1. Apoptosis Cell Cycle/DNA Damage Anti-infection
  2. Apoptosis DNA/RNA Synthesis Antibiotic
  3. Dehydroaltenusin

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.

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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].

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

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].

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

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.
SMILES

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

Structure Classification
Initial Source

Talaromyces flavus B 5

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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
References
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Product Name:
Dehydroaltenusin
Cat. No.:
HY-100513A
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