5-HT7 modulator-1 hydrochloride
5-HT7 modulator-1 hydrochloride is a selective 5-HT7 receptor antagonist with a Ki of 92 nM. 5-HT7 modulator-1 hydrochloride blocks 5-HT7 receptor signaling to reduce FOXM1, phosphorylated FOXM1, cyclin B1, and cdc25B levels. 5-HT7 modulator-1 hydrochloride acts as an antiproliferative, clonogenic inhibitor, and cell cycle inhibitor that induces G2/M arrest, reduces G0/G1 population. 5-HT7 modulator-1 hydrochloride can be used for the research of triple-negative breast cancer.
For research use only. We do not sell to patients.
- Formula: C26H33ClN8
- Molecular Weight:493.05
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
All 5-HT Receptor Isoforms
More
Biological Activity
5-HT7 modulator-1 hydrochloride (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 hydrochloride (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 hydrochloride (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 hydrochloride (1.5 × IC50; 24 h) induces G2/M phase cell cycle arrest in MDA-MB-231 TNBC cells[1].
5-HT7 modulator-1 hydrochloride (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 hydrochloride (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.
-
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 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.
-
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 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.
Chemical Information
-
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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
5-HT7 modulator-1 hydrochloride Related Classifications
HY-182285A Related Classifications
Powered by Bioz