BC-1618

BC-1618 is an inhibitor of F-box only protein 48 (FBXO48), an E3 ubiquitin ligase.¹ It is selective for FBXO48 over FBXO30 at 3 µM. BC-1618 (0.5-10 µM) increases the levels of phosphorylated AMP-activated protein kinase (pAMPK) and phosphorylated acetyl-CoA carboxylase (pACC), an AMPK downstream substrate, in HEK293T cells expressing human FBXO48. It induces mitochondrial fission in BEAS-2B cells and autophagy in HEK293A cells expressing GFP-tagged LC3. BC-1618 also inhibits LPS-induced activation of NF-κB in THP-1 cells in a reporter assay and cytokine release in isolated human peripheral blood mononuclear cells (PBMCs). It increases insulin sensitivity in a mouse model of high-fat diet-induced obesity when administered at a dose of 20 mg/kg.

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1. Liu, Y., Jurczak, M.J., Lear, T.B., et al. A Fbxo48 inhibitor prevents pAMPKα degradation and ameliorates insulin resistance. Nat. Chem. Biol. 17(3), 298-306 (2021).