CR1-02

CR1-02 is a potent and selective small molecule inhibitor of the CBP/p300 bromodomain. Developed primarily as a chemical probe, it targets the CREB-binding protein (CBP) and E1A-binding protein p300, which are closely related transcriptional coactivators with intrinsic histone acetyltransferase activity. By binding to the bromodomain of these proteins, CR1-02 prevents their interaction with acetylated histones and other transcription factors, thereby modulating the expression of genes involved in cell proliferation and survival. Research has demonstrated that CR1-02 effectively inhibits the growth of various cancer cell lines, most notably in models of prostate cancer, where it has shown the ability to suppress androgen receptor (AR) signaling and downstream target genes. While it serves as a valuable tool for studying the biological roles of CBP/p300 in health and disease, it is primarily utilized in a research context rather than as a clinical-stage therapeutic asset.

Other names

CR102CR-102CR 102