2. Apoptosis NF-κB MAPK/ERK Pathway
  3. Apoptosis Necroptosis NF-κB p38 MAPK
  4. 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.

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Apoptosis/necroptosis inducer 1

Apoptosis/necroptosis inducer 1 Chemical Structure

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Apoptosis/necroptosis inducer 1 Related Antibodies

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Description

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[1].

In Vitro

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.

Apoptosis/necroptosis inducer 1 Related Antibodies

Cell Migration Assay[1]

Cell Line: U87 and U251 glioblastoma cells
Concentration: 2, 4, 8 μM
Incubation Time: 12 h
Result: Dose-dependently reduced the number of migrating cells compared to control.

Cell Invasion Assay[1]

Cell Line: U87 glioblastoma cells
Concentration: 2, 4, 8 μM
Incubation Time: 19 h
Result: Dose-dependently reduced the number of invading cells compared to control.

Cell Invasion Assay[1]

Cell Line: U251 glioblastoma cells
Concentration: 3, 6, 9 μM
Incubation Time: 19 h
Result: Dose-dependently reduced the number of invading cells compared to control.

Cell Cycle Analysis[1]

Cell Line: U87 glioblastoma cells
Concentration: 2, 4, 8 μM
Incubation Time: 48 h
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.

Cell Cycle Analysis[1]

Cell Line: U251 glioblastoma cells
Concentration: 3, 6, 9 μM
Incubation Time: 48 h
Result: Induced G1/G0 phase arrest following high-concentration treatment.

Apoptosis Analysis[1]

Cell Line: U87 glioblastoma cells
Concentration: 2, 4, 8 μM
Incubation Time: 48 h
Result: Elevated early and late apoptosis percentages compared to control.

Apoptosis Analysis[1]

Cell Line: U251 glioblastoma cells
Concentration: 3, 6, 9 μM
Incubation Time: 48 h
Result: Elevated early and late apoptosis percentages compared to control.

Western Blot Analysis[1]

Cell Line: U87 glioblastoma cells
Concentration: 2, 4, 8 μM
Incubation Time: 48 h
Result: Decreased Caspase 9, Caspase 3, and Bcl-2 protein levels; increased BAX and Cleaved Caspase 8 expression.

Western Blot Analysis[1]

Cell Line: U87 and U251 glioblastoma cells
Concentration: 2, 4, 8 μM (U87), 3, 6, 9 μM (U251)
Incubation Time: 48 h
Result: Revealed significant upregulation of phosphorylation at RIP1 Ser166, RIP3 Ser227, and MLKL Ser358 in U87 and U251 cells.
In Vivo

Apoptosis/necroptosis inducer 1 (compound 1f) (50-200 mg/kg; p.o.; daily; 21 days) suppresses GL261 tumor growth and enhances survival rate in orthotopic GBM mice[1].
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.

Animal Model: BALB/c (male, specific pathogen-free grade, orthotopic GL261-Luc glioblastoma model)[1]
Dosage: 50, 100, 200 mg/kg
Administration: p.o.; daily; 21 days
Result: Significantly reduced relative tumor fluorescence intensity at day 21; Extended survival rate at 100 mg/kg.
Animal Model: BALB/c (male, specific pathogen-free grade)[1]
Dosage: 100 mg/kg
Administration: i.g.; single dose
Result: Reached an average brain concentration of 261.30 ng/g
Molecular Weight

541.76

Formula

C33H51NO5
SMILES

CCCCCCCCCCCCCC(OC(C(OC)=CC=C1C[C@H]2C3C[C@H]4OC)=C1[C@]3(CCN2C)CC4=O)=O
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Purity & Documentation
References
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Apoptosis/necroptosis inducer 1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Apoptosis/necroptosis inducer 1ApoptosisNecroptosisNF-κBp38 MAPKNuclear factor-κBNuclear factor-kappaBTNF-α/NF-κB/MAPK signaling pathwaymitochondria-dependent apoptosisglioblastoma cell linesnecroptosiscell cycle arrestapoptosisU87 glioblastoma cellsreactive oxygen speciesU251 glioblastoma cellsorthotopic glioblastomaInhibitorinhibitorinhibit

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