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440(3):405-13
Formula: C21H22N2O4S
It exhibits 15-fold selectivity for the BAZ2 bromodomain over the CERC2 bromodomain and >100-fold selectivity over a range of other bromodomains
The azide group can react with alkyne
37)/t27-/m0/s1
PFI-1 - BET Inhibitor. CAS# 1403764-72-6 size:2 mg solid 440(3):405-13PFI 1, CAS No. 1403764 72 6, is a novel potent, selective and cell permeable inhibitor of the bromodomain and extra terminal (BET) family proteins BRD2 and BRD4 with IC50 of ~98 nM and 220 nM respectively. Co crystal structures showed that PFI 1 acts as an acetyl lysine (Kac) mimetic inhibitor efficiently occupying the Kac binding site in BRD2 and BRD4. It has an EC50 of 1. 89 M for the inhibition of IL6 production from human blood mononuclear cells
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