NVP-BEP800

NVP-BEP800 is an orally bioavailable, ATP-competitive small molecule inhibitor of Heat Shock Protein 90 (HSP90), with a high degree of selectivity for the HSP90β isoform. Developed by Novartis, it belongs to the 2-aminothieno[2,3-d]pyrimidine chemical class. The drug functions by binding to the N-terminal ATP-binding pocket of the HSP90 chaperone, which leads to the dissociation and subsequent proteasomal degradation of various oncogenic client proteins. Key clients affected by NVP-BEP800 include SRC family kinases (such as LCK in T-cell acute lymphoblastic leukemia and LYN in B-cell acute lymphoblastic leukemia) and IKKβ. Preclinical studies have demonstrated that NVP-BEP800 inhibits the growth and induces apoptosis in multiple cancer models, including acute lymphoblastic leukemia (ALL), glioblastoma, breast cancer, and multiple myeloma. It has also shown synergistic effects when combined with ionizing radiation by attenuating the compensatory upregulation of HSP70.

Other names

BEP-800BEP800BEP 800