A cell-permeable thiobarbituryl-benzoate compound that acts as a highly potent and reversible inhibitor of lymphoid tyrosine phosphatase (LYP) (IC50=508nM) and thereby enhances TCR signaling in intact cells. Exhibits competitive to mixed mode of inhibition (Ki=384nM). 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 100uM, respectively). Does not exhibit any toxicity at pharmacological doses when tested in primary human cell lines.
Formula:C26H20N2O5S
Molecular Weight:472.5
Solubility:DMSO (50mg/ml)
Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with sterile buffer or dH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
