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Tebufenozide is an insecticide that acts as a non-steroidal agonist of the insect ecdysone receptor (EcR; IC50 = 0.85 nM in a cell-free preparation of C. suppressalis integument).1 It induces a premature molt and is lethal to S. litura third instar larva (LD50 = 0.33 μM per larva).1,2 It also inhibits p-glycoprotein activity in LLC-PK1 porcine kidney epithelial cells transfected with human MDR1, the gene for p-glycoprotein (IC50 = 21.5 μM).3 Tebufenozide has low toxicity in mammals, birds, and most aquatic species, but it dose-dependently decreases colony formation and induces apoptosis and cell cycle arrest in HeLa cells when used at concentrations ranging from 50 to 200 μg/ml.4,5

1.Minakuchi, C., Nakagawa, Y., Kamimura, M., et al.Binding affinity of nonsteroidal ecdysone agonists against the ecdysone receptor complex determines the strength of their molting hormonal activityEur. J. Biochem.270(20)4095-4104(2003) 2.Yokoi, T., Minami, S., Nakagawa, Y., et al.Structure-activity relationship of imidazothiadiazole analogs for the binding to the ecdysone receptor of insect cellsPestic. Biochem. Physiol.12040-50(2015) 3.Miyata, K.-i., Nakagawa, Y., Kimura, Y., et al.Structure-activity relationships of dibenzoylhydrazines for the inhibition of P-glycoprotein-mediated quinidine transportBioorg. Med. Chem.24(14)3184-3191(2016) 4.Xu, W., Wang, B., Yang, M., et al.Tebufenozide induces G1/S cell cycle arrest and apoptosis in human cellsEnviron. Toxicol. Pharmacol

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