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Cat. No.: HY-162456

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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.

Formula: C₅₂H₆₀I₂N₄
Molecular Weight:994.87

Storage:

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

Data Sheet (277 KB)

Anticancer agent 205 Chemical Structure

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Cellular Effect

Cell Line	Type	Value	Description	References
BJ	IC₅₀	>40 μM Compound: 9	Antiproliferative activity against human BJ cells measured after 48 hrs by MTT assay Antiproliferative activity against human BJ cells measured after 48 hrs by MTT assay	[PMID: 38624086]
HCT-116	IC₅₀	3.4 μM Compound: 9	Antiproliferative activity against human HCT-116 cells measured after 48 hrs by MTT assay Antiproliferative activity against human HCT-116 cells measured after 48 hrs by MTT assay	[PMID: 38624086]
HeLa	IC₅₀	23.5 μM Compound: 9	Antiproliferative activity against human HeLa cells measured after 48 hrs by MTT assay Antiproliferative activity against human HeLa cells measured after 48 hrs by MTT assay	[PMID: 38624086]
HepG2	IC₅₀	>40 μM Compound: 9	Antiproliferative activity against human HepG2 cells measured after 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells measured after 48 hrs by MTT assay	[PMID: 38624086]
HFF-1	IC₅₀	32.7 μM Compound: 9	Antiproliferative activity against human HFF-1 cells measured after 48 hrs by MTT assay Antiproliferative activity against human HFF-1 cells measured after 48 hrs by MTT assay	[PMID: 38624086]
LoVo	IC₅₀	13.4 μM Compound: 9	Antiproliferative activity against human LoVo cells measured after 48 hrs by MTT assay Antiproliferative activity against human LoVo cells measured after 48 hrs by MTT assay	[PMID: 38624086]
MDA-MB-231	IC₅₀	34.6 μM Compound: 9	Antiproliferative activity against human MDA-MB-231 cells measured after 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells measured after 48 hrs by MTT assay	[PMID: 38624086]
PANC-1	IC₅₀	24.8 μM Compound: 9	Antiproliferative activity against human PANC-1 cells measured after 48 hrs by MTT assay Antiproliferative activity against human PANC-1 cells measured after 48 hrs by MTT assay	[PMID: 38624086]

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.

Chemical Information

Molecular Weight 994.87
Formula C₅₂H₆₀I₂N₄
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-]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Zheng BX, et al. Mitochondria-Selective Dicationic Small-Molecule Ligand Targeting G-Quadruplex Structures for Human Colorectal Cancer Therapy. J Med Chem. 2024 Apr 25;67(8):6292-6312. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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