1. MAPK/ERK Pathway Metabolic Enzyme/Protease Stem Cell/Wnt NF-κB Immunology/Inflammation Apoptosis
  2. Raf HIF/HIF Prolyl-Hydroxylase ERK MEK Reactive Oxygen Species (ROS) Apoptosis Caspase
  3. MO-2097

MO-2097 是一种 RAF-1/HIF-1α 抑制剂。MO-2097 诱导 RAF-1 不稳定,导致 EMT 相关转录因子和间质标记物减少。MO-2097 在低氧及模拟低氧条件下通过 hnRNPA2B1 介导抑制 HIF-1α 蛋白表达。MO-2097 诱导线粒体 ROS 产生,从而导致细胞凋亡 (apoptosis)。MO-2097 通过抑制 RAF/MEK/ERK 信号通路,有效抑制结直肠癌转移。MO-2097 在人结直肠癌 HCT116 细胞异种移植小鼠模型中可抑制肿瘤生长。MO-2097 可用于结直肠癌研究。

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MO-2097

MO-2097 Chemical Structure

CAS No. : 2744300-63-6

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MO-2097 is a RAF-1/HIF-1α inhibitor. MO-2097 induces RAF-1 destabilization, leading to a reduction in EMT-associated transcription factors and mesenchymal markers. MO-2097 inhibits HIF-1a protein expression mediated by hnRNPA2B1 under hypoxic and mimetic hypoxia. MO-2097 induces mitochondrial ROS, which leads to apoptosis in cells. MO-2097 effectively suppresses colorectal cancer metastasis by inhibiting the RAF/MEK/ERK signaling pathway. MO-2097 attenuates tumor growth in a xenograft HCT116 cell mouse model. MO-2097 can be used for the study of colorectal cancer[1][2].

体外研究
(In Vitro)

MO-2097 (10-30 μM, 24-48 h) 抑制 DLD-1 细胞和 HCT116 细胞的细胞迁移[1]
MO-2097 (10-50 μM, 1-6 h) 抑制 DLD-1 细胞和 HCT116 细胞中 RAF-1 驱动的 RAF/MEK/ERK 信号级联[1]
MO-2097 (10-30 μM, 5-9 days) 在三维肿瘤球体模型中抑制结直肠癌细胞 (DLD-1 细胞和 HCT116 细胞) 的侵袭性[1]
MO-2097 (30-100 μM, 4 h) 通过抑制 HUVEC 细胞的管状形成从而抑制血管生成[1]
MO-2097 (25-500 μM, 24 h) 在 HeLa CCL2 细胞和 HCT116 细胞中表现出低毒性,直接结合 hnRNPA2B1,并抑制 HIF-1α 表达[2]
MO-2097 (25-50 μM, 24 h) 在低氧条件下抑制 HeLa CCL2 细胞和 HCT116 细胞中 HIF-1α 靶基因 mRNA (HK1, MRP1, SLC1A5, IL-6, and VEGF) 的表达水平[2]
MO-2097 (12.5-50 μM, 24 h) 在 HeLa CCL2 细胞中诱导线粒体 ROS 产生,从而导致凋亡,表现为裂解的 caspase 3caspase 9[2]
MO-2097 (12.5-50 μM, 7-10 days) 在三维培养球体模型的低氧区域和三维培养的人结肠癌类器官中诱导特异性抗癌效应[2]

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

Cell Migration Assay [1]

Cell Line: DLD-1 and HCT116 cells
Concentration: 10, 20, 30 μM
Incubation Time: 24, 48 h
Result: Suppressed cell migration at 86.5% and 77.5% in DLD-1 cells and HCT116 cells, relative to the control, respectively.

Western Blot Analysis[1]

Cell Line: DLD-1 and HCT116 cells
Concentration: 10, 20, 30, 40, 50 μM
Incubation Time: 1, 2, 4, 6 h
Result: Decreased RAF-1 levels gradually in Cycloheximide (CHX) (HY-12320)-only treated cells.
Prevented RAF-1 accumulation without influencing the proteasomal degradation process.
Reduced the phosphorylation of MEK and ERK.
Decreased the levels of transcription factors Snail, Slug and ZEB1.

Immunofluorescence[2]

Cell Line: HeLa CCL2 cells
Concentration: 12.5, 25, 50 μM
Incubation Time: 24 h
Result: Decreased the amount of HIF-1a protein in the nucleus in a dose-dependent manner under hypoxic conditions.
Induced mitochondrial ROS.

Real Time qPCR[2]

Cell Line: HeLa CCL2 cells and HCT116 cells
Concentration: 25, 50 μM
Incubation Time: 24 h
Result: Inhibited HK1, MRP1, SLC1A5, IL-6, and VEGF expression levels in HeLa CCL2 cells and HCT116 cells under hypoxic conditions.
体内研究
(In Vivo)

MO-2097 (25-50 mg/kg,腹腔注射,两天一次,持续 15 天) 通过抑制 HIF-1α 表达诱导肿瘤细胞凋亡,在 HCT116 细胞异种移植小鼠模型中抑制体内肿瘤生长[1]

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

Animal Model: Male Balb/C nude mice (6 weeks) xenografted HCT116 cells (2 × 105 cells/mouse)[1]
Dosage: 25, 50 mg/kg
Administration: i.p. every other day for 15 days
Result: Reduced the embedded tumor volume by approximately 49 % without any considerable body weight loss.
Decreased HIF-1a expression.
Increased expression of cleaved caspase 3.
分子量

308.33

Formula

C19H16O4

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
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MO-2097
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HY-N13009
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