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Tocris Bioscience™ JTE 607 Dihydrochloride
Active metabolite binds CPSF3; Pro-drug
Brand: Tocris Bioscience™ 5185/50
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Beskrivelse
JTE 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.
Tekniske data
| JTE 607 dihydrochloride | |
| N-[3,5-Dichloro-2-hydroxy-4-[2-(4-methyl-1-piperazinyl)ethoxy]benzoyl]-L-phenylalanine ethyl ester dihydrochloride | |
| Soluble to 100mM in water and to 100mM in DMSO | |
| Bioactive Small Molecule |
| 188791-09-5 | |
| 50 mg | |
| Solid |
Produkttitel
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