NSC-33994 (82058-16-0) is a remarkably potent and selective JAK2 inhibitor (IC50 = 60 nM). Displays no effect on Src and TYK2 tyrosine kinase activity at a concentration of 25 μM1. Suppresses JAK2-V617F-mediated human pathological cell growth in vitro and in vivo2 and is concomitant with the disruption of intracellular vimentin filaments3. NSC-33994 reduces the tumorigenic potential of T98G glioblastoma cells in vitro and in vivo4.
1) Kiss et al. (2009), Identification of a novel inhibitor of JAK2 tyrosine kinase by structure-based virtual screening; Bioorg. Med. Chem. Lett., 19 3598
2) Kirabo et al. (2011), The stilbenoid tyrosine kinase inhibitor, G6, suppresses Jak2-V617F-mediated human pathological cell growth in vitro and in vivo; J. Biol. Chem., 286 4280
3) Majumder et al. (2011), Cell death induced by the Jak2 inhibitor, G6, correlates with cleavage of vimentin filaments; Biochemistry, 50 7774
4) Baskin et al. (2014), The Jak2 small molecule inhibitor, G6, reduces the tumorigenic potential of T98G glipblastoma cells in vitro and in vivo; PLoS One, 9(8) e105568