82058-16-0

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 μM.1?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 vivo.4

NSC-33994 is novel inhibitor of JAK2 tyrosine kinase (Janus kinase 2 ). Janus kinase 2 (JAK2) plays a crucial role in the pathomechanism of myeloproliferative disorders and hematological malignancies.

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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 glioblastoma cells in vitro and in vivo; PLoS One,?9(8)?e105568