KB-0118
Product Specifications
CAS Number
2648377-08-4
Target
Interleukin|||STAT|||Epigenetic Reader Domain
Related Pathways
Chromatin/Epigenetic|||JAK/STAT signaling|||Stem Cells|||Immunology/Inflammation
Bioactivity
KB-0118 (BBC0115) is an inhibitor targeting the BET bromodomain. It selectively binds to BRD2 and BRD4, with dissociation constants (Kd) of 36.7 ?M for BRD2 BD1 and 47.4 ?M for BRD4 BD1, while not binding to BRD3. KB-0118 suppresses the secretion of pro-inflammatory cytokines such as TNF, IL-1?, and IL-23a, and selectively inhibits Th17 cell differentiation. The compound regulates Th17-driven inflammation through the epigenetic suppression of BRD4, as evidenced by the downregulation of STAT3 and BRD4 target genes. Additionally, KB-0118 exhibits immunomodulatory effects in inflammatory bowel disease (IBD) models.
Smiles
O=C1C(O)=C(OC=2C=C(O)C=C(O)C12)C=3C=CC=4C=CNC4C3
Molecular Formula
C17H11NO5
Molecular Weight
309.27
Shipping Conditions
Cool pack
Storage Temperature
-20°C
Available Sizes
Curated Selection
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