KY-226

KY-266 is an inhibitor of protein tyrosine phosphatase 1B (PTP1B; IC₅₀ = 0.28 µM).¹ It enhances insulin-induced phosphorylation of insulin receptors in HepG2 cells when used at concentrations of 1, 3, and 10 µM. In vivo, KY-266 (10 and 30 mg/kg) reduces plasma glucose and triglyceride levels and hemoglobin A1c (HbA1c) levels in db/db mice. It decreases body weight gain, food intake, and fat volume gain in a mouse model of high-fat diet-induced obesity when administered at 30 and 60 mg/kg per day for four weeks. Intraperitoneal administration of KY-226 (10 mg/kg) restores Akt phosphorylation and reduces cortical reactive oxygen species (ROS) production in a mouse model of ischemia-reperfusion injury induced by middle cerebral artery occlusion (MCAO).²

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1. Ito, Y., Fukui, M., Kanda, M., et al. Therapeutic effects of the allosteric protein tyrosine phosphatase 1B inhibitor KY-226 on experimental diabetes and obesity via enhancements in insulin and leptin signaling in mice. J. Pharmacol. Sci. 137(1), 38-46 (2018).

2. Sun, M., Izumi, H., Shinoda, Y., et al. Neuroprotective effects of protein tyrosine phosphatase 1B inhibitor on cerebral ischemia/reperfusion in mice. Brain Res. 1694, 1-12 (2018).