D5193
17-Dimethylaminoethylamino-17-demethoxygeldanamycin
Synonym(s):
17-DMAG
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About This Item
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biological source
synthetic
Quality Level
form
powder
color
dark red-purple to black
solubility
ethanol: ~10 mg/mL (lit.)
DMSO: >25 mg/mL (lit.)
antibiotic activity spectrum
neoplastics
Mode of action
protein synthesis | interferes
storage temp.
−20°C
General description
Chemical structure: benzenoid
Application
17-DMAG has been used to block the NF-κB inflammatory cascade in the murine model. It a potential therapeutic agent for non-small-cell lung cancers (NSCLC).
Biochem/physiol Actions
17-DMAG is a heat shock protein (HSP90) inhibitor. 17-DMAG is a more potent analog of geldanamycin. It inhibits cancer growth and promotes apoptosis in multiple cell lines. 17-DMAG is a more potent antitumor agent than 17-AAG.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
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Lung cancer (Amsterdam, Netherlands), 75(2), 161-166 (2011-07-20)
Acquired resistance to epidermal growth factor receptor-tyrosine kinase inhibitors (EGFR-TKIs), gefitinib and erlotinib, is frequently observed after initiation of TKIs therapy. Non-small-cell lung cancers (NSCLC) with activating EGFR mutations were reported to be sensitive to heat shock protein 90 (Hsp90)
HSP90 inhibition by 17-DMAG reduces inflammation in J774 macrophages through suppression of Akt and nuclear factor-κB pathways.
Inflammation Research, epub (2012)
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