2231079-74-4

NCT-505 is an Orally Bioavailable aldehyde Dehydrogenase 1A1 (ALDH1A1) Inhibitor with Potent Cellular Activity (IC50 = 7 nM). NCT-505 demonstrated target engagement in a cellular thermal shift assay (CETSA), inhibited the formation of 3D spheroid cultures of OV-90 cancer cells, and potentiated the cytotoxicity of paclitaxel in SKOV-3-TR, a paclitaxel resistant ovarian cancer cell line. NCT-505 also exhibit high specificity over other ALDH isozymes and unrelated dehydrogenases.

NCT-505 is a potent and selective aldehyde dehydrogenase (ALDH1A1) inhibitor, with an IC50 of 7 nM, and weakly inhibits hALDH1A2, hALDH1A3, hALDH2, hALDH3A1 (IC50s, >57, 22.8, 20.1, >57 μM).

ALDH1

[1] Yang SM, et al. Discovery of Orally Bioavailable, Quinoline-Based Aldehyde Dehydrogenase 1A1 (ALDH1A1) Inhibitors with Potent Cellular Activity. J Med Chem. 2018 Jun 14;61(11):4883-4903. DOI:10.1021/acs.jmedchem.8b00270