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Ganetespib

Manufactured by Adooq

Ganetespib is a synthetic inhibitor of the heat shock protein 90 (Hsp90) molecular chaperone. Hsp90 is involved in the folding and stabilization of various client proteins, including those implicated in cancer cell growth and survival. Ganetespib binds to the N-terminal domain of Hsp90, disrupting its chaperone function and leading to the degradation of Hsp90 client proteins.

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2 protocols using ganetespib

1

Evaluating USP22 in Tumor Growth

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Immunodeficient SCID mice were housed in a controlled, germ-free environment. Animals were randomized into treatment groups and anesthetized by isoflurane inhalation (2–3%, Forene) and HCT116 USP22+/+ and USP22−/− cells (1.0 × 106 cells in Corning® Matrigel®) were injected subcutaneously into the left and right flank, respectively, using a 0.3 ml Micro-Fine syringe (BD Bioscience). The bodyweight, as well as the size of the growing tumors, were monitored daily. After the tumors reached a volume of approximately 100 mm³, 25 mg/kg Ganetespib (AdooQ) or vehicle solution (10% DMSO (v/v), 20% (v/v) pre-warmed Cremophor RH40 (55 °C; Sigma-Aldrich), 5% (w/v) dextrose) was injected i.v. for three consecutive days and after 4 days break, for 3 further days. Experiments were performed with six replicates per group in order to assure reproducibility. Experiments were performed blinded during tumor size measurement and subsequent immunohistochemical staining.
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2

Evaluating Small Molecule Inhibitors

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Where indicated, lenalidomide (Sigma), pomalidomide (Selleckchem), thalidomide (Tocris), BCH (Sigma), JPH-203 (Tocris), 17-AAG (Selleckchem), Geldanamycin, Ganetespib, HSP990, SNX-4112, PU-H71 (all AdooQ Bioscience) were used at the indicated concentrations.
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