Geldanamycin Introduction
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Geldanamycin is a yellow powder that is slightly soluble in water. Its CAS number is 30562-34-6. Molecular formula: C29H40N2O9; Molecular weight: 560.64; EINECS: 999-999-2. Geldanamycin is a secondary metabolic natural product. It can also be obtained through microbial liquid deep fermentation, and then purified through extraction, chromatography, and full chemical synthesis, which is extremely costly. Its main application fields include tumor research, molecular biochemistry basic experiments, inflammatory and immune mechanism studies, virus research, and the preliminary development of new compounds.
What Is The Function Of Geldanamycin?
Geldanamycin is not a clinical application reagent. It is a highly valuable tool molecule and lead research substrate in biomedical research. In the fields of molecular biology and pharmacological research, it is a classic specific inhibitor targeting heat shock protein Hsp90, and is often used to explore the regulatory mechanisms of Hsp90 in cell signal transduction, protein folding, and tumor evolution processes.
Geldanamycin has broad-spectrum potential for tumor intervention and can effectively degrade various tumor-related functional proteins. Its structural derivatives, 17-AAG, have also entered the clinical research stage. At the same time, numerous basic experiments have confirmed that it also possesses diverse biological activities such as antiviral, antibacterial, and antiprotozoal properties.
Due to its obvious physical and chemical defects such as liver irritation and poor water solubility, geldanamycin is not suitable for direct use in human-related applications. Currently, its core value mainly lies in serving as the core parent structure, providing important structural support for the development of safer and more efficient Hsp90-targeted research molecules and PROTAC degradation systems.
What Are The Pharmacological Effects Of Geldanamycin?
Geldanamycin is a core research tool molecule targeting the heat shock protein Hsp90. By precisely regulating the biological activity of Hsp90 and interfering with the operation of cellular pathways, it is widely used in various studies related to cellular mechanisms. Its core mechanism of action is that Hsp90 maintains its activity by relying on its ATP binding region, and performs the molecular chaperone function of protein folding, stabilization, and metabolic regulation within the cell. Geldanamycin can competitively bind to the terminal ATP binding site of Hsp90, inhibit its ATPase activity, directly block the molecular chaperone function of Hsp90, and disrupt the stable state of downstream target proteins.
As a natural microbial metabolite, geldanamycin possesses multiple biological activities. It has good inhibitory effects on most Gram-positive bacteria and some Gram-negative bacteria, and also has antiviral activity. It can be used in various research studies on microbial mechanisms.
In addition, geldanamycin has excellent synergistic regulatory capabilities. It can interfere with the mitochondrial transport of Hsp90, activate succinate dehydrogenase, increase the intracellular reactive oxygen level, enhance the effect of azole antibacterial components, significantly improve the inhibitory and clearance ability of the microbial community, and provide a new research direction for the study of complex antibacterial systems.
MF of geldanamycin
| CAS | 30562-34-6 |
| Molecular formula | C29H40N2O9 |
| Molecular weight | 560.64 |
| EINECS | 999-999-2 |
| Density | 1.2443 |
| Boiling point | 627.87°C |
Specification
| Item | Specification | Result |
| Appearance | Yellow powder | Complies |
| Assay | ≥97.0% | 98.89% |
| Conclusion | Conform with enterprise specification | |
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FAQ:
Q1:Who is the "renowned descendant" of geldanamycin?
To overcome the toxicity, scientists synthesized various derivatives, among which the most well-known ones are 17-AAG and 17-DMAG. These were the first Hsp90 inhibitors to enter clinical trials.
Q2:Does geldanamycin have any other activities?
Yes. It was initially discovered for its antibacterial and antiprotozoal properties, and subsequent studies have also shown that it possesses various biological activities such as antiviral properties.
Q3:Can geldanamycin be used directly as a medicine?
No. Although the prospect is attractive, due to serious liver toxicity, poor water solubility, and unstable metabolism, it cannot be directly used as a compound on its own.
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