In vitro activity: PTP1B-IN-1 is a potent and new class of inhibitor of protein tyrosine phosphatase-1B (PTP1B) with IC50 of 1.6 mM; It incorporates the 1,2,5-thiadiazolidin-3-one-1,1-dioxide template that was identified through structure-based design. The site specific functionalization of phosphate groups with amino acid side chains of substrate proteins represents one of the most important regulatory mechanisms of biological systems. Phosphorylation and dephosphorylation are reversibly catalyzed by protein kinases and protein phosphatases, and the aberrant regulation of these enzymes is associated with the onset and progression of various disease states such as cancer, diabetes, neurodegenerative and autoimmune disorders, making these proteins attractive targets for drug discovery.

Kinase Assay: PTP1B-IN-1 is a potent and new class of inhibitor of protein tyrosine phosphatase-1B (PTP1B) with IC50 of 1.6 mM;

Cell Assay: