Apoptosis/necroptosis inducer 1
Apoptosis/necroptosis inducer 1 is an orally active and brain-penetrant apoptosis and necroptosis inducer. Apoptosis/necroptosis inducer 1 induces mitochondria-dependent (intrinsic pathway) apoptosis. Apoptosis/necroptosis inducer 1 induces necroptosis by activating the TNF-α/NF-κB/MAPK signaling pathway. Apoptosis/necroptosis inducer 1 exhibits antiproliferative activity in glioblastoma cell lines and multiple solid tumor types. Apoptosis/necroptosis inducer 1 inhibits growth of orthotopic glioblastoma in animal models and improves survival rate. Apoptosis/necroptosis inducer 1 can be used for the research of glioblastoma.
For research use only. We do not sell to patients.
- Formula: C33H51NO5
- Molecular Weight:541.76
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Apoptosis/necroptosis inducer 1 (compound 1F) (24-72 h) exhibits concentration- and time-dependent antiproliferative activity against U87 glioblastoma cells with IC50 values of 6.87 μM (24 h), 3.85 μM (48 h), and 3.68 μM (72 h)[1].
Apoptosis/necroptosis inducer 1 (24-72 h) exhibits consistent antiproliferative activity against U251 glioblastoma cells with IC50 values ranging from 5.28 to 5.90 μM over 24, 48, and 72 hours[1].
Apoptosis/necroptosis inducer 1 (2-8 μM; 48 h) dose-dependently inhibits DNA synthesis in U87 glioblastoma cells[1].
Apoptosis/necroptosis inducer 1 (3-9 μM; 48 h) dose-dependently inhibits DNA synthesis in U251 glioblastoma cells[1].
Apoptosis/necroptosis inducer 1 (2-8 μM; 12 h) dose-dependently inhibits migration of U87 and U251 glioblastoma cells[1].
Apoptosis/necroptosis inducer 1 (2-8 μM; 19 h) dose-dependently inhibits invasion of U87 and U251 glioblastoma cells[1].
Apoptosis/necroptosis inducer 1 (2-8 μM; 48 h) reduces mitochondrial membrane potential in U87 glioblastoma cells[1].
Apoptosis/necroptosis inducer 1 (3-9 μM; 48 h) reduces mitochondrial membrane potential in U251 glioblastoma cells[1].
Apoptosis/necroptosis inducer 1 (2-8 μM; 48 h) increases reactive oxygen species levels in U87 glioblastoma cells[1].
Apoptosis/necroptosis inducer 1 (3-9 μM; 48 h) increases reactive oxygen species levels in U251 glioblastoma cells[1].
Apoptosis/necroptosis inducer 1 (2-8 μM; 48 h) induces G2/M phase cell cycle arrest in U87 glioblastoma cells[1].
Apoptosis/necroptosis inducer 1 (3-9 μM; 48 h) induces G1/G0 phase cell cycle arrest in U251 glioblastoma cells[1].
Apoptosis/necroptosis inducer 1 (2-8 μM; 48 h) induces apoptosis in U87 glioblastoma cells[1].
Apoptosis/necroptosis inducer 1 (3-9 μM; 48 h) induces apoptosis in U251 glioblastoma cells[1].
Apoptosis/necroptosis inducer 1 (2-8 μM; 48 h) modulates apoptosis-related proteins (decreases Caspase 9, Caspase 3, Bcl-2; increases BAX, Cleaved Caspase 8) in U87 glioblastoma cells[1].
Apoptosis/necroptosis inducer 1 (2-9 μM; 48 h) triggers necroptosis in U87 and U251 glioblastoma cells via coordinated regulation of TNF-α/NF-κB/MAPK signaling pathway[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U87 and U251 glioblastoma cells
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Concentration:2, 4, 8 μM
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Incubation Time:12 h
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Result:Dose-dependently reduced the number of migrating cells compared to control.
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Cell Line:U87 glioblastoma cells
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Concentration:2, 4, 8 μM
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Incubation Time:19 h
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Result:Dose-dependently reduced the number of invading cells compared to control.
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Cell Line:U251 glioblastoma cells
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Concentration:3, 6, 9 μM
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Incubation Time:19 h
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Result:Dose-dependently reduced the number of invading cells compared to control.
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Cell Line:U87 glioblastoma cells
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Concentration:2, 4, 8 μM
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Incubation Time:48 h
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Result:Increased the proportion of cells in G2/M phase from 10.9% to 19.6% and decreased G1/G0 population from 61.9% to 51.6% following high-concentration treatment.
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Cell Line:U251 glioblastoma cells
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Concentration:3, 6, 9 μM
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Incubation Time:48 h
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Result:Induced G1/G0 phase arrest following high-concentration treatment.
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Cell Line:U87 glioblastoma cells
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Concentration:2, 4, 8 μM
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Incubation Time:48 h
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Result:Elevated early and late apoptosis percentages compared to control.
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Cell Line:U251 glioblastoma cells
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Concentration:3, 6, 9 μM
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Incubation Time:48 h
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Result:Elevated early and late apoptosis percentages compared to control.
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Cell Line:U87 glioblastoma cells
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Concentration:2, 4, 8 μM
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Incubation Time:48 h
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Result:Decreased Caspase 9, Caspase 3, and Bcl-2 protein levels; increased BAX and Cleaved Caspase 8 expression.
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Cell Line:U87 and U251 glioblastoma cells
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Concentration:2, 4, 8 μM (U87), 3, 6, 9 μM (U251)
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Incubation Time:48 h
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Result:Revealed significant upregulation of phosphorylation at RIP1 Ser166, RIP3 Ser227, and MLKL Ser358 in U87 and U251 cells.
Apoptosis/necroptosis inducer 1 (compound 1F) (100 mg/kg; i.g.; single dose) exhibits favorable blood-brain barrier permeability in healthy BALB/c mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (male, specific pathogen-free grade, orthotopic GL261-Luc glioblastoma model)[1]
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Dosage:50, 100, 200 mg/kg
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Administration:p.o.; daily; 21 days
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Result:Significantly reduced relative tumor fluorescence intensity at day 21; Extended survival rate at 100 mg/kg.
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Animal Model:BALB/c (male, specific pathogen-free grade)[1]
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Dosage:100 mg/kg
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Administration:i.g.; single dose
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Result:Reached an average brain concentration of 261.30 ng/g
Chemical Information
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Molecular Weight 541.76
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Formula C33H51NO5
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SMILES
CCCCCCCCCCCCCC(OC(C(OC)=CC=C1C[C@H]2C3C[C@H]4OC)=C1[C@]3(CCN2C)CC4=O)=O
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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)
Apoptosis/necroptosis inducer 1 Related Classifications
Cat. No.: HY-181073
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- Apoptosis/necroptosis inducer 1
- Apoptosis
- Necroptosis
- NF-κB
- p38 MAPK
- TNF-α/NF-κB/MAPK signaling pathway
- mitochondria-dependent apoptosis
- glioblastoma cell lines
- necroptosis
- cell cycle arrest
- apoptosis
- U87 glioblastoma cells
- reactive oxygen species
- U251 glioblastoma cells
- orthotopic glioblastoma
- Inhibitor
- inhibitor
- inhibit