GSK3117391 (ESM-HDAC391; CHR-5154; HDAC-IN-3) is an orally active HDAC inhibitor with a IC 50 of 55 nM. Using esterase-sensitive motif technology, GSK3117391 is selectively converted into its active acid metabolite HDAC189 in cells expressing carboxylesterase-1. GSK3117391 induces sustained global protein acetylation in monocytes, inhibits the production of proinflammatory cytokines, depletes circulating monocytes, downregulates the expression of CSF1R , and inhibits monocyte adhesion and differentiation. GSK3117391 can be used in the research of chronic inflammatory diseases.
Products | Products > Disease Areas > Inflammation or Immune System Disease | Products > Signaling Pathways > Cell Cycle/DNA Damage | Products > Signaling Pathways > Epigenetics | Products > Signaling Pathways > Protein Tyrosine Kinase/RTK | Products > Research Areas > Inflammation/Immunology | Products > Signaling Pathways > HDAC | Products > Signaling Pathways > c-Fms
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