JTE 607 dihydrochloride

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JTE 607 dihydrochloride | CAS No. 188791-09-5 | Cytokine Compounds
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Description: Active metabolite binds CPSF3; Pro-drug
Alternative Names: TO-207

Chemical Name: N-[3,5-Dichloro-2-hydroxy-4-[2-(4-methyl-1-piperazinyl)ethoxy]benzoyl]-L-phenylalanine ethyl ester dihydrochloride

Purity: ≥98%

Product Details
Citations (3)

Biological Activity

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.

Technical Data

Soluble to 100 mM in water and to 100 mM in DMSO
Desiccate at RT

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

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Citations for JTE 607 dihydrochloride

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