| 货号 | 18383-500ug |
| 描述 | Heat shock protein 90 (Hsp90) isoforms are molecular chaperones that modulate intracellular signaling and protein folding, trafficking, and turnover. Inhibitors of Hsp90, such as geldanamycin (Item No. 13355), have shown promise as anti-tumor agents. NVP-BEP800 is a potent inhibitor of Hsp90β (IC50 = 58 nM) that is 70-fold less effective against two related Hsps, Grp94 (Hsp90B1) and Trap-1 (Hsp75).1 It is without effect (IC50 > 10 µM) against a panel of twenty kinases.1 NVP-BEP800 causes p23/Hsp90 dissociation and client protein degradation, which leads to growth inhibition (GI50s from 53 to 190 nM) or induction of cell death in cancer cell lines.1 It is orally available and has antitumor effects in human tumor xenografts in mice.1 Hsp90 inhibitors, including NVP-BEP800, increase the sensitivity of tumor cells to ionizing radiation.2,3,4 They also direct the proteasomal degradation of viral Hsp90 client proteins, including those required for latency and infectivity of Kaposi sarcoma-associated herpes virus.5 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Massey, A.J.,Schoepfer, J.,Brough, P.A., et al. Preclinical antitumor activity of the orally available heat shock protein 90 inhibitor NVP-BEP800. Molecular Cancer Therapeutics 9(4), 906-919 (2010). 2.Stingl, L.,Stühmer, T.,Chatterjee, M., et al. Novel HSP90 inhibitors, NVP-AUY922 and NVP-BEP800, radiosensitise tumour cells through cell-cycle impairment, increased DNA damage and repair protraction. British Journal of Cancer 102(11), 1578-1591 (2010). 3.Niewidok, N.,Wack, L.J.,Schiessl, S., et al. Hsp90 inhibitors NVP-AUY922 and NVP-BEP800 may exert a significant radiosensitization on tumor cells along with a cell type-specific cytotoxicity. Transl.Oncol. 5(5), 356-369 (2012). 4.Wu, J.,Wang, W.,Shao, Q., et al. Irradiation facilitates the inhibitory effect of the heat shock protein 90 inhibitor NVP-BEP800 on the proliferation of malignant glioblastoma cells through attenuation of the upregulation of heat shock protein 70. Exp.Ther.Med. 8(3), 893-898 (2014). 5.Chen, W.,Sin, S.H.,Wen, K.W., et al. Hsp90 inhibitors are efficacious against Kaposi Sarcoma by enhancing the degradation of the essential viral gene LANA, of the viral co-receptor EphA2 as well as other client proteins. PLoS Pathogens 8, (2012). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 480.4 |
| 分子式 | C21H23Cl2N5O2S |
| CAS号 | 847559-80-2 |
| 稳定性 | ≥ 2 years |
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