Anticancer agent 239
Anticancer agent 239 (Compound 5) is a ligand of hTERT promoter G-quadruplex DNA structures (hTERT G4) (Kd = 1.1 μM), and downregulates hTERT expression. Anticancer agent 239 decreases telomerase activity, shortens telomere length, and induces DNA damage, acute cellular senescence, and apoptosis. Anticancer agent 239 causes mitochondrial dysfunction, disrupts iron metabolism and activates ferroptosis in cancer cells. Anticancer agent 239 inhibits tumor growth in MDA-MB-231 xenograft mouse model.
For research use only. We do not sell to patients.
- Formula: C37H36F3IN4S
- Molecular Weight:752.67
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Cellular Effect
|
Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
2.1 μM
Compound: 5
|
Cytotoxicity against telomerase-positive human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Cytotoxicity against telomerase-positive human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
|
[PMID: 38987863] |
| HeLa | IC50 |
2.6 μM
Compound: 5
|
Cytotoxicity against telomerase-positive human HeLa cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Cytotoxicity against telomerase-positive human HeLa cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
|
[PMID: 38987863] |
| HepG2 | IC50 |
2.9 μM
Compound: 5
|
Cytotoxicity against telomerase-positive human HepG2 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Cytotoxicity against telomerase-positive human HepG2 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
|
[PMID: 38987863] |
| HK-2 | IC50 |
9.4 μM
Compound: 5
|
Cytotoxicity against human HK-2 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Cytotoxicity against human HK-2 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
|
[PMID: 38987863] |
| HUVEC | IC50 |
8.7 μM
Compound: 5
|
Cytotoxicity against HUVEC cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Cytotoxicity against HUVEC cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
|
[PMID: 38987863] |
| MDA-MB-231 | IC50 |
0.67 μM
Compound: 5
|
Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs in presence of TBHP by MTT assay
Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs in presence of TBHP by MTT assay
|
[PMID: 38987863] |
| MDA-MB-231 | IC50 |
1 μM
Compound: 5
|
Cytotoxicity against telomerase-positive human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Cytotoxicity against telomerase-positive human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
|
[PMID: 38987863] |
| MDA-MB-231 | IC50 |
1.2 μM
Compound: 5
|
Cytotoxicity against human MDA-MB-231 cells without hTERT overexpression assessed as inhibition of cell growth measured after 48 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells without hTERT overexpression assessed as inhibition of cell growth measured after 48 hrs by MTT assay
|
[PMID: 38987863] |
| MDA-MB-231 | IC50 |
3.3 μM
Compound: 5
|
Cytotoxicity against human MDA-MB-231 cells transfected with hTERT-pcDNA3.1(+)-C-eBFP overexpressing hTERT assessed as inhibition of cell growth measured after 48 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells transfected with hTERT-pcDNA3.1(+)-C-eBFP overexpressing hTERT assessed as inhibition of cell growth measured after 48 hrs by MTT assay
|
[PMID: 38987863] |
| PC-3 | IC50 |
2.5 μM
Compound: 5
|
Cytotoxicity against telomerase-positive human PC-3 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Cytotoxicity against telomerase-positive human PC-3 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
|
[PMID: 38987863] |
| U2OS | IC50 |
3.9 μM
Compound: 5
|
Cytotoxicity against alternative lengthening of telomere-positive human U2OS cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Cytotoxicity against alternative lengthening of telomere-positive human U2OS cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
|
[PMID: 38987863] |
Chemical Information
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Molecular Weight 752.67
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Formula C37H36F3IN4S
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SMILES
C[N+]1=C(C=C(C2=CC=CC=C21)/C=C3SC4=C(N\3CCCN5CCC(CC5)C(F)(F)F)C=CC=C4)/C=C/C6=CNC7=C6C=CC=C7.[I-]
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Hot Topics
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All
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Topics
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Most Recent
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Oldest
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Topics Cellular Senescence & Age-related Diseases
Cellular senescence is a stable state of cell-cycle arrest triggered by diverse forms of cellular stress, including telomere shortening, DNA damage, oncogene activation, mitochondrial dysfunction, oxidative stress, and chromatin perturbation.
2026-06-18
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Topics G-quadruplex & DNA Replication
G-quadruplexes (G4s) are noncanonical nucleic acid secondary structures formed by guanine-rich sequences through stacked G-tetrads stabilized by Hoogsteen hydrogen bonding.
2026-06-18
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Topics Senolytics and Senomorphic Strategies in Aging Research
Cellular senescence is a stable state of cell-cycle arrest triggered by DNA damage, telomere attrition, oncogenic signaling, and other forms of cellular stress.
2026-06-18
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Topics Molecular Spark of cGAS-STING-Mediated Cellular Senescence
Cellular senescence is a stress-response program characterized by irreversible cell-cycle arrest and the senescence-associated secretory phenotype (SASP), originally recognized as a tumor-suppressive mechanism and now considered a central process in aging biology, inflammation, and cancer research.
2026-06-18
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)