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Cat. No.: HY-162688

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Anticancer agent 239

Anticancer agent 239 (Compound 5) is a ligand of hTERT promoter G-quadruplex DNA structures (hTERT G4) (K_d = 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

Storage:

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

Data Sheet (270 KB)

Anticancer agent 239 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
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Cellular Effect

Cell Line	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

Molecular Weight 752.67
Formula C₃₇H₃₆F₃IN₄S
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-]
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 (270 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]. Long W, et al. Targeting hTERT Promoter G-Quadruplex DNA Structures with Small-Molecule Ligand to Downregulate hTERT Expression for Triple-Negative Breast Cancer Therapy. J Med Chem. 2024 Jul 10. [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.

Keywords

100 mg

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