PLX2853

PLX2853 is an orally bioavailable, small-molecule inhibitor of the bromodomain and extraterminal (BET) family of proteins, with a particular focus on inhibiting bromodomain-containing protein 4 (BRD4). It binds to the acetylated lysine recognition motifs in the BRD4 protein's bromodomains, preventing BRD4 from binding to acetylated lysines on histones. This disrupts chromatin remodeling and dysregulates gene expression, leading to antineoplastic effects. By regulating genes such as MYC and BCL2 that are critical for cancer cell proliferation and survival, PLX2853 has demonstrated broad anti-leukemic activity both as a single agent and in combination with other agents in preclinical models. The drug is being developed primarily for hematologic malignancies (such as myelofibrosis), gynecologic cancers with ARID1A mutations, ovarian cancer (including platinum-resistant disease), acute myeloid leukemia (AML), myelodysplastic syndromes (MDS), prostate cancer, solid tumors, and graft-versus-host disease[1][2][6][7][8].

Other names

PLX2853PLX-2853PLX 2853OPN 2853OPN2853OPN-2853