Inobrodib (CCS1477) is an orally active, potent, and selective inhibitor of the p300/CBP bromodomain. It binds to p300 and CBP with Kd values of 1.3 and 1.7 nM, respectively, showing 170/130-fold selectivity compared with BRD4 (Kd of 222 nM). It inhibits cell proliferation in prostate cancer cell lines and decreases androgen receptor (AR)- and C-MYC-regulated gene expression. Inobrodib also suppresses the growth of mouse xenograft models with an associated reduction in AR signaling.
- Potent and selective inhibitor of p300/CBP bromodomain
- Binds to p300 and CBP with high affinity
- Exhibits significant selectivity over BRD4
- Inhibits cell proliferation in prostate cancer cell lines
- Decreases androgen receptor (AR)- and C-MYC-regulated gene expression
- Suppresses tumor growth in mouse xenograft models