Geldanamycin

SKU: orb1300850

Description

Geldanamycin

Research Area

Cancer Biology, Cell Biology, Protein Biochemistry

Key Properties

• CAS Number: 30562-34-6
• MW: 560.7
• Purity: >98%
• Formula: C₂₉H₄₀N₂O₉
• SMILES: [H][C@@]1(C)CC2=C(OC)C(=O)C=C(NC(=O)\C(C)=C/C=C\[C@]([H])(OC)[C@]([H])(OC(N)=O)\C(C)=C/[C@@]([H])(C)C(O)[C@@]([H])(C1)OC)C2=O
• Target: HSP (Heat shock protein)
• Solubility: Soluble in DMSO (up to 50 mg/ml).

Bioactivity

• Target IC50:
  HSP90 (N-terminal domain):0.78 μM(Kd)|HSP90:1.2 μM(Kd)|p185:70 nM
• In Vivo:
  Geldanamycin (50 mg//kg) shows 30% inhibition on pl85-associated phosphotyrosine levels in FRE/erbB-2 mice.
• In Vitro:
  Geldanamycin binds in the ATP-binding site in the N-terminus domain of Hsp90s (residues 1-220). Geldanamycin inhibits the ATPase activity of Hsp90 in a dose-dependent manner. Geldanamycin causes a dose-dependent G2 arrest and reversible inhibiton o f entry into the S phase in A2780 human ovarian cell line. This inhibition is accompanied by p53 increase and finally demonstrated to be p53 dependent. Geldanamycin causes polyubiquitination and proteasomal degradation of the p185 receptor protein-tyrosin kinase and shows a IC50 with 70 nM. [3, 4] Geldanamycin is a typical anti-tumor reagent, shows a mean GI50 with 0.18 μM against the panel of 60 human tumor cell lines.
• Cell Research:
  Exponentially growing cells are treated with Geldanamycin and at various times DNA synthesis is assessed by incorporation of bromodeoxyuridine (BrdUrd) and flow cytometric analysis. No marked difference in total cell number is noted during this time course for treated and untreated cultures. BrdUrd (10 μM) is incorporated over a 4-h incubation period at 37 °C and cells are harvested and fixed in 70% ethanol. After denaturation of the DNA with 2 N HC1, cells are incubated with an anti-BrdUrd mouse monoclonal antibody followed by a fluorescein isothiocyanate (FITC)-linked goat anti-mouse IgG. Cells are stained for 30 minutes at room temperature with propidium iodide and analysed by flow cytometry using a Coulter EPICS Profile Analyzer. (Only for Reference)

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

NSC 122750; U-29135

Compound Identifiers

PubChem CID

71307093