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.
| Marque | Tocris Bioscience |
|---|---|
| Réf. B-LABO | BL-RE-163324 |
| Réf. fabricant | 18733939 |
| Nom chimique ou matériau | JTE 607 dihydrochloride |
| CAS | 188791-09-5 |
| Synonyme | N-[3,5-Dichloro-2-hydroxy-4-[2-(4-methyl-1-piperazinyl)ethoxy]benzoyl]-L-phenylalanine ethyl ester dihydrochloride |
| Quantité | 10 mg |
| Solubilité | Soluble to 100mM in water and to 100mM in DMSO |
| Formule moléculaire | C<sub>2</sub><sub>5</sub>H<sub>3</sub><sub>1</sub>Cl<sub>2</sub>N<sub>3</sub>O<sub>5</sub>·2HCl |
| Poids de la formule | 597.36 |
| Forme physique | Solid |
| Type de produit | Bioactive Small Molecule |
| Pureté | >98% |
