PFI-1 is a potent and highly selective protein interaction Inhibitor, which targets BET bromodomain. PFI-1 that efficiently blocks the interaction of BET BRDs with acetylated histone tails. Co-crystal structures showed that PFI-1 acts as an acetyl-lysine (Kac) mimetic inhibitor efficiently occupying the Kac binding site in BRD4 and BRD2. PFI-1 has antiproliferative effects on leukaemic cell lines and efficiently abrogates their clonogenic growth. Exposure of sensitive cell lines with PFI-1 results in G1 cell cycle arrest, down-regulation of MYC expression as well as induction of apoptosis and induces differentiation of primary leukaemic blasts.
Epigenetic Reader Domain Inhibitors Related Products:
ICG-001; (+)-JQ1; I-BET151; Molibresib; Apabetalone; C646; Curcumin; Bromosporine; Birabresib; UNC1215; GSK6853; CPI-637; BI-9564; PFI-4; XMD8-92; MS436; CPI-203; KG-501; Mivebresib; GSK2801