Geldanamycin

Product details

• Chemical name: 17-Demethoxy-17-(2-propenylamino) geldanamycin.
• Also known as: Geldanomycin, U-29135
• CAS number: 30562-34-6
• Molecular formula: C29H40N2O9.
• Purity: >99%
• Concentration: 100 nM - 1 µM.
• Form: Lyophilized powder.
• Solubility: DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
• Reconstitution: DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
• Shipping: Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
• Source: Natural
• Activity: Geldanamycin is a potent antitumor antibiotic1 active against more than 50 tumor cell lines2. It binds to the ATPase binding pocket in Hsp903,4 and induces the degradation of proteins required by this chaperone.
• Alternative names: Geldanomycin, U-29135

Scientific background

Geldanamycin is a potent antitumor antibiotic1 active against more than 50 tumor cell lines.2 Hsp90 is a molecular chaperone that regulates the folding, assembly and conformational maturation of proteins. It has a key role in cell response to environmental stress and in maintaining the malignant phenotype of tumor cells.3Geldanamycin binds into the ATPase binding pocket in Hsp90,4,5 and induces the degradation of proteins required by this chaparone to induce conformational maturation. Hsp90 client proteins include transcription factors (mutated p53, HIF-1a, EF-2),6,7 tyrosine kinases (v-Src, Bcr-Abl, erbB2),8,9 serine-threonine kinases (Raf-1),10,11 and the nuclear receptor family (androgen, estrogen).12 Hsp90 client proteins play important roles in the regulation of the cell cycle, cell growth, apoptosis, and oncogenesis, geldanamycin inhibits the proliferation of cultured cancer cells and shows anticancer activity in experimental animals.The antitumor effects involve different mechanisms such as destabilization of mutant p53 protein (breast and prostate cell lines)13 cell cycle arrest,13 inhibition of c-Jun expression,14 destabilization of Raf-1, destruction of EF-2 kinase, and inhibition of telomerase activity.15 Recently, synergistic effects of Geldanamycin with cytotoxic drugs16,17 increased tumor cell sensitivity to radiation.18,19

Lead time: 1-2 Business Days

Country of origin: Israel/IL

Applications key

Application key: FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay.

Bioassay tested: Yes

• SDS (PDF)

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