PTP1B Inhibitor

• CAT Number: R065099
• CAS Number: 765317-72-4
• Molecular Formula: C26H19Br2N3O7S3
• Molecular Weight: 741.44
• Purity: ≥95%
• Synonyms: Protein Tyrosine Phosphatase 1B Inhibitor
• Target: Phosphatase
• Storage: -20°C
• IUPAC Name: 3-(3,5-dibromo-4-hydroxybenzoyl)-2-ethyl-N-[4-(1,3-thiazol-2-ylsulfamoyl)phenyl]-1-benzofuran-6-sulfonamide
• InChI: InChI=1S/C26H19Br2N3O7S3/c1-2-21-23(24(32)14-11-19(27)25(33)20(28)12-14)18-8-7-17(13-22(18)38-21)41(36,37)30-15-3-5-16(6-4-15)40(34,35)31-26-29-9-10-39-26/h3-13,30,33H,2H2,1H3,(H,29,31)
• InChIKey: SXKBTDJJEQQEGE-UHFFFAOYSA-N
• SMILES: CCC1=C(C2=C(O1)C=C(C=C2)S(=O)(=O)NC3=CC=C(C=C3)S(=O)(=O)NC4=NC=CS4)C(=O)C5=CC(=C(C(=C5)Br)O)Br

Protein tyrosine phosphatase 1B (PTP1B) has critical roles in cell signaling relevant to diabetes, obesity, and cancer. PTP1B inhibitor is a cell-<wbr></wbr>permeable allosteric inhibitor of PTP1B (IC50s = 4 and 8 µM for 403 and 298 residue PTP1B forms, respectively). It binds reversibly and non-<wbr></wbr>competitively, altering the conformation of the catalytic pocket. PTP1B inhibitor selectively increases the phosphorylation of the insulin receptor, insulin receptor substrate 1, and Akt, mimicking the action of insulin.

Reference

1.Zhang, S., and Zhang, Z.Y. PTP1B as a drug target: recent developments in PTP1B inhibitor discovery. Drug Discovery Today 12(9/10), 373-381 (2007).