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

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.

For research use only. We do not sell to patients.

Anticancer agent 205 Chemical Structure

Anticancer agent 205 Chemical Structure

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Description

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].

In Vitro

Anticancer agent 205 (compound 9) (4 µM; 1 h) interacts with G4-mtDNA in HCT116 cells[1].
Anticancer agent 205 (0, 1, 2, 4 µM; 48 h) reduces the mRNA level of ND2 and ND5 in HCT116, HFF1 cells[1].
Anticancer agent 205 (0, 1, 2, 4 µM; 48 h) reduces the protein levels of ND3, ND4, ND6, COX1, COX2, COX3, CYTB, ATP6, and ATP8 in HCT116 cells[1].
Anticancer agent 205 (0-4 µM) increases the ROS level in a concentration-dependent manner[1].
Anticancer agent 205 (0-4 µM; 72 h) induces DNA damage and cellular senescence[1].

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

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%.
In Vivo

Anticancer agent 205 (5 mg/kg; i.v.; every 2 days for 16 days) inhibits tumor growth in xenograft mouse model of HCT116[1].

MedChemExpress (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.
Molecular Weight

994.87

Formula

C52H60I2N4

Unlabeled Cas

SMILES

C12=CC=CC=C1C=CC(/C=C/C3=CC=C(C=C3)N4CCCCC4)=[N+]2CCCCCCCC[N+]5=C(C=CC6=C5C=CC=C6)/C=C/C7=CC=C(C=C7)N8CCCCC8.[I-].[I-]

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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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.

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Anticancer agent 205
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HY-162456
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