1621673-53-7

KY-226 (CAS 1621673-53-7)? is a selective allosteric protein tyrosine phosphatase 1B (PTP1B) inhibitor (IC50?= 250 nM) with no activity at PPARγ.1?It significantly reduced plasma glucose, triglyceride, and A1c levels without weight gain in db/db mice.2?It has been suggested that KY-226’s anti-diabetic effects occur?via?enhancements in insulin signaling and anti-obesity effects via leptin signaling enhancements.2?KY-226 has also been shown to protect neurons from cerebral ischemia.3?This effect is mediated by restoration of tight junction proteins?via?activation of the Akt/FoxO1 pathway.4

KY-226 is a potent, selective, orally active and allosteric protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 0.25 μM, and without PPARγ 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[1][2].

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1) Morashita (2017),?Novel Non-carboxylate Benzoylsulfonamide-Based Protein Tyrosine Phosphatase 1B Inhibitor with Non-competitive Actions;?Chem.Pharm.Bull.?65?1144 2) Ito?et al.?(2018),?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?38 3) Sun?et al.?(2018),?Neuroprotective effects of protein tyrosine phosphatase 1B on cerebral ischemia/reperfusion in mice;?Brain Res.?1694?1 4) Sun?et al.?(2019),?KY-226 Protects Blood-brain Barrier Function Through the Akt/FoxO1 Signaling Pathway on Brain Ischemia;?Neuroscience?399?89