NVP-BEP800

NVP-BEP800 is an inhibitor of heat shock protein 90 (Hsp90; IC₅₀ = 58 nM for recombinant human Hsp90β).¹ It is selective for Hsp90 over the chaperones GRP94 and TRAP1 (IC₅₀s = 4.1 and 5.5 µM, respectively). NVP-BEP800 inhibits the growth of BT474, SK-BR-3, MCF-7, MDA-MB-157, MDA-MB-231, MDA-MB-468, and BT-20 breast cancer cells (GI₅₀s = 53, 56, 118, 89, 190, 173, and 162 nM, respectively). It reduces levels of the Hsp90 target proteins HER2 and Raf-1 in MCF-7 cells. NVP-BEP800 induces apoptosis and attenuates X-ray-induced increases in Hsp70 levels in T98G glioblastoma cells.² NVP-BEP800 (15-50 mg/kg) reduces tumor volume in A375 melanoma and BT474 breast cancer mouse xenograft models.¹ It also reduces tumor volume in an L1T2 Kaposi sarcoma mouse xenograft model.³

WARNING This product is not for human or veterinary use.

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. Mol. Cancer Ther. 9(4), 906-919 (2010).

2. 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).

3. 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 Pathog. 8, (2012).