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 No.: 3122097-27-9
- 화학식: C26H32N8
- 분자량:456.59
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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5-HT7 Receptor 92 nM (Ki) |
5-HT7 Receptor 11 nM (Kb) |
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.
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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 No. 3122097-27-9
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분자량 456.59
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
5-HT7 modulator-1 Related Classifications
HY-182285 Related Classifications
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