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Beschreibung

A cell-permeable steroidal-purinethione compound that targets JAK3 kinase domain and selectively inhibits JAK3, but not JAK1, JAK2, or TYK2, activity in cell-free immuncomplex kinase assays, and effectively blocks the constitutive Jak3 and STAT5 phosphorylations (complete inhibition at 10 µ,M) in BaF3-JAK3V674A and BLNK-/- BKO84 culltures. Shown to prevent the JAK3-dependent survival of L540, BaF3-JAK3WT, BaF3-JAK3V674A, and BLNK-/- BKO84 cells in a time- and dose-dependent manner (by 40%, 50%, 57%, and 85%, respectively, after 72 h incubation with 20 µ,M inhibitor), while exhibiting no effect against the JAK3-independent growth in DU145, HDLM-2, and MDA-MB-468 cultures., A cell-permeable steroidal-purinethione that targets JAK3 kinase domain and selectively inhibits JAK3, but not JAK1, JAK2, or TYK2, activity and effectively blocks the constitutive Jak3 and STAT5 phosphorylations (complete inhibition at 10 µ,M) in BaF3-JAK3V674A and BLNK-/- BKO84 culltures. Shown to prevent the JAK3-dependent survival of L540, BaF3-JAK3WT, BaF3-JAK3V674A, and BLNK-/- BKO84 cells (by 40%, 50%, 57%, and 85%, respectively, 20 µ,M, 72 h), while exhibiting no effect against the JAK3-independent growth in DU145, HDLM-2, and MDA-MB-468 cultures.