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<i>Tribolium castaneum</i> is a damaging pest of stored grains, causing significant losses and secreting lethal quinones, which render the grains unfit for human consumption. Chemical insecticides are the most commonly used approach for control; however, they create insecticide resistance and affect the health of humans, animals, and the environment. As a result, it is critical to find an environmentally friendly pest-management strategy. In this study, two naturally occurring chemicals, benzyl alcohol (BA) and benzoyl benzoate (BB), were investigated for insecticidal activity against <i>T. castaneum</i> using different assays (impregnated-paper, contact toxicity, fumigant, and repellency assays). The results showed that BA had a significant insecticidal effect, with the LC₅₀ achieved at a lower concentration in the direct-contact toxicity test (1.77%) than in the impregnated-paper assay (2.63%). BB showed significant effects in the direct-contact toxicity test, with an LC₅₀ of 3.114%, and a lower toxicity in the impregnated-paper assay, with an LC₅₀ of 11.75%. Furthermore, BA exhibited significant fumigant toxicity against <i>T. castaneum</i>, with an LC₅₀ of 6.72 µL/L, whereas BB exhibited modest fumigant toxicity, with an LC₅₀ of 464 µL/L. Additionally, at different concentrations (0.18, 0.09, 0.045, and 0.0225 µL/cm²), BA and BB both showed a notable and potent repelling effect. BA and BB significantly inhibited acetylcholinesterase, reduced glutathione (GSH), and increased malondialdehyde (MDA) in treated <i>T. castaneum</i>. This is the first report of BA insecticidal activity against the red flour beetle. Also, the outcomes of various assays demonstrated that the application of BA induces a potent bio-insecticidal effect. BA may be a promising eco-friendly alternative to control <i>T. castaneum</i> due to its safety and authorization by the EFSA (European Food Safety Authority).