c-MYC/BCL2 ligand 1 iodide
c-MYC/BCL2 ligand 1 iodide is a dual-targeting c-MYC/Bcl-2 G4 ligand with Kd values of 0.90 μM (c-MYC G4) and 0.56 μM (Bcl-2 G4). c-MYC/BCL2 ligand 1 iodide inhibits c-MYC and Bcl-2 gene transcription by binding to G4-forming sequences and downregulates their protein expression. c-MYC/BCL2 ligand 1 iodide inhibits suppresses migration, induces caspase-dependent apoptosis, and triggers cell cycle G1 arrest in MCF-7 cells. c-MYC/BCL2 ligand 1 iodide significantly suppresses tumor growth in a 4T1 syngeneic model with no observable toxicity. c-MYC/BCL2 ligand 1 iodide can be used for the research of breast cancer.
For research use only. We do not sell to patients.
- Formula: C36H45IN2O3S
- Molecular Weight:712.72
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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]
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Biological Activity
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Chemical Information
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Biological Activity
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Bcl-2 0.56 μM (Kd) |
Caspase 9 |
c-MYC/BCL2 ligand 1 iodide (Compound Z4) displays high potency with IC50 values of 4.14 μM (4T1 cells) and 5.47 μM (MCF-7 cells)[1].
c-MYC/BCL2 ligand 1 iodide (2.5-10 μM, 48 h) significantly downregulates the expression levels of c-MYC and Bcl-2, and induces cell death through the mitochondrial-dependent apoptotic pathway in MCF-7 cells[1].
c-MYC/BCL2 ligand 1 iodide (2.5-10 μM, 24-48 h) dependently impeds migration and inhibits proliferation by arresting the cell cycle at the G1 phase in MCF-7 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7 cells
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Concentration:2.5, 5, 10 μM
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Incubation Time:48 h
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Result:Significantly downregulated c-MYC and Bcl-2 protein expression in a concentration-dependent manner.
Dose dependently elevated the expression of cleaved caspase-9.
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Cell Line:MCF-7 cells
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Concentration:2.5, 5, 10 μM
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Incubation Time:24-48 h
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Result:Concentration dependently suppressed cell migration toward the scratch center, indicating its potent anti-migratory activity.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:4T1 breast cancer syngeneic mice (female BALB/c, 4-5 weeks) models[1]Dosage:12 mg/kgAdministration:Intraperitoneal injections, every other day for 21 days.Result:Reduced tumor volume by 49.97 % compared to the PBS group.
Markedly reduced terminal tumor weights with a tumor growth inhibition (TGI) rate of 47.81%.
Exhibited marked cellular shrinkage and nuclear fragmentation (H&E staining), suggesting the possible presence of apoptosis.
Remained body weight stable and showed no remarkable histopathological abnormalities of major organs (heart, liver, spleen, lungs, and kidneys) via H&E staining.
Chemical Information
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Molecular Weight 712.72
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Formula C36H45IN2O3S
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SMILES
CC[N+]1=C(/C=C/C2=CC=C(OCCNS(C3=C(C(C)C)C=C(C(C)C)C=C3C(C)C)(=O)=O)C=C2)C=CC4=CC=CC=C41.[I-]
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Shipping
Room temperature in continental US; may vary elsewhere.
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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)
c-MYC/BCL2 ligand 1 iodide Related Classifications
HY-174403 Related Classifications
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