The LYP Inhibitor II, LTV-1 controls the biological activity of LYP. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
Synonym(s):
LYP Inhibitor II, LTV-1, ( E)-3-((4-((4,6-Dioxo-2-thioxo-1- o-tolyltetrahydropyrimidin-5(6H)-ylidene)methyl)phenoxy)methyl)benzoic acid, Lymphoid Tyrosine Phosphatase Inhibitor II, LTV-1, (E)-3-((4-((4,6-Dioxo-2-thioxo-1-o-tolyltetrahydropyrimidin-5(6H)-ylidene)methyl)phenoxy)methyl)benzoic acid, Lymphoid Tyrosine Phosphatase Inhibitor II, LTV-1
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
Warning
Toxicity: Standard Handling (A)
Reconstitution
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
Storage Class Code
11 - Combustible Solids
WGK
WGK 2
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
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