Biochem/physiol Actions

Cell permeable: no

Reversible: yes

Product competes with ATP.

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

Primary TargetSHP-2

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).

An uncharged, 1,4-di-substituted, phenyl-linked bis-trifluoromethylsulfonamido (TFMS) phosphate mimetic that acts as a potent, reversible, competitive, and active-site directed inhibitor of protein tyrosine phosphatases (PTP; 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).

Legal Information

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

Other Notes

Huang, P., et al. 2003. Bioorg. Med. Chem.11, 1835.

Packaging

Packaged under inert gas

10 mg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)