ZM39923

ZM 39923 is an inhibitor of JAK3 (IC₅₀ = 79 nM) that less potently inhibits epidermal growth factor receptor, JAK1, and cyclin-dependent kinase 4 (IC₅₀s = 2.4, 40, and 10 ?M, respectively).¹ In the absence of the reducing agent dithiothreitol, ZM 39923 also inhibits human tissue transglutaminase 2 (TGM2) and the transglutaminase Factor XIIIa (IC₅₀s= 10 and 25 nM, respectively).² It breaks down in neutral buffer to form ZM 449829, which is also an inhibitor of JAK3, TGM2, and Factor XIIIa.^1,2

1.Brown, G.R., Bamford, A.M., Bowyer, J., et al.Naphthyl ketones: A new class of Janus kinase 3 inhibitorsBioorg. Med. Chem. Lett.10(6)575-579(2000) 2.Lai, T.-S., Liu, Y., Tucker, T., et al.Identification of chemical inhibitors to human tissue transglutaminase by screening existing drug librariesChem. Biol.15(9)969-978(2008)