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 |