540218-M

LYP Inhibitor II, LTV-1

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
• Empirical Formula (Hill Notation): C₂₆H₂₀N₂O₅S
• Molecular Weight: 472.51
• UNSPSC Code: 12352200
• NACRES: NA.28

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: powder
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: orange
• solubility: DMSO: 50 mg/mL
• storage temp.: 2-8°C

Description

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.

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 2
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable