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Geldanamycin

HSP90 inhibitor
 
BML-EI280-0001 1 mg 95.00 USD
 
BML-EI280-0005 5 mg 410.00 USD
Do you need bulk/larger quantities?
 
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 Specification

Formula:C29H40N2O9
 
MW:560.6
 
CAS:30562-34-6
 
RTECS:LX8920000
 
Purity:≥95% (HPLC)
 
Appearance:Yellow solid.
 
Solubility:Soluble in DMSO (10mg/ml); insoluble in water.
 
Shipping:Ambient
 
Long Term Storage:-20°C
 
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.
 
Handling:Protect from light.
 
Technical Info/Product Notes:Replacement for ADI-HPK-102
 
ALX-380-054
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ALX-380-054

Product Literature References

Elevated Serum Antibody Levels against Cyclin L2 in Patients with Esophageal Squamous Cell Carcinoma: H. Shimada, et al.; J. Cancer Sci. Ther. 7, 60 (2015), Application(s): Cell Culture, Full Text
Radicicol induces intracellular accumulation of glycan-deficient clusterin variant: I. Choi, et al.; Biochem. Biophys. Res. Commun. 458, 555 (2015), Application(s): Cell Culture, Abstract;
Reversing drug resistance of cisplatin by hsp90 inhibitors in human ovarian cancer cells: Z. Zhang, et al.; Int. J. Clin. Exp. Med. 8, 6687 (2015), Application(s): Cell Culture, Abstract; 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 27, 3091 (2008), Abstract;
Geldanamycin enhances hepatocyte growth factor stimulation of eNOS phosphorylation in endothelial cells: K. Makondo, et al.; Eur. J. Pharmacol. 582, 110 (2007), Abstract;
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. 71, 344 (2007), Abstract; 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. 28, 33 (2007), Abstract; 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. 85, 721 (2007), Abstract;
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), Abstract;
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), Abstract; Full Text
Low dose geldanamycin inhibits hepatocyte growth factor and hypoxia-stimulated invasion of cancer cells: F. Koga, et al.; Cell Cycle 6, 1393 (2007), Abstract;
Relationship among ligand conformations in solution, in the solid state, and at the Hsp90 binding site: geldanamycin and radicicol: P. Thepchatri, et al.; JACS 129, 3127 (2007), Abstract;
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. 213, 170 (2007), Abstract;
Chaperoning oncogenes: HSP90 as a target of geldanamycin: L. Neckers; Handb. Exp. Pharmacol. 172, 259 (2006), (Review), Abstract;
Inhibition of telomerase activity by geldanamycin and 17-allylamino, 17-demethoxygeldanamycin in human melanoma cells: R. Villa, et al.; Carcinogenesis 24, 851 (2003), Abstract;
Hsp-90-associated oncoproteins: multiple targets of geldanamycin and its analogs: M.V. Blagosklonny; Leukemia 16, 455 (2002), (Review), Abstract;
Pharmacological prevention of Parkinson disease in Drosophila: P.K. Auluck & N.M. Bonini; Nat. Med. 8, 1185 (2002), Abstract;
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. 59, 3935 (1999), Abstract;
Geldanamycin as a potential anti-cancer agent: its molecular target and biochemical activity: L. Neckers, et al.; Invest. New Drugs 17, 361 (1999), (Review), Abstract;
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. 16, 5839 (1996), Abstract;
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. 271, 4974 (1996), Abstract; Full Text
Polyubiquitination and proteasomal degradation of the p185c-erbB-2 receptor protein-tyrosine kinase induced by geldanamycin: E.G. Mimnaugh, et al.; J. Biol. Chem. 271, 22796 (1996), Abstract;
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), Abstract;
Geldanamycin selectively destabilizes and conformationally alters mutated p53: M.V. Blagosklonny, et al.; Oncogene 11, 933 (1995), Abstract;
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), Abstract;
Inhibition of heat shock protein HSP90-pp60v-src heteroprotein complex formation by benzoquinone ansamycins: essential role for stress proteins in oncogenic transformation: L. Whitesell, et al.; PNAS 91, 8324 (1994), Abstract;
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), Abstract;
Phenotypic change from transformed to normal induced by benzoquinonoid ansamycins accompanies inactivation of p60src in rat kidney cells infected with Rous sarcoma virus: Y. Uehara, et al.; Mol. Cell. Biol. 6, 2198 (1986), Abstract;
Geldanamycin, a new antibiotic: C. DeBoer, et al.; J. Antibiot. 23, 442 (1970), Abstract;

Related Products

Herbimycin A 

Tyrosine kinase inhibitor
70563-58-5, ≥98% (HPLC) | Print as PDF
 
BML-EI227-0100 100 µg 158.00 USD
 
BML-EI227-1000 1 mg 904.00 USD
Do you need bulk/larger quantities?
 

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