2229039-45-4

ZL0420 is a potent and selective BRD4 inhibitor. ZL0420 reduces airway inflammation and inhibits the TLR3-dependent innate immune gene program, including ISG54, ISG56, IL-8, and Groβ genes in cultured human small airway epithelial cells (hSAECs).

(E/Z)-ZL0420 is a racemic compound of (Z)-ZL0420 and (E)-ZL0420 isomers. (E)-ZL0420 is a potent and selective bromodomain-containing protein 4 (BRD4) inhibitor with IC50 values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2[1].

[1] Zhiqing Liu, et al. Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation. Eur J Med Chem. 2018 May 10;151:450-461. DOI:10.1016/j.ejmech.2018.04.006