2. Apoptosis Immunology/Inflammation Cell Cycle/DNA Damage Cytoskeleton Neuronal Signaling
  3. Apoptosis COX Caspase Microtubule/Tubulin Monoamine Oxidase
  4. Geiparvarin

Geiparvarin 是一种抗癌剂，是 MAO-B 的抑制剂 (pIC50 = 6.84 μM)。Geiparvarin 通过下调 COX2 表达，抑制血管生成发挥抗肿瘤作用。Geiparvarin 阻滞细胞周期于 G1 期并诱导癌细胞凋亡 (Apoptosis)。Geiparvarin 有抗微管活性 (Microtubule/Tubulin) 并破坏细胞骨架发挥抗增殖作用。Geiparvarin 对肺癌、白血病、乳腺癌具有研究意义。

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Geiparvarin

Geiparvarin Chemical Structure

CAS No. : 36413-91-9

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Geiparvarin 相关抗体

Top Publications Citing Use of Products

查看 COX 亚型特异性产品:

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COX COX-1 COX-2 COX-3

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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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MAO-A MAO-B

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Geiparvarin is an anticancer agent and an inhibitor of MAO-B (pIC50 = 6.84 μM). Geiparvarin exerts anti-tumor effects by downregulating COX2 expression and inhibiting angiogenesis. Geiparvarin blocks the cell cycle at the G1 phase and induces apoptosis of cancer cells. Geiparvarin has anti-microtubule activity and destroys the cytoskeleton to exert anti-proliferative effects. Geiparvarin has research significance for lung cancer, leukemia, and breast cancer[1][2][3][4][5].

IC50 & Target

COX-2

 

Caspase 3

 

MAO-B

6.84 μM (pIC50)

体外研究
(In Vitro)

Geiparvarin (Compound 8) (72 h) (48 h) 对人类多种肿瘤细胞系的增值有抑制作用 (IC50: 5.7 μM for SHSY5Y, 6.3 μM for HL-60, 9.2 μM for K562, 9.8 μM for HT-1080, 11.5 μM for A-549)[1]。

Geiparvarin (8 μM, 24-72 h) 阻滞 HL-60 细胞周期于 G1 期，诱导非 caspase 依赖性凋亡[1]。

Geiparvarin (72 h) 对耐药细胞系均显示出完全抑制作用，不受介导抗肿瘤药物外排的转运蛋白的影响[1]。

Geiparvarin (1 μM, 24 h) 在 HOS 和 143B 细胞中抑制其侵袭能力[2]。

Geiparvarin (0.5-2 μM, 24-48 h) 在 HOS 和 143B 细胞中激活凋亡通路，抑制 COX2 及下游血管生成通路，诱导 caspase 依赖性凋亡[2]。

Geiparvarin 在骨肉瘤细胞中依赖 COX2 下调发挥抗肿瘤作用，COX2 过表达逆转其对增殖和侵袭的抑制[2]。

Geiparvarin (10 μM, 24 h) 在 Balb/c 3T3 成纤维细胞中破坏细胞骨架，尤其是中间丝[3]。

Geiparvarin (0.01-10 μM) 在鼠肝线粒体提取的 MAO-B 中，抑制率随浓度升高显著增加 pIC50 = 6.84 (IC50 = 1.45 μM)[4]。

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

Geiparvarin 相关抗体:

Cell Viability Assay[1]

Cell Line: K562 cells, HL-60 cells, HT-1080 cells, A-549 cells, SHSY5Y cells , CEM cells, CEM/Vbl100 cells, LoVo cells, LoVo/Doxo cells;
Concentration:
Incubation Time: 72 h
Result: Had an IC50 range of 5.7 μM-11.5 μM in human tumor cell lines.

Cell Cytotoxicity Assay[5]

Cell Line: L02 cells, A-549 cells, HeLa cells, QGY-7701 cells, SW480 cells , SGC7901 cells, MDA-MB-231 cells
Concentration:
Incubation Time: 48 h
Result: Had significant inhibitory activity against a variety of cancer cells (such as SGC7901: IC₅₀=7.59 μM; HeLa: IC₅₀=9.09 μM) and had low toxicity to normal liver cells L02 (IC₅₀>300 μM).
Ranged in IC₅₀ values of cells after treatment: 7.59-20.34 μM.

Apoptosis Analysis[1][2]

Cell Line: HOS Cells, 143B Cells, HL-60 cells
Concentration: 0.5 μM, 1 μM, 2 μM for HOS Cells and 143B Cells 8 μM for HL-60 cells
Incubation Time: 24 h, 48 h for HOS Cells and 143B Cells; 72 h for HL-60 cells
Result: Significantly increased Caspase-3 enzyme activity.
Reduced the proportion of G1 phase cells from 43.7 % to S phase cells from 34.8 % after 72 hours.
Induced DNA fragmentation in HL-60 cells.
Caused chromatin condensation and apoptotic body formation in HL-60 cells, as observed by electron microscopy.

Cell Invasion Assay[2]

Cell Line: HOS Cells, 143B Cells
Concentration: 1 μM
Incubation Time: 24 h
Result: Significantly reduced the number of cells penetrating the membrane.

Western Blot Analysis[2]

Cell Line: HOS Cells, 143B Cells
Concentration: 0.5 μM, 1 μM, 2 μM
Incubation Time: 24 h, 48 h
Result: Down-regulated COX2, VEGF, CD31 (angiogenesis-related proteins) and up-regulated cleaved PARP/caspase-3 (apoptosis proteins).

Immunofluorescence[3]

Cell Line: Balb/c 3T3 fibroblasts
Concentration: 10 μM
Incubation Time: 24 h
Result: Slightly shortened microfilaments and reduced their density, inhibited microtubule polymerization, and caused the intermediate filament vimentin to reorganize into short fibers and accumulate around the nucleus.
体内研究
(In Vivo)

Geiparvarin (Compound 8) (0.5 mg/kg, i.p, 每三天持续数周/每天) 在裸鼠的 143B/9901 细胞异种移植瘤模型中抑制肿瘤生长和肺转移，无显著毒性[2]。

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

Animal Model: 143B/9901 cells xenograft tumor model in female nude mice (6 weeks)[2]
Dosage: 0.5 mg/kg
Administration: Intraperitoneal injection (i.p.), every 3 days for several weeks; Intraperitoneal injection (i.p.),every day (for safety assessment)
Result: Significantly reduced the tumor volume and weight of the subcutaneous transplanted tumor model, and increased the apoptotic cells in the tumor tissue.
Inhibited the growth of primary tumors and lung metastasis, and reduced the number and size of lung metastatic nodules.
Increased the weight of mice, and there was no pathological damage to major organs.
分子量

326.34

Formula

C19H18O5
CAS 号
结构分类
初始来源
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

Geiparvarin 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

Geiparvarin36413-91-9ApoptosisCOXCaspaseMicrotubule/TubulinMonoamine OxidaseCyclooxygenaseMAOOsteosarcomaLung Metastasis143B cells9901 cellsK562 cellsHL-60 cellsHT-1080 cellsA-549 cellsSHSY5Y cellsLoVo/Doxo cellsCEM/Vbl100 cellsBalb/c 3T3 fibroblasts CancerInhibitorinhibitorinhibit

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