Tocris Bioscience™ JTE 607 Dihydrochloride

Description

Cytokine release inhibitor; anti-inflammatory

JTE 607 dihydrochloride is a pro-drug that is cleaved by carboxylesterase 1 (CES1) to its active metabolite, which then binds to cleavage and polyadenylation specificity factor 3 (CPSF3; Kd = 370 nM at human CPSF3). Treatment of A-673 cells with JTE 607 results in inhibition of mRNA cleavage and accumulation of nuclear R-loops. JTE 607 induces apoptosis in leukemia cells in vitro and prolongs survival in a mouse leukemia model. JTE 607 inhibits cytokine release and inhibits production of IL-1β, IL-8, IL-6, IL-10 and TNFα (IC50 values are 5.9, 7.3, 8.8, 9.1 and 11.0 nM, respectively) from LPS-stimulated PBMCs. In a rat model of lung injury, JTE 607 reduces proinflammatory cytokine-release and attenuates lung permeability.

Specifications

• Chemical Name or Material: JTE 607 dihydrochloride
• CAS: 188791-09-5
• Synonym: N-[3,5-Dichloro-2-hydroxy-4-[2-(4-methyl-1-piperazinyl)ethoxy]benzoyl]-L-phenylalanine ethyl ester dihydrochloride
• Quantity: 10 mg
• Solubility: Soluble to 100mM in water and to 100mM in DMSO
• Molecular Formula: C₂₅H₃₁Cl₂N₃O₅·2HCl
• Formula Weight: 597.36
• Physical Form: Solid
• Product Type: Bioactive Small Molecule
• Purity: >98%

Research Use Only. Not For Human or Veterinary Use