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NSC122750; BRN1633093; U-29135

Chemical

C29H40N2O9

560.6

30562-34-6

LX8920000

Isolated from Streptomyces hygroscopicus.

≥98% (HPLC)

Yellow solid.

Soluble in methanol or DMSO; insoluble in water.

Determined by 1H-NMR.

Manufactured by BioViotica.

QTQAWLPCGQOSGP-GAEFGYQESA-N

AMBIENT

+4°C

-20°C

Protect from light when in solution.

Stable for at least 1 year after receipt when stored at -20°C.After reconstitution protect from light at -20°C.

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• Antibiotic.
• Potent antitumor compound.
• pp60src tyrosine kinase inhibitor.
• Inhibits c-mycgene expression in murine lymphoblastoma cells.
• Inhibits the transforming activity of abl, erbB, fps, src and yes.
• Binds specifically to heat shock protein 90 (HSP90) and to its endoplasmic reticulum homolog GP96 (GRP94).
• Destabilizes several oncogene and proto-oncogene products.
• Potent nuclear hormone receptor family inhibitor.

Product References

Geldanamycin, a new antibiotic: C. DeBoer, et al.; J. Antibiot. 23, 442 (1970)

Inhibition of c-myc gene expression in murine lymphoblastoma cells by geldanamycin and herbimycin, antibiotics of benzoquinoid ansamycin group: H. Yamaki, et al.; J. Antibiot. 42, 604 (1989)

Geldanamycin selectively destabilizes and conformationally alters mutated p53: M.V. Blagosklonny, et al.; Oncogene 11, 933 (1995)

Inhibition of the oncogene product p185erbB-2 in vitro and in vivo by geldanamycin and dihydrogeldanamycin derivatives: R.C. Schnur, et al.; J. Med. Chem. 38, 3806 (1995)

Stable and specific binding of heat shock protein 90 by geldanamycin disrupts glucocorticoid receptor function in intact cells: L. Whitesell & P. Cook; Mol. Endocrinol. 10, 705 (1996)

Geldanamycin as a potential anti-cancer agent: its molecular target and biochemical activity: L. Neckers, et al.; Invest. New Drugs 17, 361 (1999), (Review)

Hsp-90-associated oncoproteins: multiple targets of geldanamycin and its analogs: M.V. Blagosklonny; Leukemia 16, 455 (2002), (Review)

Geldanamycin enhances hepatocyte growth factor stimulation of eNOS phosphorylation in endothelial cells: K. Makondo, et al.; Eur. J. Pharmacol. 582, 110 (2007)

HSP90 antagonist, geldanamycin, inhibits proliferation, induces apoptosis and blocks migration of rhabdomyosarcoma cells in vitro and seeding into bone marrow in vivo: E. Lesko, et al.; Anticancer Drugs 18, 1173 (2007)

Inhibition of heat shock protein 90 impairs epidermal growth factor-mediated signaling in gastric cancer cells and reduces tumor growth and vascularization in vivo: S.A. Lang, et al.; Mol. Cancer Ther. 6, 1123 (2007)

Low dose geldanamycin inhibits hepatocyte growth factor and hypoxia-stimulated invasion of cancer cells: F. Koga, et al.; Cell Cycle 6, 1393 (2007)

Hsp90-inhibitor geldanamycin abrogates G(2) arrest in p53-negative leukemia cell lines through the depletion of Chk1: K. Sugimoto, et al.; Oncogene 27, 3091 (2008)

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