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BCP-T.A. is a ferroptosis inducer.¹ It induces ferroptosis in NCI H522 non-small cell lung cancer (NSCLC) cells (IC₅₀ = 17 nM), an effect that can be blocked by the ferroptosis inhibitor liproxstatin-1 . BCP-T.A. binds to glutathione peroxidase (GPX4) and increases the accumulation of lipid peroxides in NCI H522 cells when used at a concentration of 0.5 μM. It is cytotoxic to WI38 human lung fibroblasts and mouse embryonic fibroblasts (MEFs; IC₅₀s = 22 and 10 nM, respectively), as well as NCI H522, HT-1080 fibrosarcoma, MDA-MB-468 and MDA-MB-231 breast, and HeLa cervical cancer cells (IC₅₀s = 17, 19, 84, 21, and 242 nM, respectively).

BCP-T.A, a tunable heterocyclic electrophile, is a potent ferroptosis inducer by binding to GPX4[1]. BCP-T.A is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

1. Karaj, E., Sindi, S.H., Kuganesan, N., et al. Tunable cysteine-targeting electrophilic heteroaromatic warheads induce ferroptosis J. Med. Chem. 65(17),11788-11817(2022).