Fig. 1: Chemical structure of FM and highly selective inhibition of JAK2 in JAK family. | Blood Cancer Journal

Fig. 1: Chemical structure of FM and highly selective inhibition of JAK2 in JAK family.

From: Preclinical studies of Flonoltinib Maleate, a novel JAK2/FLT3 inhibitor, in treatment of JAK2V617F-induced myeloproliferative neoplasms

Fig. 1

A Chemical structure of FM. B Selectivity profile of FM against JAK family. C Surface plasmon resonance assay for monitoring the affinity of JAK2 JH1, JAK2 JH2, and JAK2 JH2V617F with FM. D Cocrystal structure of JAK2-JH2 domain (cartoon) in complex with FM (sticks). E Magnified view between JAK2-JH2 and FM. Hydrogen bonds are represented by yellow dashed lines. F Electron densities of FM (2Fo-Fc, gray mesh, contoured at 3σ). G Identification of FM as a highly selective JAK2 inhibitor. Cells were preliminarily treated with FM for 1 h, prior to treatment with IFN-γ, GM-CSF, and IFN-α for an additional 20–60 min in U2OS and TF-1 cell lines, and analyzed via western blotting.

Back to article page