JTE 607 dihydrochloride
Chemical Name: N-[3,5-Dichloro-2-hydroxy-4-[2-(4-methyl-1-piperazinyl)ethoxy]benzoyl]-L-phenylalanine ethyl ester dihydrochloride
Biological ActivityJTE 607 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 also inhibits cytokine release; it 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
JTE-607, a multiple cytokine production inhibitor, induces apoptosis accompanied by an increase in p21waf1/cip1 in acute myelogenous leukemia cells.
Tajima et al.
Cancer Sci., 2010;101:774
JTE-607, a novel inflammatory cytokine synthesis inhibitor without immunosuppression, protects from endotoxin shock in mice.
Kakutani et al.
JTE-607, a cytokine release blocker, attenuates acid aspiration-induced lung injury in rats.
CPSF3-dependent pre-mRNA processing as a druggable node in AML and Ewing's sarcoma.
Ross et al.
Citation for JTE 607 dihydrochloride
The citations listed below are publications that use Tocris products. Selected citations for JTE 607 dihydrochloride include:
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