Bcl-2-IN-26
Bcl-2-IN-26 is an inhibitor targeting β-tubulin and BCL-2. Bcl-2-IN-26 disrupts the intracellular microtubule network and interferes with cell mitosis, inducing G2/M phase cell cycle arrest. Bcl-2-IN-26 suppresses antiapoptotic BCL-2 function via p53 upregulation, thereby triggering mitochondrial dysfunction, elevated ROS production and robust tumor cell apoptosis. Bcl-2-IN-26 can be used in lung cancer research.
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- CAS. Nr.: 3119834-80-6
- Formel: C20H16F2N2O4
- Molecular Weight:386.35
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
Bcl-2 |
β-Tubulin |
In Vitro
Bcl-2-IN-26 (Compound 45) (72 h) exhibits potent inhibitory activity against NCI-H460 and A549 lung cancer cells with IC50s of 0.66 nM and 0.73 nM, respectively[1].
Bcl-2-IN-26 (1-5 nM; 24 h) blocks tubulin polymerization, disrupts microtubule networks and impairs mitosis in H460 cells[1].
Bcl-2-IN-26 (2-200 nM; 24 h) induces G2/M phase arrest and apoptosis in H460 cells in a dose-dependent manner[1].
Bcl-2-IN-26 (1-5 nM; 24 h) affects the expression of various apoptotic proteins, thereby inducing apoptosis in H460 cells[1].
Bcl-2-IN-26 (1-5 nM; 24 h) reduces mitochondrial transmembrane potential, induces dose-dependent ROS accumulation in H460 cells[1].
Bcl-2-IN-26 (1 nM; 48 h) triggers H460 cell death mainly by activating the p53 pathway to modulate BAX/BCL-2, with caspase activation only exerting weak auxiliary cytotoxic effects[1].
Bcl-2-IN-26 displays optimal antitumor activity owing to synergistic fluorine and alkene-mediated binding interactions with microtubules[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NCI-H460 cells
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Concentration:2 nM, 5 nM, 100 nM, 200 nM
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Incubation Time:24 h
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Result:Induced G2/M-phase arrest and apoptosis in H460 cells.
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Cell Line:NCI-H460 cells
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Concentration:1 nM, 2 nM, 5 nM
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Incubation Time:24 h
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Result:Induced irregular morphology in H460 cells.
Disrupted filamentous microtubule structures, loosened microtubules and blocked mitosis.
Showed the strongest green fluorescence, indicating a decrease in MMP.
Promoted intracellular ROS accumulation in H460 cells in a dose-dependent manner.
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Cell Line:NCI-H460 cells
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Concentration:1 nM, 2 nM, 5 nM
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Incubation Time:24 h
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Result:Significantly upregulated the level of p53 protein expression in a dose-dependent manner.
Increased the level of pro-apoptotic BAX.
Blocked the anti-apoptotic function of BCL-2.
Activated caspase-3 and caspase-8 and triggers apoptosis in NCI-H460 cells.
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Cell Line:NCI-H460 cells
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Concentration:1 nM
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Incubation Time:48 h
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Result:Triggered cell death that pan-caspase inhibitors only weakly reversed.
Induced cell death that inhibiting the p53 pathway markedly rescued.
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Cell Line:NCI-H460 cells
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Concentration:1 nM
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Incubation Time:48 h
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Result:Downregulated BAX and BCL-2 expression when p53 was inhibited.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:5-8-week-old male C57BL/6 mice were adaptively fed for one week before subcutaneous injection of 2.5 × 106 LLC cells[1].
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Dosage:5 mg/kg, 10 mg/kg
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Administration:i.p., every 3 days, for 15 days
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Result:Significantly inhibited tumor growth in mice.
Did not cause a significant decrease in the body weight of the mice.
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- ROS/oxidative-stress fluorescent staining
- Mitochondrial membrane-potential and mitochondrial mass staining
- Apoptosis Solutions
- Protocol for Cell Cycle
Chemical Information
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CAS. Nr. 3119834-80-6
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Molecular Weight 386.35
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Formel C20H16F2N2O4
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SMILES
FC1=CC(F)=CC(/C=C2NC(/C(NC\2=O)=C/C3=CC=C(COCC=C)O3)=O)=C1
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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.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Bcl-2-IN-26 Related Classifications
HY-184443 Related Classifications
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