SIK2-IN-4 is a highly selective inhibitor of SIK1 and SIK2, exhibiting IC50 values of 0.143 μM and 0.076 μM, respectively. By targeting SIK1/2, SIK2-IN-4 reduces the phosphorylation of transcription coactivator 3 (CRTC3), thereby modulating cAMP response element binding protein (CREB)-dependent transcriptional activity. This compound demonstrates inhibitory effects on pro-inflammatory cytokines such as TNF, IL-12/23 p40, and IL-23, while promoting the expression of the anti-inflammatory cytokine IL-10. SIK2-IN-4 is a valuable tool for investigating intestinal inflammation and other chronic inflammatory conditions.
SIK2-IN-4 is a highly selective inhibitor of SIK1 and SIK2, exhibiting IC50 values of 0.143 μM and 0.076 μM, respectively. By targeting SIK1/2, SIK2-IN-4 reduces the phosphorylation of transcription coactivator 3 (CRTC3), thereby modulating cAMP response element binding protein (CREB)-dependent transcriptional activity. This compound demonstrates inhibitory effects on pro-inflammatory cytokines such as TNF, IL-12/23 p40, and IL-23, while promoting the expression of the anti-inflammatory cytokine IL-10. SIK2-IN-4 is a valuable tool for investigating intestinal inflammation and other chronic inflammatory conditions.
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