2. Apoptosis Metabolic Enzyme/Protease Immunology/Inflammation NF-κB
  3. Apoptosis Reactive Oxygen Species
  4. Anticancer agent 205

Anticancer agent 205 (compound 9) 是一种有效的抗癌剂。Anticancer agent 205 与 G4-mtDNA 靶标结合并抑制 mtDNA (线粒体基因组) 的复制、转录和翻译。Anticancer agent 205 会导致线粒体功能障碍、增加 ROS 产生、诱导 DNA 损伤和细胞衰老。Anticancer agent 205 诱导细胞凋亡 (apoptosis) 和细胞周期停滞在 G0/G1 期。Anticancer agent 205 具有研究结直肠癌的潜力。

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Anticancer agent 205 Chemical Structure

Anticancer agent 205 Chemical Structure

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Anticancer agent 205 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Anticancer agent 205 (compound 9) is a potent anticancer agent. Anticancer agent 205 binds to G4-mtDNA target and inhibits the replication, transcription, and translation of mtDNA (mitochondrial genome). Anticancer agent 205 causes mitochondrial dysfunction, increases ROS production, induces DNA damage and cellular senescence. Anticancer agent 205 induces apoptosis and cell cycle arrests at G0/G1 phase. Anticancer agent 205 has the potential for the research of colorectal cancer[1].

体外研究
(In Vitro)

Anticancer agent 205 (compound 9) (4 µM; 1 h) 与 HCT116 细胞中的 G4-mtDNA 相互作用[1]。
Anticancer agent 205 (0, 1, 2, 4 µM; 48 h) 可降低 HCT116、HFF1 细胞中 ND2 和 ND5 的 mRNA 水平[1]。
Anticancer agent 205 (0, 1, 2, 4 µM; 48 h) 可降低 HCT116 细胞中 ND3、ND4、ND6、COX1、COX2、COX3、CYTB、ATP6 和 ATP8 的蛋白水平[1].
Anticancer agent 205 (0-4 µM) 以浓度依赖性方式提高 ROS 水平[1]。
Anticancer agent 205 (0-4 µM; 72 h) 会诱导 DNA 损伤和细胞衰老[1]。

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

Anticancer agent 205 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: HCT116, LoVo, HeLa, HepG2, PANC-1, MDA-MB-231, HFF1, BJ cells
Concentration: 0-40 µM
Incubation Time: 48 h
Result: Showed cytotoxicity for HCT116, LoVo, HeLa, HepG2, PANC-1, MDA-MB-231, HFF1, BJ cells with IC50s of 3.4, 13.4, 23.5, >40, 24.8, 34.6, 32.7, >40 µM, respectively.

RT-PCR[1]

Cell Line: HCT116, HFF1 cells
Concentration: 0, 1, 2, 4 µM
Incubation Time: 48 h
Result: Caused a significant reduction of mRNA levels for ND1, ND2, ND3, ND4, ND4L, ND5, COX2, ATP6, and ATP8 in HCT116, only ND2 and ND5 showed a significant reduction in HFF1 cells.

Western Blot Analysis[1]

Cell Line: HCT116 cells
Concentration: 0, 1, 2, 4 µM
Incubation Time: 48 h
Result: Showed that the protein levels of ND3, ND4, ND6, COX1, COX2, COX3, CYTB, ATP6, and ATP8 were decreased markedly.

Cell Cycle Analysis[1]

Cell Line: HCT116 cells
Concentration: 0, 1, 2, 4 µM
Incubation Time: 48 h
Result: Induced cell cycle arrested in the G0/G1 phase with The percentage of the G0/G1 phase is increased from 50.66 to 66.01%, in a concentration-dependent manner, induces apoptosis by increases the expression of cleaved-caspase3 and the apoptosis cell increased from 2.64% to 27.4%.
体内研究
(In Vivo)

Anticancer agent 205 (5 mg/kg; i.v.; every 2 days for 16 days) 可抑制 HCT116 异种移植小鼠模型中的肿瘤生长[1]。

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

Animal Model: male Balb/c nude mice (HCT116 cells)[1].
Dosage: 5 mg/kg
Administration: I.v.; every 2 days for 16 days
Result: Significantly inhibited the growth of tumors with the tumor growth reduced by 70% approximately.
分子量

994.87

Formula

C52H60I2N4
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

Anticancer agent 205 相关分类

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  • 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:

Anticancer agent 205Anticancer agent205Anticancer agent-205ApoptosisReactive Oxygen SpeciesG4-mtDNAHCT116 cellsROS levelapoptosisDNA damagecellular senescenceG0/G1 phaseanticancerInhibitorinhibitorinhibit

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