Apoptosis inducer 65
Apoptosis inducer 65 is an apoptosis inducer with antiproliferative activity against cancer cells. Apoptosis inducer 65 induces G0/G1 cell cycle arrest and intrinsic apoptosis by upregulating p53, BAX, and caspase-7, while downregulating Bcl-2. Apoptosis inducer 65 inhibits ROS, NO, TNF-α, IL-1β, and IL-6 in macrophages. Apoptosis inducer 65 can be used for research on hepatocellular carcinoma and inflammation.
For research use only. We do not sell to patients.
- Formula: C26H18Br3N3O4
- Molecular Weight:676.15
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Caspase Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
IL-6 |
IL-1β |
Bax |
Caspase-7 |
Bcl-2 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | IC50 |
7.81 μM
|
Cytotoxicity against human HepG-2 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay.
Cytotoxicity against human HepG-2 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay.
|
42630597 |
| HCT-116 | IC50 |
15.34 μM
|
Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay.
Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay.
|
42630597 |
| MCF7 | IC50 |
44.66 μM
|
Cytotoxicity against human MCF-7 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay.
Cytotoxicity against human MCF-7 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay.
|
42630597 |
| PANC-1 | IC50 |
63.24 μM
|
Cytotoxicity against human Panc-1 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay.
Cytotoxicity against human Panc-1 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay.
|
42630597 |
| WI-38 | IC50 |
67.2 μM
|
Cytotoxicity against normal human WI-38 fibroblasts assessed as reduction in cell viability incubated for 24 hrs by MTT assay.
Cytotoxicity against normal human WI-38 fibroblasts assessed as reduction in cell viability incubated for 24 hrs by MTT assay.
|
42630597 |
In Vitro
Apoptosis inducer 65 (7.81 μM; 24 h) triggers apoptosis in HepG2 cells through activation of a p53-dependent pathway, upregulating p53 (5.89-fold) and BAX (3.71-fold) while downregulating Bcl-2 (0.64-fold)[1].
Apoptosis inducer 65 (10 μM; 24 h) inhibits the expression of pro-inflammatory cytokines in LPS-stimulated RAW 264.7 macrophages, reducing TNF-α to 0.36-fold, IL-1β to 0.47-fold, and IL-6 to 0.51-fold[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2
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Concentration:7.81 μM
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Incubation Time:24 h
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Result:Increased the total apoptotic population (early + late) from 3.12% to 35.14%.
Increased late apoptosis from 0.18% to 23.27%.
Increased early apoptosis from 0.65% to 3.69%.
Increased necrotic cell death from 2.29% to 8.18%.
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Cell Line:HepG2
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Concentration:7.81 μM
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Incubation Time:24 h
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Result:Upregulated p53 expression to 5.89-fold relative to control.
Upregulated BAX expression to 3.71-fold.
Downregulated Bcl-2 expression to 0.64-fold.
Increased the BAX/Bcl-2 ratio by 5.8-fold.
Elevated cytochrome c (CYC) expression to 3.94-fold.
Upregulated caspase-7 expression to 2.65-fold.
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Cell Line:RAW 264.7
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Concentration:12.5, 25, 50, 100, 150, 200 μM
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Incubation Time:2 h pretreatment; 24 h incubation
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Result:In the absence of LPS, maintained viability of 98.3%, 96.7%, and 98.6% at 12.5, 25, and 50 μM, respectively, and 83.6%, 75.4%, and 48.1% at 100, 150, and 200 μM, respectively.
Under LPS-stimulated conditions, maintained viability of 97.1%, 93.8%, and 96.4% at 12.5, 25, and 50 μM, respectively, and 76.3%, 60.7%, and 37.2% at 100, 150, and 200 μM, respectively.
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Cell Line:RAW 264.7
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Concentration:10 μM
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Incubation Time:24 h
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Result:Reduced TNF-α expression to 0.36-fold relative to LPS-stimulated control cells.
Decreased IL-1β expression to 0.47-fold.
Reduced IL-6 levels to 0.51-fold.
- 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
- Apoptosis Solutions
- Protocol for Cell Cycle
- Liver Cancer Modeling
- Research Protocol for Inflammation-related Diseases
- Cell Viability Determination by MTT Colorimetric Assay
- Pyroptosis Solutions
Chemical Information
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Molecular Weight 676.15
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Formula C26H18Br3N3O4
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SMILES
BrC1=C(O)C(Br)=CC(/C(N2C3=CC=CC=C3NC(C4=CC(Br)=CC=C4O)=C2)=C(C(OCC)=O)\C#N)=C1
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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)
Keywords
- Apoptosis inducer 65
- Apoptosis inducer65
- Apoptosis inducer-65
- Apoptosis
- MDM-2/p53
- Caspase
- Bcl-2 Family
- TNF Receptor
- Reactive Oxygen Species (ROS)
- Interleukin Related
- intrinsic apoptosis
- hepatocellular carcinoma
- inflammatory pathways
- IL-1β
- IL-6Rα binder
- TNF-α
- G0/G1 phase cell cycle arrest
- RAW 264.7 macrophages
- HepG-2 cells
- antiproliferative activity
- Inhibitor
- inhibitor
- inhibit