GSK046 (GSK-046, iBET-BD2) is a potent, highly selective inhibitor of BET BD2 with pIC50 of 7.3 (BRD4 BD2), >1000-fold over BRD4 BD1.
GSK046 (iBET-BD2) potently inhibits BRD2/BRD3/BRDT BD2 with pIC50 of 6.6/7.0/6.7.
GSK046 (iBET-BD2) inhibits MCP-1 cytokine release (pIC50=7.5) with a minimal drop-off from the biochemical BRD4 BD2 potency observed in an LPS-stimulated PBMC cellular assay.
GSK046 (iBET-BD2) is efficacious in a broad range of inflammatory pathologies and selective BD2 inhibition may be a useful new therapeutic strategy for immunoinflammatory diseases.
