NVP-BEP800 (CAS 847559-80-2)
QUICK LINKS
NVP-BEP800 is an ATP-competitive inhibitor of Hsp90β (IC50 of 58 nM). NVP-BEP800 exhibits selectivity (>70-fold) against Hsp90 family members Grp94 (IC50 of 4.1 μM) and Trap-1 (IC50 of 5.5 μM). NVP-BEP800 does not inhibit the closely related GHKL ATPase, topoisomerase II, and the structurally unrelated ATPase, Hsp70 at the concentration of 10 μM. NVP-BEP800 is a potent inhibitor of the proliferation of various tumor cell lines including A375 (GI50 of 38 nM) and PC3 (GI50 of 1.05 μM), and primary human tumors (IC50 of 0.75 μM and IC70 of 1.8 μM). NVP-BEP800 treatment at the concentration of five times the GI50 increases the percentage of G2-M phase in A2058 (29.5%) and A549 (33.6%) cells and sub-G1 phase in BT-474 (42.7%), HCT116 (12.1%), A2058 (5.9%) and A549 (7.1%) cells. NVP-BEP800 treatment causes Akt (IC50 of 218 nM) and ErbB2 (IC50 of 39.5 nM) dephosphorylation, ErbB2 degradation (IC50 of 137 nM), and Hsp70 induction (IC50 of 207 nM) in a concentration-dependent manner in BT-474 cells.
NVP-BEP800 (CAS 847559-80-2) References
- Anti-myeloma activity of the novel 2-aminothienopyrimidine Hsp90 inhibitor NVP-BEP800. | Stühmer, T., et al. 2009. Br J Haematol. 147: 319-27. PMID: 19686236
- Preclinical antitumor activity of the orally available heat shock protein 90 inhibitor NVP-BEP800. | Massey, AJ., et al. 2010. Mol Cancer Ther. 9: 906-19. PMID: 20371713
- Novel HSP90 inhibitors, NVP-AUY922 and NVP-BEP800, radiosensitise tumour cells through cell-cycle impairment, increased DNA damage and repair protraction. | Stingl, L., et al. 2010. Br J Cancer. 102: 1578-91. PMID: 20502461
- Hsp90 Inhibitors NVP-AUY922 and NVP-BEP800 May Exert a Significant Radiosensitization on Tumor Cells along with a Cell Type-Specific Cytotoxicity. | Niewidok, N., et al. 2012. Transl Oncol. 5: 356-69. PMID: 23066444
- Hsp90 inhibition by NVP-AUY922 and NVP-BEP800 decreases migration and invasion of irradiated normoxic and hypoxic tumor cell lines. | Hartmann, S., et al. 2013. Cancer Lett. 331: 200-10. PMID: 23340178
- 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. | Wu, J., et al. 2014. Exp Ther Med. 8: 893-898. PMID: 25120620
- Hsp90β promoted endothelial cell-dependent tumor angiogenesis in hepatocellular carcinoma. | Meng, J., et al. 2017. Mol Cancer. 16: 72. PMID: 28359326
- HSP90 inhibitor NVP-BEP800 affects stability of SRC kinases and growth of T-cell and B-cell acute lymphoblastic leukemias. | Mshaik, R., et al. 2021. Blood Cancer J. 11: 61. PMID: 33737511
- DUSP4 promotes esophageal squamous cell carcinoma progression by dephosphorylating HSP90β. | Zhou, L., et al. 2023. Cell Rep. 42: 112445. PMID: 37141098
- Using ChEMBL to Complement Schistosome Drug Discovery. | Padalino, G., et al. 2023. Pharmaceutics. 15: PMID: 37242601
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
NVP-BEP800, 10 mg | sc-364552 | 10 mg | $480.00 | |||
NVP-BEP800, 50 mg | sc-364552A | 50 mg | $1455.00 |