In Silico and In Vitro Study of Janus Kinases Inhibitors from Naphthoquinones.

ABSTRACT: Janus kinases (JAKs) are involved in numerous cellular signaling processes related to immune cell functions. JAK2 and JAK3 are associated with the pathogenesis of leukemia and common lymphoid-derived illnesses. JAK2/3 inhibitors could reduce the risk of various diseases by targeting this pathway. Herein, the naphthoquinones were experimentally and theoretically investigated to identify novel JAK2/3 inhibitors. Napabucasin and 2'-methyl napabucasin exhibited potent cell growth inhibition in TF1 (IC₅₀ = 9.57 and 18.10 μM) and HEL (IC₅₀ = 3.31 and 6.65 μM) erythroleukemia cell lines, and they significantly inhibited JAK2/3 kinase activity (in a nanomolar range) better than the known JAK inhibitor, tofacitinib. Flow cytometric analysis revealed that these two compounds in

SUBMITTER: Sanachai K 

PROVIDER: S-EPMC9866339 | biostudies-literature | 2023 Jan

REPOSITORIES: biostudies-literature