression by over 2.6-fold and reduced p-FOXM1 levels by approximately 2.7-fold in Hs578T cells.
Caused a reduction in cyclin B1 and cdc25B protein levels in MDA-MB-231 cells.
Chemical Information
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CAS. Nr. 3122097-27-9
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Molecular Weight 456.59
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Formel C26H32N8
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SMILES
NC1=NC(NCCN2CCN(C3=CC=CC=C3)CC2)=CC(NCCC4=CNC5=C4C=CC=C5)=N1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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Flow cytometric DNA-content cell-cycle staining
Flow cytometric DNA-content cell-cycle staining measures the fluorescence intensity of DNA-bound fluorochromes in single cells or nuclei to estimate DNA content distributions, allowing assignment of populations to G0/G1, S, and G2/M phases by DNA histogram deconvolution. Propidium iodide (PI) intercalates into DNA, and PI fluorescence is proportional to cellular DNA content when staining is performed under conditions that make DNA accessible and minimize non-DNA signal. Cells with G2/M DNA content are expected to show approximately twice the fluorescence intensity of G0/G1 cells, while S-phase cells occupy intermediate fluorescence values. PI-based DNA-content analysis can also detect cells with fractional DNA content, often reported as sub-G1, when DNA fragmentation and extraction during staining reduce retained DNA signal in apoptotic cells. DAPI is an alternative DNA fluorochrome for univariate DNA-content analysis, while bivariate approaches combining DNA content with proliferation
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BrdU Incorporation Assay
Bromodeoxyuridine (BrdU) incorporation assay is based on the principle that BrdU, a thymidine analog, is incorporated into newly synthesized DNA during the S phase of the cell cycle, thereby serving as a marker of DNA replication and cellular proliferation. Incorporated BrdU can be detected using anti-BrdU antibodies following DNA denaturation, enabling visualization or quantification of proliferating cells through immunochemical detection methods such as immunofluorescence or immunohistochemistry.
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Protocol for Cell Cycle
Cell-cycle analysis by flow cytometry measures DNA content in single cells to estimate the fraction of cells in G0/G1, S, and G2/M phases. Propidium iodide intercalates into DNA, and after RNA removal with RNase, fluorescence intensity reflects cellular DNA content: 2N cells are assigned to G0/G1, cells between 2N and 4N to S phase, and 4N cells to G2/M. DNA-content analysis alone cannot reliably separate G0 from G1 or G2 from M. Ki-67 can distinguish quiescent G0 cells from cycling cells, EdU or BrdU incorporation marks active DNA synthesis in S phase, and phospho-histone H3 staining identifies mitotic cells within the 4N population.
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)