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 是一种 caspase-3 激活剂与 caspase-7 激活剂。Caspase-3/7 activator 4 可抑制雌激素生物合成中的关键酶，包括芳香化酶 (aromatase) (IC50 = 38.3 nM) 和类固醇硫酸酯酶 (steroid sulfatase) (IC50 = 12.7 µM)，并可选择性抑制 COX-2 (IC50 = 5.38 µM)。Caspase-3/7 activator 4 具有较强的抗氧化活性 (DPPH: IC50 = 16.26 µM)。Caspase-3/7 activator 4 可抑制雌激素合成、降低雌激素可利用度、减少前列腺素生成、上调 caspase-3/7 表达、诱导 G0/G1 细胞周期阻滞、诱导细胞凋亡 (apoptosis)、降低循环 TNF-α 和 VEGFR-II 水平、恢复肝肾功标志物水平与组织结构、恢复抗氧化防御酶活性、减轻脂质过氧化、对乳腺癌细胞发挥抗增殖活性、在 Ehrlich 腹水癌模型中发挥抗肿瘤活性。Caspase-3/7 activator 4 可用于乳腺癌、Ehrlich 腹水癌的研究。

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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 相关抗体

Top Publications Citing Use of Products

查看 Caspase 亚型特异性产品:

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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

查看 COX 亚型特异性产品:

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COX COX-1 COX-2 COX-3

查看 Cytochrome P450 亚型特异性产品:

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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)

体外研究
(In Vitro)

Caspase-3/7 activator 4 (compound 6) (0.5-80 μM；作用 48 h) 可强效抑制 MDA-MB-231 和 MCF-7 乳腺癌细胞的增殖，其 IC50 值分别为 2.25 μM 和 6.70 μM，且相较于非致瘤性 MCF-10A 细胞，该试剂对癌细胞具有高选择性[1]。
Caspase-3/7 activator 4 (2.25 μM；作用 24 h) 可在 MDA-MB-231 细胞中诱导 G0/G1 细胞周期阻滞[1]。
Caspase-3/7 activator 4 (2.25 μM；24 h) 在 MDA-MB-231 细胞中诱导大量凋亡性细胞死亡，且以早期凋亡为主要形式[1]。
Caspase-3/7 activator 4 (2.25 μM；作用 24 h) 可激活 MDA-MB-231 细胞中的 caspase-3 和 caspase-7，表明其可诱导细胞凋亡通路[1]。

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

Caspase-3/7 activator 4 相关抗体:

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.
体内研究
(In Vivo)

Caspase-3/7 activator 4 (compound 6) (2.5-20 mg/kg；腹腔注射；每 2 天 1 次；持续 10 天) 在荷艾氏腹水癌小鼠中展现出剂量依赖性的抗肿瘤活性：在 15 mg/kg 剂量下，可使存活肿瘤细胞数最高降低 81.9%，腹水体积减少 74.3%，同时还能改善肝肾功能及氧化应激标志物[1]。
Caspase-3/7 activator 4 (1-200 mg/kg；腹腔注射；一次) 给予小鼠，并密切监测 48 小时，观察死亡、行为变化和明显的毒性症状。剂量高达 120 mg/kg 时，未观察到死亡或异常行为表现，动物保持正常的梳理毛发、进食和运动活动，表明该浓度具有良好的安全范围。相比之下，给予 200 mg/kg 剂量导致全部动物死亡，因此该剂量被认为是近似致死剂量 (LD100)[1]。

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.
分子量

355.80

Formula

C14H14ClN3O4S
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Caspase-3/7 activator 4 相关分类

  • 摩尔计算器

  • 稀释计算器

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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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