5-Aminoimidazole-4 -carboxamide-1-β-D-ribofuranoside (AICAR) is an activator of AMPK that also decreases mTORC1 signaling; it displays anticancer, antihypertensive, anti-diabetic, and anti-inflammatory activities. AICAR enhances the efficacy of rapamycin in several cancer cells and suppresses signaling by HER2 and EGFR2 in breast cancer cells. This compound also decreases mean arterial pressure in ApoE-/- animal models and induces vasodilation in aortic rings. In animal models of insulin resistance, AICAR decreases hyperglycemia, lowers insulin levels, and improves insulin signaling. Additionally, AICAR inhibits LPS/D-Gal-induced upregulation of TNF-α, NO, and myeloperoxidase in animal models of hepatitis.