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NVP-AUY922
- VER 52296 - Luminespib- Soluble in DMSO
- MF: C26H31N3O5
- MW: 465.54
Description
NVP-AUY922 (Luminespib, VER52296) is a highly potent Hsp90 inhibitor with reported IC50 value of 21 nM in an Hsp90 fluorescence polarization binding assay.
Hsp90 stabilizes many oncogenic client proteins, including receptor tyrosine kinases and signaling kinases. NVP-AUY922 is useful for probing proteostasis stress, client-protein degradation and Hsp90-dependent survival pathways in cancer models.
Key Features
- Potent inhibitor of heat shock protein 90
- Reported IC50: 21 nM in Hsp90 FP binding assay
- Destabilizes Hsp90 client proteins involved in oncogenic signaling
- Useful for proteostasis and chaperone-dependence studies
Applications
- Hsp90 inhibitor pharmacology
- Oncogenic client-protein degradation research
- Proteostasis and stress-response studies
- Cancer cell survival assays
More Information
| Parent CAS No. | 747412-49-3 |
|---|---|
| Chemical Name | 5-(2,4-Dihydroxy-5-isopropyl-phenyl)-4-(4-morpholin-4-ylmethyl-phenyl)-isoxazole-3-carboxylic acid ethylamide |
| SMILES | C1(O)C(C(C)C)=CC(C2=C(C3C=CC(CN4CCOCC4)=CC=3)C(C(NCC)=O)=NO2)=C(O)C=1 |
| MFCD | MFCD14635361 |
| InChi | InChI=1S/C26H31N3O5/c1-4-27-26(32)24-23(18-7-5-17(6-8-18)15-29-9-11-33-12-10-29)25(34-28-24)20-13-19(16(2)3)21(30)14-22(20)31/h5-8,13-14,16,30-31H,4,9-12,15H2,1-3H3,(H,27,32) |
| InChiKey | NDAZATDQFDPQBD-UHFFFAOYSA-N |
| CID | 135539077 |
| Short Description | Hsp90 inhibitor |
References
- MR Jensen et al. NVP-AUY922: a small molecule HSP90 inhibitor with potent antitumor activity in preclinical breast cancer models. Breast Cancer Res. 2008, 10, R33.
- SA Eccles et al. NVP-AUY922: A Novel Heat Shock Protein 90 Inhibitor Active against Xenograft Tumor Growth, Angiogenesis, and Metastasis. Cancer Res. 2008, 68, 2850.
- PA Brough et al. 4,5-Diarylisoxazole Hsp90 Chaperone Inhibitors: Potential Therapeutic Agents for the Treatment of Cancer. J. Med. Chem., 2008, 51 (2), pp 196–218.
- T Taldone et al. Targeting Hsp90: small-molecule inhibitors and their clinical development. Cur. Opin. Pharmacol. 2008, 8(4), 370-374.
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