PELI1-IN-1 (compound 3d) is a potent inhibitor of PELI1, E3 ubiquitin ligase. PELI1-IN-1 has anti-tumPELI1-IN-1, a Resveratrol (HY-16561) derivative, is an orally active PELI1 Inhibitor (Kd = 8.2 µM). PELI1-IN-1 markedly interrupts the interaction of PELI1 and SNAIL/SLUG, and inhibits the K63-polyubiquitization of SNAIL/SLUG by PELI1, subsequently downregulating the protein levels of epithelial-mesenchymal transition (EMT) effectors SNAIL/SLUG. PELI1-IN-1 significantly reduces the level of SNAIL, SLUG and Vimentin without affecting the PELI1 expression. PELI1-IN-1 targets the FHA domain of PELI1 and disrupts the interaction, leading to the anti-metastasis of TNBC cells in vitro and in vivo. PELI1-IN-1 shows no evident toxicity in vivo[1].
Molekulargewicht:
320.34
Reinheit:
98.02
Formel:
C20H16O4
Target-Kategorie:
Cytochrome P450,E1/E2/E3 Enzyme,Proteasome
Anwendungsbeschreibung:
MCE Product type: Reference compound
* Mehrwertsteuer und Versandkosten nicht enthalten. Irrtümer und Preisänderungen vorbehalten
