Halicin

Halicin is a JNK1 inhibitor (IC₅₀ = 0.7 µM).^1,2 It is selective for JNK1 over p38α, Furin, and lethal factor (IC₅₀s = >100, >100, and >50 µM, respectively), as well as Akt at 100 µM.¹ Halicin inhibits TNF-α-induced phosphorylation of c-Jun in a cell-based assay (EC₅₀ = 6.23 µM). In vivo, halicin (25 mg/kg) reduces blood glucose levels and restores insulin sensitivity in insulin insensitive mice. Halicin is active against carbapenem-resistant Enterobacteriaceae (MICs = 1-10 µg/ml), as well as multidrug-resistant A. baumannii and P. aeruginosa (MICs = 1-10 and 1-100 µg/ml, respectively).² It reduces the number of wound tissue colony forming units (CFUs) in a mouse model of A. baumannii wound infection. Halicin (15 mg/kg) also reduces fecal bacterial load in a mouse model of C. difficile infection.

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1. De, S.K., Stebbins, J.L., Chen, L.-H., et al. Design, synthesis, and structure-activity relationship of substrate competitive, selective, and in vivo active triazole and thiadiazole inhibitors of the c-Jun N-terminal kinase. J. Med. Chem. 52(7), 1943-1952 (2009).

2. Stokes, J.M., Yang, K., Swanson, K., et al. A deep learning approach to antibiotic discovery. Cell 180(4), 688-702 (2020).