Cell Signaling Technology

Product Pathways - Protein Folding

Geldanamycin #9843

Molecular Formula:
C29H40N2O9
Molecular Weight:
560.64 g/mol
Purity:
>99%

Directions for Use

Geldanamycin is supplied as 600 μg powder. Store at or below -20ºC. Before usage, dissolve the chemical in 1.08 ml DMSO to make 1 mM Geldanamycin. For working concentrations of 300 nM-1 μM, dilute 1:3000 to 1:1000. Treat cells with the desired concentration for 20-48 hours. Store liquid form at or below -20ºC.

Note: Geldanamycin is not stable in liquid form (quality decreased in 1-2 weeks). Use freshly dissolved geldanamycin each time.

Western Blotting

Western Blotting

Western blot analysis of extracts from HEK293 cells, untreated or treated with indicated concentrations of Geldanamycin for 20 hours, using IKKα Antibody #2682 showing IKKα degradation (upper). β-Actin Antibody #4967 was used as a loading control (lower).

Structure

Structure

Structure of Geldanamycin

Background

Geldanamycin (GA) is a naturally existing HSP90 inhibitor that belongs to the benzoquinone ansamycin family. GA binds to the amino terminal ATP-binding pocket of HSP90 and inhibits ATP binding and hydrolysis. HSP90 is a chaperone interacting with a wide variety of important target proteins for cell signaling and regulation during tumorgenesis (1,2). The binding of GA to HSP90 interferes with HSP-mediated target protein folding, leading to target aggregation and degradation (1-3). GA and its synthetic derivatives show higher affinity to HSP90 in tumor cells as compared to normal tissues and constitute a class of protential antitumor drugs (2-3).

  1. Ochel, H.J. et al. (2001) Cell Stress Chaperones 6, 105-112.
  2. Sharp, S. and Workman, P. (2006) Adv.Cancer Res. 95, 323-348.
  3. Kamal, A. et al. (2003) Nature 425, 407-410.

Application References

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Companion Products

For Research Use Only. Not For Use In Diagnostic Procedures.

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