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Inhibitor for DNA Helicase Heliquinomycin

Date:February 24 2016Web Page No:80631

Heliquinomycin is a natural product derived from actinomycetes and inhibits DNA helicase.

Heliquinomycin-Structure

What is DNA Helicase

In 1976, Hoffmann-Berling et al.5, 6), Heidelberg University in Germany and Mackay and Linn 7), UC Berkeley in the United States first reported that a protein untwisted double-stranded DNA in an ATP-dependent manner. In 1978, the term "Helicase," referring to ATP-dependent double-stranded DNA unwinding enzyme, was proposed by Hoffmann-Berling 8).
DNA helicases move across DNA using energy from ATP hydrolysis and generate single-stranded DNA breaking hydrogen bonds between nucleotide base pairs in DNA double helix. DNA helicases play important roles in maintaining genomic integrity and cellular homeostasis, such as DNA replication, transcription and DNA repair. The importance is evident from the fact that mutations in helicase genes are associated with genetic disorders such as Werner syndrome, Bloom syndrome and RRAPADILINO syndrome as well as various types of cancer 9).

Selective inhibitors of helicase activity are useful in elucidating helicase functions in cell proliferation and expected as lead compounds for development of selective antitumor agents. Compounds that inhibit DNA helicases, such as Heliquinomycin 4), have been reported, and compounds that inhibit viral helicase-primase complex are being developed as antiviral agents.

Reference

  1. Abdel-Monem, M. and Hoffmann-Berling, H., Eur. J. Biochem., 65 (2), 431~440 (1976). [PMID:133022]
  2. Abdel-Monem, M., et al., Eur. J. Biochem., 65 (2), 441~449 (1976). [PMID:133023]
  3. Mackay, V. and Linn, S., J. Biol. Chem., 251 (12), 3716~3719 (1976). [PMID:776974]
  4. Geider, K., et al., The Single-Stranded DNA Phages, p.378~387 (1978). Edited by Denhardt, D., et al., Cold Spring Harbor Laboratory, NY, USA. ()
  5. Brosh, R.M.Jr., Nat. Rev. Cancer, 13 (8), 542~558 (2013). [PMID:23842644]

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Specification

CAS#178182-49-5
Molecular FormulaC33H30O17
Molecular Weight698.586
SourceStreptomyces sp. MJ929-SF2
Purity> 80% (HPLC)
SolubilitySoluble in Ethyl acetate, Ethanol and DMSO.
Insoluble in H2O, Hexane

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Application Note

  • Inhibits DNA helicase from HeLa cell (Ki=6.8 mM)
  • Inhibits Topoisomerase II (IC50=30 μg/ml) and Topoisomerase I (IC50=30 μg/ml)
  • Inhibits the growth of human tumor cell lines (IC50=0.96~2.8 μg/ml)
  • Inhibits both DNA and RNA synthesis in cell culture however does not inhibit protein synthesis

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Reference

  1. Chino, M., et al., J. Antibiotics, 49 (8), 752~757 (1996). [PMID:8823506]
  2. Chino, M., et al., J. Antibiotics, 50 (2), 143~146 (1997). [PMID:9099224]
  3. Chino, M., et al., J. Antibiotics, 50 (9), 781~784 (1997). [PMID:9360626]
  4. Chino, M., et al., J. Antibiotics, 51 (5), 480~486 (1998). [PMID:9666176]

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[Date : June 25 2024 00:08]

Detail Product Name Product Code Supplier Size Price
Heliquinomycin,DNA Helicase Inhibitor
DatasheetThis may not be the latest data sheet.
10665 IMCInstitute of Microbial Chemistry 1 mg $500

Description Inhibitor for DNA Helicase.
Storage 4°C CAS 178182-49-5
Link

Bioactive Compounds
Natural compound Product List

[Date : June 25 2024 00:08]

Heliquinomycin,DNA Helicase Inhibitor


  • Product Code: 10665
  • Supplier: IMC
  • Size: 1mg
  • Price: $500

Description Inhibitor for DNA Helicase.
Storage 4°C CAS 178182-49-5
Link

Bioactive Compounds
Natural compound Product List

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