Catalog No.: PC-38126Not For Human Use, Lab Use Only.
CCS1477 (Inobrodib) is an orally bioavailable, potent, and selective inhibitor of the p300/CBP bromodomain, binds to p300 and CBP with Kds of 1.3 and 1.7 nM respectively.
CCS1477 (Inobrodib) is an orally bioavailable, potent, and selective inhibitor of the p300/CBP bromodomain, binds to p300 and CBP with Kds of 1.3 and 1.7 nM respectively.
CCS1477 (Inobrodib) displays > 170/130-fold selectivity compared with BRD4, CCS1477 binding to cellular histones in an in-cell BRET assay, with an IC50 of 19 nM for p300 and 1060 nM for BRD4.
CCS1477 (Inobrodib) has only minimal binding to BRD2, 3, 4, 9 and WDR9 (14-33% of control at 1 uM) in a bromoscan assay of 32 bromodomains.
CCS1477 inhibits cell proliferation in prostate cancer cell lines and decreases AR- and C-MYC-regulated gene expression.
CCS1477 has antitumor activity, regulating AR and C-MYC signaling in AR-SV-driven models.
CCS1477 modulates KLK3 blood levels and regulates CRPC biopsy biomarker expression.
