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Product Name
Geldanamycin
Catalog #
SIH-111B
Size
5mg
Type
Inhibitor
Description
Hsp90 inhibitor
Research Area
Heat Shock
CAS Number
30562-34-6
Formula
C29H40N2O10
Molecular weight
561.6
Source/Host
Produced by fermentation
Purity
›95%
Solubility
Slightly soluble in methanol, chloroform or DMSO (10mg/mL); insoluble in water
Appearance
Yellow Solid
Storage Temp
-20°C
Shipping Temp
Blue Ice or 4°C
Safety Phrases
Classification: Harmful. May be harmful if inhaled, swallowed or absorbed through skin.

Safety Phrases: S22 - Do not breathe dust
S24/25 - Avoid contact with skin and eyes
S36/37/39 - Wear suitable protective clothing, gloves and eye/face protection

Risk Phrases: R68- Possible risk of irreversible effects Hazard Phrases: Precautionary Phrases:
Datasheet
SIH 111 Geldanamycin Heat Shock Inhibitor
Price
$345.00 USD Add to Cart

Structure of Geldanamycin
Research Background
Geldanamycin is a benzoquinoid ansamycin produced by Streptomyces hygroscopicus. It binds specifically to heat shock protein HSP90 and downregulates target proteins including tyrosine kinases, steroid receptors, transcription factors and cell cycle regulatory kinases (1,2). It induces the inactivation, destabilization and eventual degradation of HIF-1α (3). It is also an inhibitor of pp60src tyrosine kinase and of c-myc gene expression in murine lymphoblastoma cells. It inhibits the transforming activity of abl, erbB, fps, src, and yes (4). Geldanamycin is capable of destabilizing several oncogene and proto-oncogene products; it is a potent inhibitor of the nuclear hormone receptor family (5). It protects against α-synuclein toxicity to dopaminergic neurons in Drosophila, and destabilizes mutant p53 protein from a number of breast, leukemic, and prostate cell lines (6). Inhibits basal and hypoxia-induced expression of c-Jun (IC50=75nM) and abolishes hypoxia-induced increase in c-Jun N-terminal kinase (JNK) activity. Inhibits telomerase activity through inhibition of HSP90, a chaperone required for the assembly and activation of telomerase in human cells (6). It is ~10-fold more potent than herbimycin A.
References
1. Whitesell L., et al. (1994) Proc. Natl. Acad. Sci. USA 91:8324.
2. Neckers L. (2002) Trends Mol. Med. 8: S55.
3. Mabjeesh N.J., et al. (2002) Cancer Res. 62: 2478.
4. Chavany C., et al. 1996) Amer. Society Biochem Mol Bio. 9: 4974-4977.
5. Villa R., et al. (2003) Carcinogenesis. 24(5): 851-9.
6. Yamaki H., Iguchi-Ariga S.M., and Ariga H. (1989) J Antibiot (Tokyo) 42(4): 604-10.
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