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PFI-1 PF-6405761

PFI-1 PF-6405761 1403764-72-6
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Chemical Information
Product name:PFI-1 PF-6405761 Purity:98% min
CAS NO:1403764-72-6 Solubility:DMSO : 33.33 mg/mL (95.94 mM)
Molecular Formula:C16H17N3O4S Package:Package according to customer requirements
Molecular Weight:347.389 Storage:Store at -20℃
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Remarks

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.


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