I-BET151

I-BET151 is a **synthetic small molecule inhibitor** that selectively targets **bromodomain and extra-terminal (BET) proteins**, specifically BRD2, BRD3, and BRD4, and indirectly affects BRD9[1][4][7][10][14]. By binding to the acetyl-lysine recognition pocket of these proteins, I-BET151 **displaces BET proteins from nuclear chromatin**, resulting in repression of transcription of oncogenic drivers such as MYC and BCL2, cell cycle regulatory proteins (e.g., CDK6), and effectors of Hedgehog signaling (e.g., GLI1)[1][3][6][9]. This leads to **cell cycle arrest, apoptosis, and inhibition of proliferation** in various cancer models, including hematologic malignancies (e.g., mixed lineage leukemia and multiple myeloma) and solid tumors (such as breast cancer, glioma, melanoma, neuroblastoma, and ovarian cancer)[1][3][9]. In preclinical studies, I-BET151 also **suppresses inflammation** by attenuating pro-inflammatory cytokine production and immune cell infiltration[2]. I-BET151 was developed by **GSK** and remains in the preclinical stage for all indications[1][15].

Other names

7-(3,5-dimethyl-4-isoxazolyl)-8-(methyloxy)-1-[(1R)-1-(2-pyridinyl)ethyl]-1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-one