PY-Alo
PY-Alo is a DNA intercalator with a Ka of 3.46 × 105 M−1. PY-Alo induces DNA damage through backbone intercalation and non-covalent hydrogen bonding, downregulates the transcription of key genes in mitochondrial oxidative phosphorylation, and disrupts mitochondrial homeostasis, thereby synergistically inducing apoptosis (apoptosis) and autophagy (autophagy) in cells. PY-Alo exhibits cytotoxicity against both wild-type and Cisplatin (HY-17394)-resistant ovarian cancer cells. PY-Alo can be used for research on ovarian cancer.
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- Formule: C33H43ClN4
- Masse moléculaire:531.17
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Stockage:
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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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
Caspase-9 |
Caspase 3 |
Bax |
Bcl-2 |
MMP |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| SK-OV-3 | IC50 |
2.57 μM
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Cytotoxicity against human ovarian cancer SKOV3 cells assessed as viability reduction by cell viability assay.
Cytotoxicity against human ovarian cancer SKOV3 cells assessed as viability reduction by cell viability assay.
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acs.jmedchem.6c00799 |
| A2780 | IC50 |
2.34 μM
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Cytotoxicity against human ovarian cancer A2780 cells assessed as viability reduction by cell viability assay.
Cytotoxicity against human ovarian cancer A2780 cells assessed as viability reduction by cell viability assay.
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acs.jmedchem.6c00799 |
In Vitro
PY-Alo (3.0-5.0 μM; 30 min-24 h) accumulates in the nuclear DNA of A2780/DDP cells and induces γ-H2AX DNA damage[1].
PY-Alo (1.0 μM; 24 h) exhibits activity in A2780/DDP cells by synergizing with Cisplatin (HY-17394) and reducing the viability of DDP-resistant cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:IOSE-80, SKOV3, A2780, A2780/DDP
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Concentration:0.25, 0.5, 1, 2, 4, 8 μM
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Incubation Time:24 h
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Result:Inhibited cell viability in all four cell lines and exhibited significant cytotoxicity against cisplatin-resistant A2780/DDP cells with an IC50 of 2.89 μM.
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Cell Line:A2780, A2780/DDP
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Concentration:3.0 μM
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Incubation Time:24 h
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Result:Induced significant DNA damage, evidenced by strong green fluorescence of γ-H2AX in both A2780 and A2780/DDP cells.
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Cell Line:A2780, A2780/DDP
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Concentration:3.0 μM
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Incubation Time:24 h
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Result:Elevated the Bax/Bcl-2 ratio and p53 levels, induced Cleaved Caspase-9/3 expression, and increased LC3B II and p62 levels, triggering a synergistic apoptosis-autophagy pathway.
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Cell Line:A2780, A2780/DDP
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Concentration:3.0 μM
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Incubation Time:24 h
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Result:Inhibited cell migration in both A2780 and A2780/DDP cells.
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Cell Line:A2780, A2780/DDP
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Concentration:3.0 μM
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Incubation Time:24 h
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Result:Inhibited cell invasion in both A2780 and A2780/DDP cells.
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Cell Line:A2780/DDP
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Concentration:3.0 μM
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Incubation Time:24 h
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Result:Significantly downregulated the mRNA expression of multiple subunits of the NADH dehydrogenase (MT-ND), cytochrome c (MT-CYB), cytochrome c oxidase (MT-CO), and ATP synthase (MT-ATP).
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (female) were injected with 5×106 A2780 or A2780/DDP cells into the unilateral axilla[1]
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Dosage:10 mg/kg
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Administration:i.v.; once daily; 15 days
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Result:Effectively inhibited tumor growth (decreased tumor volume and tumor weight) in both A2780 and cisplatin-resistant A2780/DDP xenograft models.
Demonstrated acceptable biosafety, showing minimal influence on mouse body weight and minimal damage to major organs (heart, liver, spleen, lungs, and kidneys).
Induced DNA damage (γ-H2AX), apoptosis (Ki67 reduction), and autophagy (LC3B II and p62 increase) in the tumor tissues in vivo.
- Western Blot
- Mammalian live/dead viability and cytotoxicity staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- Cell Viability Determination by MTT Colorimetric Assay
- Kinase activity and phosphorylation assays
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Cell Cytotoxicity Assay
- Autophagy
- Apoptosis Solutions
- Protocol for Kinase activity and phosphorylation assays
- Lysosome and acidic-vesicle live-cell staining
- Macroautophagy Solutions
- Genotoxicity/Mutagenicity Study
Chemical Information
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Masse moléculaire 531.17
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Formule C33H43ClN4
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SMILES
CN(C1=CC(CC2=C/C3=[N+](C)\C)=C(C(N4[C@]5([C@H]6CN7CCCC[C@@]7([C@H](C6)C=C5CCC4)[H])[H])=C2C=C3)C=C1)C.[Cl-]
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PY-Alo Related Classifications
HY-189656 Related Classifications
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