Biochem/physiol Actions

Primary TargetLYP

Secondary TargetOthet PTPases

Target IC₅₀: 508 nM for LYP

General description

A cell-permeable thiobarbituryl-benzoate compound that acts as a highly potent and reversible inhibitor of lymphoid tyrosine phosphatase (LYP) (IC₅₀ = 508 nM) and thereby enhances TCR signaling in intact cells. Exhibits competitive to mixed mode of inhibition (K_i = 384 nM). Also shown to inhibit the mutant, disease associated LYP-Trp⁶²⁰ activity. Binds to the phosphate-binding loop and mimicks the phosphotyrosine moiety of substrates. Displays acceptable selectivity over a wide range of protein phosphatases (TCPTP, PTP1B, PEP (mouse LYP), SHP1, CD45 and PTP-PEST: IC₅₀ = 1.52, 1.59, 7.56, 23.2, 30.1, and 100 µM, respectively). Does not exhibit any toxicity at pharmacological doses when tested in primary human cell lines.

Legal Information

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

Other Notes

Vang, T., et al. 2012. Nat. Chem. Biol.8, 437.

Packaging

10 mg in Glass bottle

Reconstitution

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

Warning

Toxicity: Standard Handling (A)