LRE1

LRE1 is an allosteric inhibitor of soluble adenylyl cyclase (sAC; IC₅₀ = <10 µM).¹ It is selective for sAC over AC1, -2, -5, -8, and -9 at 50 µM. LRE1 inhibits cAMP accumulation in HEK293 cells overexpressing human sAC (IC₅₀ = 11 µM). It inhibits the activity of mitochondrial complex IV, also known as cytochrome c oxidase, in wild-type but not sAC knockout mouse embryonic fibroblasts (MEFs) when used at a concentration of 50 µM. Ex vivo, LRE1 (1.2 mg/kg) reduces ischemia and reperfusion-induced swelling of, and ATP content decreases in, rat liver mitochondria.²

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1. Ramos-Espiritu, L., Kleinboelting, S., Navarrete, F.A., et al. Discovery of LRE1 as a specific and allosteric inhibitor of soluble adenylyl cyclase. Nat. Chem. Biol. 12(10), 838-844 (2016).

2. Teodoro, J.S., Amorim, J.A., Machado, I.F., et al. The soluble adenylyl cyclase inhibitor lre1 prevents hepatic ischemia/reperfusion damage through improvement of mitochondrial function. Int. J. Mol. Sci. 21(14), 4896 (2020).