JTE-607

Modify Date: 2024-01-02 19:12:03

JTE-607 Structure
JTE-607 structure
Common Name JTE-607
CAS Number 188791-09-5 Molecular Weight 597.36
Density N/A Boiling Point N/A
Molecular Formula C25H33Cl4N3O5 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of 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].

 Names

Name ethyl (2S)-2-[[3,5-dichloro-2-hydroxy-4-[2-(4-methylpiperazin-1-yl)ethoxy]benzoyl]amino]-3-phenylpropanoate,dihydrochloride
Synonym More Synonyms

 JTE-607 Biological Activity

Description 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].
Related Catalog
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]. RT-PCR[1] Cell Line: human peripheral blood mononuclear cells (PBMCs) Concentration: 100 nM Incubation Time: 20 hours Result: Reduced the increase in the level of mRNAs of TNF-α, IL-1b, IL-6 and IL-8.
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]. Animal Model: Male C57BL/6 mice (5 to 6 weeks old) are sensitized by injecting Corynebacterium parvum[1] Dosage: 0.3, 1, 3, 10 mg/kg Administration: Administered intravenously 10 min before the LPS challenge. Result: Showed dose dependent inhibition of the mortality at 0.3 to 10 mg/kg and significant effect at 3 and 10 mg/kg.
References

[1]. M Kakutani, et al. JTE-607, a novel inflammatory cytokine synthesis inhibitor without immunosuppression, protects from endotoxin shock in mice. Inflamm Res. 1999 Aug;48(8):461-8.

[2]. Nathan T Ross, et al. CPSF3-dependent pre-mRNA processing as a druggable node in AML and Ewing's sarcoma. Nat Chem Biol. 2020 Jan;16(1):50-59.

 Chemical & Physical Properties

Molecular Formula C25H33Cl4N3O5
Molecular Weight 597.36
Exact Mass 595.11700
PSA 94.83000
LogP 5.28400

 Synonyms

unii-2b68h6bwcx
jte-607
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