KB-0118 [CAS 2648377-08-4]

KB-0118 (BBC0115) is an orally active BET bromodomain inhibitor. KB-0118 selective binds to BRD2 and BRD4 over BRD3, with Kd values of 36.7 μM for BRD2 BD1 and 47.4 μM for BRD4 BD1. KB-0118 inhibits pro-inflammatory cytokines, including TNF, IL-1β, and IL-23a and selectively suppresses Th17 cell differentiation. KB-0118 modulates Th17-driven inflammation occurs through epigenetic suppression of BRD4, confirmed by downregulation of STAT3 and BRD4 target genes. KB-0118 has immunomodulatory effects in inflammatory bowel disease (IBD) model[1].

[2648377-08-4]

C17H11NO5

309.27

O=C1C(O)=C(C2=CC3=C(C=CN3)C=C2)OC4=C1C(O)=CC(O)=C4

Epigenetic Reader Domain; Interleukin Related; STAT

BRD2; BRD4; IL-1; IL-23; STAT3

Room temperature