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Detailed Description
CAS Number: 30562-34-6
Molecular Formula: C29H40N2O9
Molecular Weight: 560.64 g/mol
Mechanism of Action: Geldanamycin binds specifically to the heat shock protein Hsp90 and to its endoplasmic reticulum homologue GP96, and thus interferes with conformational maturation of proteins and the cellular stress response. In addition, it is a potent inhibitor of the nuclear hormone receptor family.
Storage Conditions: -20 °C; Protect from light
Tariff Code: 2941.90.1050
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Applications
Spectrum: Moderately active in vitro against bacteria, protozoa, fungi.
Microbiology Applications: Geldanamycin can inhibit the replication of severe acute respiratory syndrome coronavirus. Its antiviral mechanism appears to be broad-spectrum antiviral activity. It can also inhibit the replication of Herpes SImplex Virus Type 1 in vitro (Li et al, 2004).
Cancer Applications:
In normal cells, Hsp90 stabilizes and folds proteins, however, in tumor cells, Hsp90 activity helps stabilize mutated growth factor and signal proteins which facilitate tumor growth. To prevent this complication, Geldanamycin binds to and inactivates Hsp90 in cancerous cells leading to degradation of cancer cell proteins.
Geldanamycin was used to synthesize 2 new geldanamycines: 17-(tryptamine)-17-demethoxygeldanamycin (2) and 17-(5′-methoxytryptamine)- 17-demethoxygeldanamycin. Findings showed these derivatives had selective cytotoxicity toward some cancer cell at a lower concentration, so future studies could be useful (Taechowisan et al, 2020)
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Specifications
Form: Solution
Appearance: Yellow solution
Source: Streptomyces Hygroscopicus
Purity Level: ≥99.0%
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References
References:
DeBoer C, Meulman PA, Wnuk RJ and Peterson DH (1970) GEldanamycin, a new antibiotic. J. Antibiotics 23(9):442-447
Franke J, Eichner S, Zelinger C and Kirschning A (2013) Targeting heat-shock-protein 90 (Hsp90) by natural products: Geldanamycin, a show case in cancer therapy. Natural Product Reports 30:1299-1323
Kai E (2001) Geldanamycin: The prototype of a class of antitumor drugs targeting the heat shock protein 90 family of molecular chaperones. Cell Stress Chaperones 6(2):105-112
Li YH, Tao PZ, Liu YZ, Jiang JD (2004) Geldanamycin, a ligand of heat shock protein 90, inhibits the replication of herpes simplex virus type 1 in vitro. Antimicrob Agents Chemother.48(3):867-72 PMID 14982777
Taechowisan T, Samsawat T, Puckdee W, Phutdhawong WS (2020) Cytotoxicity activity of Geldanamycin derivatives against various cancer cell lines. J. Appl. Pharm. Sci. 10(06):012-021
Geldanamycin ReadyMadeTM solution is provided as a sterile-filtered solution of Geldanamycin formulated in DMSO at a concentration of 1 mg/ml. It has been filter-sterilized using a 0.22 μm filter.
Geldanamycin is a 1,4-benzoquinone ansamycin antibiotic which inhibits the stress-induced chaperone heat shock protein 90 (Hsp90). All derivates that can be synthesized from this compound also share its HSP90 inhibition, but very in toxicity and water solubility. It is a natural product and was derived from Streptomyces hygroscopicus. The compound can be used in cancer research as an anti-tumor agent. It can also be used in monocyte and myeloid cell research during the cell differentiation and maturation phases of the workflow. Geldanamycin is soluble in DMSO and methanol but insoluble in water.
We also offer:
- Geldanamycin (G005)
CAS Number: 30562-34-6
Molecular Formula: C29H40N2O9
Molecular Weight: 560.64 g/mol
Mechanism of Action: Geldanamycin binds specifically to the heat shock protein Hsp90 and to its endoplasmic reticulum homologue GP96, and thus interferes with conformational maturation of proteins and the cellular stress response. In addition, it is a potent inhibitor of the nuclear hormone receptor family.
Storage Conditions: -20 °C; Protect from light
Tariff Code: 2941.90.1050
Spectrum: Moderately active in vitro against bacteria, protozoa, fungi.
Microbiology Applications: Geldanamycin can inhibit the replication of severe acute respiratory syndrome coronavirus. Its antiviral mechanism appears to be broad-spectrum antiviral activity. It can also inhibit the replication of Herpes SImplex Virus Type 1 in vitro (Li et al, 2004).
Cancer Applications:
In normal cells, Hsp90 stabilizes and folds proteins, however, in tumor cells, Hsp90 activity helps stabilize mutated growth factor and signal proteins which facilitate tumor growth. To prevent this complication, Geldanamycin binds to and inactivates Hsp90 in cancerous cells leading to degradation of cancer cell proteins.
Geldanamycin was used to synthesize 2 new geldanamycines: 17-(tryptamine)-17-demethoxygeldanamycin (2) and 17-(5′-methoxytryptamine)- 17-demethoxygeldanamycin. Findings showed these derivatives had selective cytotoxicity toward some cancer cell at a lower concentration, so future studies could be useful (Taechowisan et al, 2020)
Form: Solution
Appearance: Yellow solution
Source: Streptomyces Hygroscopicus
Purity Level: ≥99.0%
References:
DeBoer C, Meulman PA, Wnuk RJ and Peterson DH (1970) GEldanamycin, a new antibiotic. J. Antibiotics 23(9):442-447
Franke J, Eichner S, Zelinger C and Kirschning A (2013) Targeting heat-shock-protein 90 (Hsp90) by natural products: Geldanamycin, a show case in cancer therapy. Natural Product Reports 30:1299-1323
Kai E (2001) Geldanamycin: The prototype of a class of antitumor drugs targeting the heat shock protein 90 family of molecular chaperones. Cell Stress Chaperones 6(2):105-112
Li YH, Tao PZ, Liu YZ, Jiang JD (2004) Geldanamycin, a ligand of heat shock protein 90, inhibits the replication of herpes simplex virus type 1 in vitro. Antimicrob Agents Chemother.48(3):867-72 PMID 14982777
Taechowisan T, Samsawat T, Puckdee W, Phutdhawong WS (2020) Cytotoxicity activity of Geldanamycin derivatives against various cancer cell lines. J. Appl. Pharm. Sci. 10(06):012-021