Chemical Name: Ethyl (2S)-2-[[3,5-Dichloro-2-hydroxy-4-[2-(4-methylpiperazin-1-yl)ethoxy]benzoyl]amino]-3-phenylpropanoate dihydrochloride
mRNA processing inhibitor
Molekulargewicht:
597.36
Reinheit:
98% by HPLC NMR (Conforms)
Formulierung:
White solid
CAS Nummer:
[188791-09-5]
Formel:
C25H31Cl2N3O52HCl
Anwendungsbeschreibung:
JTE-607 inhibits inflammatory cytokine production in human peripheral blood mononuclear cells (PBMCs) without causing immunosuppression: IC50s = 11 nM (TNF-), 5.9 nM (IL-1), 8.8 nM (IL-6), 7.3 nM (IL-8), and 9.1 nM (IL-10).1 It displayed efficacy in a mouse model of septic shock.2 JTE-607 also showed inhibitory activity against acute myelogenous leukemia cell lines.3,4 Recently, the mechanism of action of JTE-607 (a pro-drug, with the active species being the free acid) has been found to be inhibition of pre-messenger RNA endonuclease Cleavage and Polyadenylation Specificity Factor 3 (CPSF3).5,6 This prevents release of newly synthesized mRNAs resulting in read-through transcription and the formation of DNA-RNA hybrid R-loop structures. Transcripts down-regulated by JTE-607 were related to DNA damage-based phenotype
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