1. Apoptosis Cell Cycle/DNA Damage
  2. Apoptosis DNA/RNA Synthesis Caspase Bcl-2 Family MDM-2/p53
  3. Apoptosis inducer 56

Apoptosis inducer 56 is an apoptosis inducer. Apoptosis inducer 56 induces DNA damage (upregulation of γH2AX and p-ATM expression) by minor groove binding. Apoptosis inducer 56 induces intrinsic apoptosis (upregulation of p53 and Bax/Bcl-2 ratio, cleaved caspase-7) via S-phase cell cycle arrest. Apoptosis inducer 56 shows selectivity for cancer cells over normal breast epithelial cells. Apoptosis inducer 56 can be used for the research of breast cancer.

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Apoptosis inducer 56

Apoptosis inducer 56 Chemical Structure

CAS No. : 952306-31-9

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Description

Apoptosis inducer 56 is an apoptosis inducer. Apoptosis inducer 56 induces DNA damage (upregulation of γH2AX and p-ATM expression) by minor groove binding. Apoptosis inducer 56 induces intrinsic apoptosis (upregulation of p53 and Bax/Bcl-2 ratio, cleaved caspase-7) via S-phase cell cycle arrest. Apoptosis inducer 56 shows selectivity for cancer cells over normal breast epithelial cells. Apoptosis inducer 56 can be used for the research of breast cancer[1].

IC50 & Target[1]

Caspase-7

 

Bax

 

Bcl-2

 

In Vitro

Apoptosis inducer 56 (compound 1) (5-60 μM; 24 h) selectively induces cytotoxicity in MCF-7 human breast cancer cells with an IC50 of 21.18 μM and does not exhibit notable cytotoxicity in non-malignant MCF-10A breast epithelial cells[1].
Apoptosis inducer 56 (21.18 μM; 24 h) inhibits proliferation and colony formation, and induces S-phase cell cycle arrest in MCF-7 human breast cancer cells[1].
Apoptosis inducer 56 (21.18 μM; 24 h) induces 45% apoptosis in MCF-7 human breast cancer cells and does not induce apoptosis in non-malignant MCF-10A breast epithelial cells[1].
Apoptosis inducer 56 (21.18 μM; 24 h) induces DNA damage-mediated apoptosis, and induces mitochondrial membrane depolarization in 75.8% of MCF-7 human breast cancer cells[1].
Apoptosis inducer 56 (21.18 μM) activates the DNA damage response (upregulates γ-H2AX, p-ATM, p-Chk2) and suppresses DNA repair (downregulates p-BRCA1) in MCF-7 human breast cancer cells[1].
Apoptosis inducer 56 (21.18 μM; 24 h) induces mitochondria-dependent apoptosis in MCF-7 human breast cancer cells via upregulation of pro-apoptotic proteins, cytochrome c release, caspase activation, and PARP cleavage[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay[1]

Cell Line: MCF-7 human breast cancer cells, MCF-10A non-malignant breast epithelial cells
Concentration: 5, 10, 20, 40, 60 μM
Incubation Time: 24 h
Result: Induced cytotoxicity in MCF-7 cells with an IC₅₀ of 21.18 ± 2.01 μM; maintained >70% viability in MCF-10A cells across 5, 10, 20, 40, 60 μM.

Cell Proliferation Assay[1]

Cell Line: MCF-7 human breast cancer cells
Concentration: 21.18 μM
Incubation Time: 24 h
Result: Reduced cell proliferation from 83.1% (control) to 66.3%.

Cell Cycle Analysis[1]

Cell Line: MCF-7 human breast cancer cells
Concentration: 21.18 μM
Incubation Time: 24 h
Result: Increased S-phase cell accumulation from 17.4% (control) to 30.1%.

Apoptosis Analysis[1]

Cell Line: MCF-7 human breast cancer cells, MCF-10A non-malignant breast epithelial cells
Concentration: 21.18 μM
Incubation Time: 24 h
Result: Induced 45% apoptosis in MCF-7 cells compared to 2.62% in the control group; maintained 95.8% viability in MCF-10A cells after 24 h treatment.

Apoptosis Analysis[1]

Cell Line: MCF-7 human breast cancer cells
Concentration: 21.18 μM
Incubation Time: 24 h
Result: Caused a substantial increase in TUNEL-positive cells (green fluorescence) compared to the untreated group.

Western Blot Analysis[1]

Cell Line: MCF-7 human breast cancer cells
Concentration: 21.18 μM
Incubation Time: 24 h
Result: Upregulated pro-apoptotic Bim and Bax; downregulated anti-apoptotic Bcl2 and Bcl-xL; elevated p53; suppressed survivin; induced cytochrome c release from mitochondria to cytoplasm; upregulated Apaf-1; activated caspase-7 and caspase-9 via cleavage; induced PARP cleavage.
In Vivo

Apoptosis inducer 56 (compound 1) (1-10 mg/kg; p.o.; daily; 28 days) is safe up to 10 mg/kg in BALB/c mice with no significant toxic effects on hematological, biochemical, renal, or hepatic parameters[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c mice (adult female, 25-28 g)[1]
Dosage: 1, 2.5, 5, 10 mg/kg
Administration: p.o.; daily; 28 days
Result: Detected no significant adverse effects on liver, renal, biochemical, or hematological parameters; observed no treatment-related behavioral deviations; maintained stable body weights across all dose groups; showed no structural abnormalities in liver and kidney tissues via histopathological analysis.
Molecular Weight

271.34

Formula

C11H17N3O3S

CAS No.
SMILES

O=C(CCCCCCC(NO)=O)NC1=NC=CS1

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Apoptosis inducer 56
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