hsp990

HSP990 is an orally bioavailable, synthetic small molecule inhibitor of heat shock protein 90 (Hsp90), specifically targeting the ATP-binding site in the N-terminal domain of Hsp90. By inhibiting Hsp90, HSP990 leads to the proteasomal degradation of oncogenic client proteins—including HER2/ERBB2 and c-Met—resulting in inhibition of tumor cell proliferation and growth. It exhibits potent activity against both Hsp90α and Hsp90β isoforms with single-digit nanomolar IC50 values. Preclinical studies have demonstrated antitumor effects across various cancer models dependent on Hsp90 client proteins, as well as potential neuroprotective and antiepileptic effects in animal models of epilepsy and Alzheimer's disease. The drug was developed by Novartis in collaboration with Vernalis for oncology indications[1][2][3][4][5][6].

Other names

heat-shock protein 990