539741

PTP1B Inhibitor

PTP1B Inhibitor, CAS 765317-72-4, is a cell-permeable, selective, reversible and non-competitive allosteric inhibitor of PTP1B (IC₅₀ = 4 µM and 8 µM for PTP1B403 and PTP1B298, respectively).

• Synonym(s): PTP1B Inhibitor, 3-(3,5-Dibromo-4-hydroxy-benzoyl)-2-ethyl-benzofuran-6-sulfonicacid-(4-(thiazol-2-ylsulfamyl)-phenyl)-amide, PTP Inhibitor XXII
• Empirical Formula (Hill Notation): C₂₆H₁₉Br₂N₃O₇S₃
• CAS Number: 765317-72-4
• Molecular Weight: 741.45
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: white
• solubility: DMSO: 100 mg/mL; ethanol: 5 mg/mL
• shipped in: wet ice
• storage temp.: −20°C
• 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)
• InChI key: SXKBTDJJEQQEGE-UHFFFAOYSA-N

Description

General description

A cell-permeable, selective, reversible, and non-competitive allosteric inhibitor of PTP1B (IC₅₀ = 4 µM and 8 µM for PTP1B₄₀₃ and PTP1B₂₉₈, respectively). Binds to a novel site away from the catalytic pocket and inhibits PTP1B activity by preventing closure of the WPD loop. Also available in InSolution format (Cat. No. 539749.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
PTP1B403

Product does not compete with ATP.

Reversible: yes

Target IC₅₀: 4 µM and 8 µM for PTP1B403 and PTP1B298, respectively

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Wiesmann, C., et al. 2004. Nat. Struct. Mol. Biol.11, 730.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 2
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable