SIK2-IN-4

Description

SIK2-IN-4 Compound 4 is a highly selective SIK1/2 inhibitor IC50s 0.143 and 0.076 ?M, respectively . SIK2-IN-4 reduces the phosphorylation of transcription coactivator 3 CRTC3 by targeting SIK1/2, thereby regulating cAMP response element binding protein CREB -dependent transcriptional activity. SIK2-IN-4 inhibits the production of pro-inflammatory cytokines such as TNF IC50: 0.11 AAasAasAAmuM , IL-12/23 p40 IC50: 0.25 AAasAasAAmuM , and IL-23 IC50: 0.47 AAasAasAAmuM , while inducing the expression of the anti-inflammatory cytokine IL-10. SIK2-IN-4 can be used to study intestinal inflammation and other chronic inflammatory diseases.