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Streptomyces hygroscopicus
C29H40N2O9
M.W.: 560.6
Purity (TLC): >99%
Melting Point: 260~262℃
Soluble in DMSO.
Geldanamycin is a benzoquinone ansamycin antibiotic which
binds to Hsp90 (Heat Shock Protein 90) and alters it function. Hsp90 is a
highly conserved and very abundant protein in the cytosol of both
eukaryotic and prokaryotic cells. Hsp90 plays a key role in regulating the
physiology of cells exposed to environmental stress and in maintaining the
malignant phenotype of tumor cells. HSP90 client proteins play important
roles in the regulation of the cell cycle, cell growth, cell survival,
apoptosis, and oncogenesis. Geldanamycin binds with a high affinity into
the ATP binding pocket in Hsp90 and induces the degradation of proteins
that require this chaperone for conformational maturation.
Whitsell, L., P.D. Sutphin, A.D. Lewis, P. Workman.,
Geldanamycin-Induced Association of Multiple Molecular Chaperone Proteins
with Mutant p53 is Altered by Geldanamycin, an hsp90-Binding Agent.,
1998., 18(3):, 1517-1524., 2. Lawson, B., J.W. Brewer, L.M Hendershot..
Gelanamycin, an hsp90/GRP94-Binding Drug, Induces Increased Transcription
of Endoplasmic Reticulum (ER) Chaperones Via the ER Stress Pathway.,
Journal of Cellular Physiology., 1998., 174(2):, 170-178., 3. Joly, G.A.,
M. Ayres, R.G. Kilbourn..
Potent Inhibition of Inducible Nitric Oxide Synthase by Geldanamycin, A
Tyrosine Kinase Inhibitor, in Endothelial, Smoothe Muscle Cells, and in
Rat Aorta., FEBS Letters., 1997., 403(1):, 40-44., 4. Schulte, T.W., M.V.
Blagosklonny, L. Romanova, J.F. Mushinski, B.P. Monia, J.F. Johnston..
Destabilization of Raf-1 by Geldanamycin Leads to Disruption of the
Raf-1-MEK-Mitogen-Activated Protein Kinase Signalling Pathway., Molecular
and Cellular Biology., 1996., 16(10):, 5839-5845..
Store at -20℃
Handling: Store in Tightly Sealed Vial. Protect from Light. |
1mg |
5250.- |