Merck, 540211-10MG, PTP Inhibitor IV

General description
An uncharged, 1,4-di-substituted, phenyl-linked, bis-trifluoromethylsulfonamido (TFMS) phosphate mimetic that acts as a potent, reversible, substrate competitive, active-site-directed inhibitor of protein tyrosine phosphatases (PTP). Reported to inhibit SHP-2 (IC₅₀ = 1.8 µM), PTP1B (IC₅₀ = 2.5 µM), PTP-ε (IC₅₀ = 8.4 µM), PTP-Meg-2 (IC₅₀ = 13 µM), PTP-ς (IC₅₀ = 20 µM), PTP-β (IC₅₀ = 6.4 µM), and PTP-µ (IC₅₀ = 6.7 µM).
Biochem/physiol Actions
Cell permeable: no
Primary Target
SHP-2
Product competes with ATP.
Reversible: yes
Target IC₅₀: 1.8, 2.5, 8.4, 13, 20, 6.4, and 6.7 µM for SHP-2, PTP1B, PTP-ε, PTP-Meg-2, PTP-σ, PTP-β, and PTP-µ, respectively
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Huang, P., et al. 2003. Bioorg. Med. Chem.11, 1835.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)