Replaces Prod. #: ALX-380-054
Potent antitumor antibiotic. Inhibitor of pp60src tyrosine kinase and of c-myc gene 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). Capable of destabilizing several oncogene and proto-oncogene products. Potent inhibitor of the nuclear hormone receptor family. Protects against α-synuclein toxicity to dopaminergic neurons in Drosophila. Destabilizes mutant p53 protein from a number of breast, leukemic, and prostate cell lines. 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. Hsp90 inhibitors geldanamycin or 17-DMAG reduces the uptake of Chaperone Mediated Autophagy (CMA) substrates by isolated lysosomes.~10-fold more potent than herbimycin A (Prod. No. BML-EI227)
Product Details
| Formula: | C29H40N2O9 |
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| MW: | 560.6 |
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| CAS: | 30562-34-6 |
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| RTECS: | LX8920000 |
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| Purity: | ≥95% (HPLC) |
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| Appearance: | Yellow solid. |
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| Solubility: | Soluble in DMSO (10mg/ml); insoluble in water. |
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| Shipping: | Ambient Temperature |
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| Long Term Storage: | -20°C |
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| Use/Stability: | Stable for at least 1 year after receipt when stored, as supplied, at -20°C. Stock solutions are stable for up to 3 months at -20°C. |
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| Handling: | Protect from light. |
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| Technical Info/Product Notes: | Replacement for ADI-HPK-102 |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
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Full Text
Radicicol induces intracellular accumulation of glycan-deficient clusterin variant: I. Choi, et al.; Biochem. Biophys. Res. Commun.
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Reversing drug resistance of cisplatin by hsp90 inhibitors in human ovarian cancer cells: Z. Zhang, et al.; Int. J. Clin. Exp. Med.
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Full Text
Hsp90-inhibitor geldanamycin abrogates G(2) arrest in p53-negative leukemia cell lines through the depletion of Chk1: K. Sugimoto, et al.; Oncogene
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Geldanamycin enhances hepatocyte growth factor stimulation of eNOS phosphorylation in endothelial cells: K. Makondo, et al.; Eur. J. Pharmacol.
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Geldanamycin interferes with the 90-kDa heat shock protein, affecting lipopolysaccharide-mediated interleukin-1 expression and apoptosis within macrophages: H.Y. Hsu, et al.; Mol. Pharmacol.
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Full Text
Geldanamycin, a heat-shock protein 90-binding agent, induces thymocyte apoptosis through destabilization of Lck in presence of 12-O-tetradecanoylphorbol 13-acetate: K. Ohta, et al.; Biomed. Res.
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Full Text
Geldanamycin, a HSP90 inhibitor, attenuates the hypoxia-induced vascular endothelial growth factor expression in retinal pigment epithelium cells in vitro: W.C. Wu, et al.; Exp. Eye Res.
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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
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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.
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Full Text
Low dose geldanamycin inhibits hepatocyte growth factor and hypoxia-stimulated invasion of cancer cells: F. Koga, et al.; Cell Cycle
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Relationship among ligand conformations in solution, in the solid state, and at the Hsp90 binding site: geldanamycin and radicicol: P. Thepchatri, et al.; JACS
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The heat-shock protein 90 inhibitor, geldanamycin, induces apoptotic cell death in Epstein-Barr virus-positive NK/T-cell lymphoma by Akt down-regulation: Y.K. Jeon, et al.; J. Pathol.
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Inhibition of telomerase activity by geldanamycin and 17-allylamino, 17-demethoxygeldanamycin in human melanoma cells: R. Villa, et al.; Carcinogenesis
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Hsp-90-associated oncoproteins: multiple targets of geldanamycin and its analogs: M.V. Blagosklonny; Leukemia
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Pharmacological prevention of Parkinson disease in Drosophila: P.K. Auluck & N.M. Bonini; Nat. Med.
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Effects of geldanamycin on signaling through activator-protein 1 in hypoxic HT29 human colon adenocarcinoma cells: I.A. Vasilevskaya and P.J. O'Dwyer; Cancer Res.
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Destabilization of Raf-1 by geldanamycin leads to disruption of the Raf-1-MEK-mitogen-activated protein kinase signalling pathway: T.W. Schulte, et al.; Mol. Cell. Biol.
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p185erbB2 binds to GRP94 in vivo. Dissociation of the p185erbB2/GRP94 heterocomplex by benzoquinone ansamycins precedes depletion of p185erbB2: C. Chavany, et al.; J. Biol. Chem.
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Polyubiquitination and proteasomal degradation of the p185c-erbB-2 receptor protein-tyrosine kinase induced by geldanamycin: E.G. Mimnaugh, et al.; J. Biol. Chem.
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Abstract;
Geldanamycin, a new antibiotic: C. DeBoer, et al.; J. Antibiot.
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