KB-0118 (BBC0115) is an orally active BET bromodomain inhibitor. KB-0118 selective binds to BRD2 and BRD4 over BRD3, with Kd values of 36.7 µM for BRD2 BD1 and 47.4 µM for BRD4 BD1. KB-0118 inhibits pro-inflammatory cytokines, including TNF, IL-1beta, and IL-23a and selectively suppresses Th17 cell differentiation. KB-0118 modulates Th17-driven inflammation occurs through epigenetic suppression of BRD4, confirmed by downregulation of STAT3 and BRD4 target genes. KB-0118 has immunomodulatory effects in inflammatory bowel disease (IBD) model[1].
Molekulargewicht:
309.27
CAS Nummer:
[2648377-08-4]
Formel:
C17H11NO5
Target-Kategorie:
Epigenetic Reader Domain,Interleukin Related,STAT
Anwendungsbeschreibung:
MCE Product type: Reference compound
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