SIK2-IN-4 (Compound 4) is a highly selective SIK1/2 inhibitor (IC 50s 0.143 and 0.076 μM, 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 (IC 50 : 0.11 µM), IL-12/23 p40 (IC 50 : 0.25 µM), and IL-23 (IC 50 : 0.47 µM), 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.
Products | Products > Disease Areas > Infection | Products > Signaling Pathways > Immunology/Inflammation | Products > Signaling Pathways > Apoptosis | Products > Research Areas > Infection | Products > Signaling Pathways > Salt-inducible Kinase (SIK) | Products > Signaling Pathways > Interleukin Related | Products > Signaling Pathways > TNF Receptor
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