| Name | Onalespib |
| Description | Onalespib (AT13387) is a synthetic, orally bioavailable, small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity. Onalespib selectively binds to Hsp90, thereby inhibiting its chaperone function and promoting the degradation of oncogenic signaling proteins involved in tumor cell proliferation and survival. Hsp90, a chaperone protein upregulated in a variety of tumor cells, regulates the folding, stability and degradation of many oncogenic signaling proteins. |
| Cell Research | The human cell lines including A375, 22RV1, T474, DU1 45, LNCa P, MCF-7, DA-MB-468 are seeded into 96-well plates before the addition of AT13387 in 0.1% (v/v) DMSO. GI50 are determined using a 10-point dose response curve for three cell doubling times. After AT13387 incubation 10% (v/v), Alamar blueis added, and cells are incubated for a further 4 hours. Fluorescence is read.(Only for Reference) |
| Kinase Assay | HSP90 competition isothermal calorimetry: Kd values for AT13387 binding to HSP90 are determined with a competition Isothermal Calorimetry (ITC) format. ITC experiments are performed on a Micro Cal VP-ITC at 25 °C in a buffer comprising 25 mM Tris, 100 mM NaCl, 1 mM MgCl2 and 1 mM Tris(2-carboxy- ethyl)phosphine at pH 7.4 in order to maintain the higher affinit |
| In vitro | AT13387 is a potent inhibitor of the proliferation and survival of many different cell lines from a wide range of different tumor types (e.g., MES-SA cell line). In a panel of 30 tumor cell lines, AT13387 effectively inhibited cell proliferation with GI50 values in the range of 13-260 nM. AT13387 inhibited the proliferation of the non-tumorigenic human prostate epithelial cell line PNT2 with a GI50 value of 480 nM. |
| In vivo | AT13387 is a potent inhibitor of the proliferation and survival of many different cell lines from a wide range of different tumor types (e.g., MES-SA cell line). In a panel of 30 tumor cell lines, AT13387 effectively inhibited cell proliferation with GI50 values in the range of 13-260 nM. AT13387 inhibited the proliferation of the non-tumorigenic human prostate epithelial cell line PNT2 with a GI50 value of 480 nM. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 2.04 mg/mL (4.98 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1 mg/mL (2.44 mM), Sonication is recommended.
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| Keywords | Onalespib | Inhibitor | inhibit | HSP90 | HSP | Heat shock proteins | AT-13387 | AT 13387 |
| Inhibitors Related | Ethoxyquin | Adezmapimod | Tamoxifen | Palmitic acid sodium | Mequinol | 7-Aminocephalosporanic acid | Benzbromarone | Elesclomol | Rifabutin | Palmitic acid | Tamoxifen Citrate | Isoxazole |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | ReFRAME Related Library | Anti-Cancer Clinical Compound Library | Anti-Viral Compound Library | Drug Repurposing Compound Library | Inhibitor Library | NO PAINS Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
United States
