KY-226

KY-226 (KY226) is a potent, allosteric, orally active inhibitor of protein tyrosine phosphatase 1B (PTP1B) with IC50 of 0.28 uM (human PTP1B), does not exhibit PPARγ agonist activity; shows no effects on adipocyte differentiation in rodent preadipocytes at 10 uM, bot not the PPARγ agonist pioglitazone; increases the phosphorylated insulin receptor (pIR) produced by insulin in human hepatoma-derived cells (HepG2) at 0.310 uM, significantly reduces plasma glucose and triglyceride levels as well as hemoglobin A1c values without increasing body weight gain in db/db mice, exerts anti-diabetic and anti-obesity effects by enhancing insulin and leptin signaling.

References 1. Ito Y, et al. J Pharmacol Sci. 2018 May;137(1):38-46. 2. Sun M, et al. Brain Res. 2018 Sep 1;1694:1-12. View Related Products by Target Protein Phosphatase/PTP