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Inhibitor of Phosphatidylinositol Turnover Inostamycin A (sodium salt)

Date:July 03 2020Web Page No:520050

Inostamycin A is isolated from the culture fluid of Streptomyces sp. MH816-AF15 and inhibits cytidine diphosphodiacylglycerol (CDP-DG): inositol transferase 1).

Inostamycin A Structure

Specification

CAS#1884611-95-3
Molecular FormulaC38H67O11 Na
Molecular Weight722.933
SourceStreptomyces sp. MH816-AF15
Purity> 90% (Quantitative NMR)
SolubilitySoluble in DMSO, DMF and CHCl3. Poorly soluble in H2O

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Mechanism

Inostamycin A Mechanism

Phosphatidylinositol 2-phosphate (PIP2), generated from phosphatidylinositol (PI) present in the cell membrane, is degraded by phospholipase C (PLC) to inositol triphosphate (IP3) and diacylglycerol (DG), and IP3 is converted to inositol (I). The inositol (I) is bound to CDP-DG and PI is resynthesized. This metabolic turnover is called the inositol phospholipid turnover. IP3 generated by this turnover releases Ca2+ from the endoplasmic reticulum, and the Ca2+ and DG activate protein kinase C (PKC), which phosphorylates various intracellular proteins to activate proliferation signals and cancer malignancy signals.
Inostamycin A inhibits the synthesis of PI from I and CDP-DG in inositol-phospholipid-turnover and arrests cell-cycle in G1 phase, thereby inhibiting cell proliferation 2).

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Application Note

  • Inhibited in vitro CDP-DG: inositol transferase activity of the A431 cell membrane, the IC50 was about 0.02 μg/ml 1)
  • Inhibited EGF-induced inositol incorporation into inositol lipids with an IC50 of about 0.5 μg/ml in the A431 cell assay system 2)
  • Showed antimicrobial activities against Gram-positive bacteria and cytocidal activity against srk-NIH-3T3 cell with IC50 value of 0.07 μg/ml 3)
  • Potenciated colchitine cytotoxicity toward KB-C4 cells at 3 μg/ml 4)
  • Enhanced the cytotoxic effect of Taxol on small cell lung cancer cells 5)
  • Caused Ms-1 cell to accumulate in the G1 phase at 0.1 μg/ml and induces morphological apoptosis at high concentration (0.3 μg/ml) 6)

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Reference

  1. Imoto M. et al. J. Biochem., 112, 299~302 (1992)
  2. Imoto M. et al. J. Nat. Prod., 53(4), 825~829 (1990)
  3. Odai H. et al. J. Antibiot., 47(8), 939~941 (1994)
  4. Kawada M. et al. J. Antibiot., 45(4), 556~562 (1992)
  5. Imoto M. et al. Jpn. J. Cancer Res., 89(9), 315~322 (1998)
  6. Simizu S. et al. Jpn. J. Cancer Res., 89(9), 970~976 (1998)

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[Date : June 20 2024 00:07]

Detail Product Name Product Code Supplier Size Price
Inostamycin A (Sodium Salt), Antitumor
DatasheetThis may not be the latest data sheet.
14652 IMCInstitute of Microbial Chemistry 1 mg $500

Description Supplied as sodium salt
Storage -20°C CAS 1884611-95-3 (sodium salt), 129905-10-8 (salt free form)
Link

Bioactive Compounds

[Date : June 20 2024 00:07]

Inostamycin A (Sodium Salt), Antitumor


  • Product Code: 14652
  • Supplier: IMC
  • Size: 1mg
  • Price: $500

Description Supplied as sodium salt
Storage -20°C CAS 1884611-95-3 (sodium salt), 129905-10-8 (salt free form)
Link

Bioactive Compounds

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