ky-226

Description: KY-226 is a novel, selective, orally bioactive and allosteric inhibitor of protein tyrosine phosphatase 1B (PTP1B) with an IC50 of 0.25 uM, and without PPARgamma agonist activity. KY-226 exerts anti-diabetic and anti-obesity effects by enhancing insulin and leptin signaling, respectively. KY-226 also protects neurons from cerebral ischemic injury. KY-226 protects neurons from cerebral ischemic injury. KY-226 restores Akt (protein kinase B) phosphorylation and extracellular signal-regulated kinase (ERK) reduction in transient middle cerebral artery occlusion (tMCAO) damage. KY-226 protects BBB integrity by restoration of TJ proteins, an effect partly mediated by Akt/FoxO1 pathway activation.

References:

1. Ito Y, 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. 2018 May; 137(1):38-46.

2. Sun M, et al. KY-226 Protects Blood-brain Barrier Function Through the Akt/FoxO1 Signaling Pathway in Brain Ischemia. Neuroscience. 2019 Feb 10; 399:89-102.