Merck, 540218-10MG, LYP Inhibitor II, LTV-1

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 (Ki = 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.
Biochem/physiol Actions
Primary Target
LYP
Secondary Target
Othet PTPases
Target IC₅₀: 508 nM for LYP
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C>
Other Notes
Vang, T., et al. 2012. Nat. Chem. Biol.8, 437.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)