KY-226
PTP1B inhibitor / 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
Biochemicals & reagents
1621673-53-7
1) Morishita et al., (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
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TARGET: Phosphatase -- PATHWAY: Carbohydrate metabolism; AKT -- RESEARCH AREA: Neuroscience -- DISEASE AREA: Diabetes; ObesityIschemia