2. Apoptosis Immunology/Inflammation Metabolic Enzyme/Protease
  3. Caspase COX Cytochrome P450 Steroid Sulfatase Apoptosis
  4. Caspase-3/7 activator 4

Caspase-3/7 activator 4 is a caspase-3 activator and caspase-7 activator. Caspase-3/7 activator 4 inhibits key enzymes in estrogen biosynthesis, including aromatase (IC50 = 38.3 nM) and steroid sulfatase (IC50 = 12.7 µM), and selectively suppresses COX-2 (IC50 = 5.38 µM). Caspase-3/7 activator 4 shows strong antioxidant activity (DPPH: IC50 = 16.26 µM). Caspase-3/7 activator 4 inhibits estrogen synthesis, suppresses estrogen availability, reduces prostaglandin production, increases caspase-3/7 expression, induces G0/G1 cell cycle arrest, induces apoptotic cell death, reduces circulating TNF-α and VEGFR-II levels, restores hepatorenal function markers and histoarchitecture, restores antioxidant defense enzyme activity, reduces lipid peroxidation, exerts antiproliferative activity against breast cancer cells, exerts antitumor activity in the Ehrlich ascites carcinoma models. Caspase-3/7 activator 4 can be used for the research of breast cancer, ehrlich ascites carcinoma.

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Caspase-3/7 activator 4

Caspase-3/7 activator 4 Chemical Structure

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Caspase-3/7 activator 4 Related Antibodies

Top Publications Citing Use of Products

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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COX COX-1 COX-2 COX-3

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CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A CYP3A4 CYP17A1

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Description

Caspase-3/7 activator 4 is a caspase-3 activator and caspase-7 activator. Caspase-3/7 activator 4 inhibits key enzymes in estrogen biosynthesis, including aromatase (IC50 = 38.3 nM) and steroid sulfatase (IC50 = 12.7 µM), and selectively suppresses COX-2 (IC50 = 5.38 µM). Caspase-3/7 activator 4 shows strong antioxidant activity (DPPH: IC50 = 16.26 µM). Caspase-3/7 activator 4 inhibits estrogen synthesis, suppresses estrogen availability, reduces prostaglandin production, increases caspase-3/7 expression, induces G0/G1 cell cycle arrest, induces apoptotic cell death, reduces circulating TNF-α and VEGFR-II levels, restores hepatorenal function markers and histoarchitecture, restores antioxidant defense enzyme activity, reduces lipid peroxidation, exerts antiproliferative activity against breast cancer cells, exerts antitumor activity in the Ehrlich ascites carcinoma models. Caspase-3/7 activator 4 can be used for the research of breast cancer, ehrlich ascites carcinoma[1].

IC50 & Target[1]

COX-2

5.38 μM (IC50)

Caspase 3

 

Caspase-7

 

Aromatase

38.3 μM (IC50)

Steroid Sulfatase

12.7 μM (IC50)

In Vitro

Caspase-3/7 activator 4 (compound 6) (0.5-80 μM; hibits the proliferation of MDA-MB-231 and MCF-7 breast cancer cells with IC50 values of 2.25 μM and 6.70 μM, respectively, and shows high selectivity for cancer cells over non-tumorigenic MCF-10A cells[1].
Caspase-3/7 activator 4 (2.25 μM; 24 h) induces G0/G1 cell cycle arrest in MDA-MB-231 cells[1].
Caspase-3/7 activator 4 (2.25 μM; 24 h) induces substantial apoptotic cell death in MDA-MB-231 cells, with early apoptosis as the predominant mode[1].
Caspase-3/7 activator 4 (2.25 μM; 24 h) activates caspase-3 and caspase-7 in MDA-MB-231 cells, indicating induction of apoptotic pathways[1].

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

Caspase-3/7 activator 4 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231, MCF-7, MCF-10A
Concentration: 0.5 μM, 1 μM, 2.5 μM, 5 μM, 10 μM, 20 μM, 40 μM, 80 μM
Incubation Time: 48 h
Result: Exhibited potent antiproliferative activity with IC50 values of 2.25 μM against MDA-MB-231 cells, 6.70 μM against MCF-7 cells, and 36.57 μM against non-tumorigenic MCF-10A cells.

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231
Concentration: 2.25 μM
Incubation Time: 24 h
Result: Induced a substantial accumulation in the G0/G1 phase (84.62%) with a concomitant decrease in the S phase (12.83%) and G2/M phase (2.55%) compared to untreated control cells.

Apoptosis Analysis[1]

Cell Line: MDA-MB-231
Concentration: 2.25 μM
Incubation Time: 24 h
Result: Resulted in a markedly higher total apoptosis/necrosis rate (24.81%) compared to untreated control cells (2.46%), with 16.26% early apoptosis, 5.61% late apoptosis, and 2.94% necrosis.

ELISA Assay[1]

Cell Line: MDA-MB-231
Concentration: 2.25 μM
Incubation Time: 24 h
Result: Significantly increased caspase-3 levels to 428.56 pg/mL (3.69-fold increase) and caspase-7 levels to 2.916 ng/mL (4.83-fold increase) compared to untreated controls.
In Vivo

Caspase-3/7 activator 4 (compound 6) (2.5-20 mg/kg; i.p.; every other day; 10 days) exerts dose-dependent antitumor activity in Ehrlich ascites carcinoma (EAC)-bearing mice, reducing viable tumor cell count by up to 81.9% and ascitic volume by 74.3% at 15 mg/kg, while improving hepatorenal function and oxidative stress markers[1].
Caspase-3/7 activator 4 (1-200 mg/kg; i.p.; once) is administered to mice and closely monitored for 48 hours for death, behavioral changes, and obvious toxic symptoms. At doses up to 120 mg/kg , no mortality or abnormal behavioral manifestations were observed, and the animals maintained normal grooming, feeding, and locomotor activity, indicating a good safety margin at these concentra-
tions. In contrast, administration of 200 mg/kg resulted in complete mortality, establishing this dose as the approximate lethal dose (LD100)[1].

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

Animal Model: Swiss albino female (20-25 g, Ehrlich ascites carcinoma model)[1]
Dosage: 2.5, 5, 10, 15, and 20 mg/kg
Administration: i.p.; every other day; 10 days
Result: Reduced viable EAC cell count to 125.94 × 106 (39.7% decrease vs. control) at 2.5 mg/kg.
Reduced viable EAC cell count to 78.76 × 106 (62.3% decrease vs. control) at 5 mg/kg.
Reduced viable EAC cell count to 58.64 × 106 (71.9% decrease vs. control) at 10 mg/kg.
Reduced viable EAC cell count to 42.17 × 106 (79.8% decrease vs. control) and ascitic tumor volume to 1.45 mL (74.3% decrease vs. control) at 15 mg/kg; reduced viable EAC cell count to 37.67 × 10⁶ (81.9% decrease vs. control) at 20 mg/kg; reduced serum TNF-α levels to 82.27 pg/mL (vs. EAC control 162.63 pg/mL); reduced serum VEGFR-II levels to 46.59 ng/mL; restored liver antioxidant markers (GSH: 31.20 pg/g tissue, CAT: 35.90 U/g tissue, SOD: 31.86 U/g tissue) and reduced MDA to 27.65 nmol/g tissue; improved liver function (ALT: 67.50 U/L, AST: 84.5 U/L) and renal function (creatinine: 0.98 mg/dL, urea: 60.50 mg/dL) vs. EAC control.
Molecular Weight

355.80

Formula

C14H14ClN3O4S
SMILES

O=C(OC)CCN1/C(SCC1=O)=N\N=C\C2=CC(Cl)=CC=C2O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Caspase-3/7 activator 4 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:

Caspase-3/7 activator 4CaspaseCOXCytochrome P450Steroid SulfataseApoptosisCyclooxygenaseCYPsehrlich ascites carcinomacyclooxygenase-2 (COX-2)CYP19A1breast cancerMDA-MB-231caspase-7caspase-3MCF-7steroid sulfatase (STS)MCF-10AInhibitorinhibitorinhibit

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