NCT-58

NCT-58 is an inhibitor of heat shock protein 90 (Hsp90).^1,2 It binds to the C-terminal domain of Hsp90α and inhibits the protein-protein interaction between the Hsp90α C-terminal domain and peptidylprolyl isomerase D (PPID), a co-chaperone. It decreases cell viability and induces apoptosis in HER2-positive BT474 and SK-BR-3 human breast cancer cells when used at concentrations ranging from 0.5 to 20 µM.¹ NCT-58 (10 µM) reduces mammosphere formation by, as well as heat shock factor 1 (Hsf1), Hsp70, and Hsp90 protein levels in, BT474 cells. It also reduces intratumoral levels of HER2 and the intracellular domain of HER2 (ICD-HER2), as well as reduces tumor growth and angiogenesis, in a trastuzumab-resistant JIMT-1 breast cancer mouse xenograft model when administered at a concentration of 30 mg/kg.

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1. Park, S., Kim, Y.-J., Park, J.M., et al. The C-terminal HSP90 inhibitor NCT-58 kills trastuzumab-resistant breast cancer stem-like cells. Cell Death Discov. 7(1), 354 (2021).

2. Nguyen, C.-T., Ann, J., Sahu, R., et al. Discovery of novel anti-breast cancer agents derived from deguelin as inhibitors of heat shock protein 90 (HSP90). Bioorg. Med. Chem. Lett. 30(17), 127374 (2020).