1. Apoptosis
    Cell Cycle/DNA Damage
  2. Apoptosis
    DNA/RNA Synthesis
  3. Dehydroaltenusin

Dehydroaltenusin 

Cat. No.: HY-100513A
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Dehydroaltenusin is a small molecule selective inhibitor of eukaryotic DNA polymerase α, a type of antibiotic produced by a fungus with an IC50 value of 0.68 μM. The inhibitory mode of action of dehydroaltenusin against mammalian pol α activity is competitive with respect to the DNA template primer (Ki=0.23 µM) and non-competitive with respect to the 2'-deoxyribonucleoside 5'-triphosphate substrate (Ki=0.18 µM). Dehydroaltenusin arrests the cancer cell cycle at the S-phase and triggers apoptosis. Dehydroaltenusin possesses anti-tumor activity against human adenocarcinoma tumor in vivo.

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

Dehydroaltenusin Chemical Structure

Dehydroaltenusin Chemical Structure

CAS No. : 31186-13-7

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Description

Dehydroaltenusin is a small molecule selective inhibitor of eukaryotic DNA polymerase α, a type of antibiotic produced by a fungus with an IC50 value of 0.68 μM. The inhibitory mode of action of dehydroaltenusin against mammalian pol α activity is competitive with respect to the DNA template primer (Ki=0.23 µM) and non-competitive with respect to the 2'-deoxyribonucleoside 5'-triphosphate substrate (Ki=0.18 µM)[1]. Dehydroaltenusin arrests the cancer cell cycle at the S-phase and triggers apoptosis[1]. Dehydroaltenusin possesses anti-tumor activity against human adenocarcinoma tumor in vivo[1].

IC50 & Target

IC50: 0.68 μM (DNA polymerase α)[1]

In Vitro

Dehydroaltenusin (38.0-44.4 μM; 24 hours) inhibits cell growth in a dose-dependent manner and the LD50 values varies from 38.0 to 44.4 μM[1].
Dehydroaltenusin (38.0 μM; 6 hours) inhibits cell growth by blocking the S-phase of DNA replication[1].
Dehydroaltenusin (75.0 μM; 24 hours) has a strong apoptotic effect on human cancer cells, DNA ladders can be detected after 12 h of incubation with dehydroaltenusin[1].

Cell Proliferation Assay[1]

Cell Line: Human cancer cell line: A549, BALL-1, HeLa and NUGC-3 cells
Concentration: 38.0-44.4 μM
Incubation Time: 24 hours
Result: Inhibited cell growth of human cancer cell lines.

Cell Cycle Analysis[1]

Cell Line: HeLa cells
Concentration: 38.0 μM
Incubation Time: 6 hours
Result: Decreased to 45% of the control value after 6 h of incubation [3H]-thymidine.

Apoptosis Analysis[1]

Cell Line: HeLa cells
Concentration: 75.0 μM
Incubation Time: 12-24 hours
Result: Detected DNA ladders after 12 hours of incubation.
In Vivo

Dehydroaltenusin (injection; 20 mg/kg; 2-day intervals; 12-39 days) shows suppressed tumor growth from 21 days[1].

Animal Model: Nude mice bearing HeLa solid tumors[1]
Dosage: 20 mg/kg
Administration: Injection; 20 mg/kg; 2-day intervals; 12-39 days
Result: Suppressed tumor growth.
Molecular Weight

288.25

Formula

C₁₅H₁₂O₆

CAS No.

31186-13-7

SMILES

O=C(C(O)=C1)C=C(C2=CC(OC)=CC(O)=C23)[[email protected]@]1(C)OC3=O

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Storage

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

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Dehydroaltenusin
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