PLX-4545 is an orally active, selective molecular glue degrader targeting IKZF2. Through a molecular glue mechanism, PLX-4545 binds to CRBN, recruits IKZF2 to form a ternary complex, and promotes its ubiquitination and proteasomal degradation. This further converts inhibitory regulatory T cells (Treg) into effector-like T cells, enhances CD8+ T cell responses, and modulates the Teff:Treg balance. PLX-4545 also increases the production of the inflammatory cytokine IL-2 and reduces the suppressive activity of Treg. PLX-4545 can be used in cancer immunotherapy research, and exhibits a synergistic effect when combined with immune checkpoint inhibitors such as anti-PD1[1][3].
Molekulargewicht:
473.56
Reinheit:
96.76
CAS Nummer:
[2892065-45-9]
Formel:
C28H31N3O4
Target-Kategorie:
IKZF Family,Ligands for E3 Ligase,Molecular Glues
Anwendungsbeschreibung:
MCE Product type: Reference compound1
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