KB-0118 is a selective inhibitor of the bromodomains BRD2 and BRD4, exhibiting Kd values of 36.7 μM and 47.4 μM, respectively. This orally active compound effectively inhibits the production of pro-inflammatory cytokines, such as TNF, IL-1β, and IL-23a, and selectively reduces Th17 cell differentiation. The compound modulates Th17-driven inflammatory processes through the epigenetic suppression of BRD4, leading to decreased expression of STAT3 and other target genes. KB-0118 demonstrates potential therapeutic benefits in models of inflammatory bowel disease (IBD).
KB-0118 is a selective inhibitor of the bromodomains BRD2 and BRD4, exhibiting Kd values of 36.7 μM and 47.4 μM, respectively. This orally active compound effectively inhibits the production of pro-inflammatory cytokines, such as TNF, IL-1β, and IL-23a, and selectively reduces Th17 cell differentiation. The compound modulates Th17-driven inflammatory processes through the epigenetic suppression of BRD4, leading to decreased expression of STAT3 and other target genes. KB-0118 demonstrates potential therapeutic benefits in models of inflammatory bowel disease (IBD).
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