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).
Specification
CAS# | 1884611-95-3 |
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Molecular Formula | C38H67O11 Na |
Molecular Weight | 722.933 |
Source | Streptomyces sp. MH816-AF15 |
Purity | > 90% (Quantitative NMR) |
Solubility | Soluble in DMSO, DMF and CHCl3. Poorly soluble in H2O |
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).
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)
Reference
- Imoto M. et al. J. Biochem., 112, 299~302 (1992)
- Imoto M. et al. J. Nat. Prod., 53(4), 825~829 (1990)
- Odai H. et al. J. Antibiot., 47(8), 939~941 (1994)
- Kawada M. et al. J. Antibiot., 45(4), 556~562 (1992)
- Imoto M. et al. Jpn. J. Cancer Res., 89(9), 315~322 (1998)
- Simizu S. et al. Jpn. J. Cancer Res., 89(9), 970~976 (1998)
[Date : January 24 2025 00:06]
Detail | Product Name | Product Code | Supplier | Size | Price | ||||||||||||||||||||||||||||||
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Inostamycin A (Sodium Salt), Antitumor DatasheetThis may not be the latest data sheet. |
14652 | IMCInstitute of Microbial Chemistry | 1 mg | $500 | |||||||||||||||||||||||||||||||
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[Date : January 24 2025 00:06]
Inostamycin A (Sodium Salt), Antitumor
DatasheetThis may not be the latest data sheet.
- Product Code: 14652
- Supplier: IMC
- Size: 1mg
- Price: $500
Description |
Supplied as sodium salt |
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Storage | -20°C | CAS | 1884611-95-3 (sodium salt), 129905-10-8 (salt free form) |
Link |
CONTACT
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