JTE-607

JTE-607, a highly selective inflammatory cytokine synthesis inhibitor, protects from endotoxin shock in mice. JTE-607 inhibits inflammatory cytokine production, including TNF-α, IL-1β, IL-6, IL-8 and IL-10, from LPS-stimulated human PBMCs, with IC₅₀s of 11, 5.9, 8.8, 7.3 and 9.1 nM, respectively^[1]. Cleavage and Polyadenylation Specificity Factor 3 (CPSF3) is the target of JTE-607^[2]. In Vitro: JTE-607 inhibits inflammatory cytokine production, including TNF-α, IL-1β, IL-6, IL-8 and IL-10, from LPS-stimulated human PBMCs, with IC₅₀s of 11, 5.9, 8.8, 7.3 and 9.1 nM, respectively. The inhibitory effects of JTE-607 are also seen in mRNA expression of those cytokines^[1].
JTE-607 inhibits inflammatory cytokine production from LPS-stimulated human PBMCs with an IC₅₀ of approximately 10 nM^[1].
JTE607 inhibits LPS-stimulated IL-8 production from monkey and rabbit PBMCs, and TNF-α production from mouse and rat PBMCs with IC₅₀s of 59, 780, 1600 and 19000 nM, respectively^[1].
JTE607 also suppresses other cytokines, granulocyte-macrophage colony stimulating factor and IL-1RA with IC₅₀s of 2.4±0.8 and 5.4±0.4 nM, respectively^[1].
JTE-607 inhibits cytokine production in monkey, rabbit, mouse and rat with IC₅₀s of 59±26, 780±120, 1600±650 and 19000±3200 nM, respectively^[1]. In Vivo: JTE-607 (0.3-10 mg/kg, i.v.) shows dose dependent inhibition of mortality after LPS challenge in C. parvum sensitized mice in accordance with a decrease of plasma TNF-α^[1].