JAK3 Inhibitor VIII; NSC114792

General description

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 µM) in BaF3-JAK3^V674A and BLNK^-/- BKO84 culltures. Shown to prevent the JAK3-dependent survival of L540, BaF3-JAK3^WT, BaF3-JAK3^V674A, and BLNK^-/- BKO84 cells in a time- and dose-dependent manner (by 40%, 50%, 57%, and 85%, respectively, after 72 h incubation with 20 µM 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 µM) in BaF3-JAK3^V674A and BLNK^-/- BKO84 culltures. Shown to prevent the JAK3-dependent survival of L540, BaF3-JAK3^WT, BaF3-JAK3^V674A, and BLNK^-/- BKO84 cells (by 40%, 50%, 57%, and 85%, respectively; 20 µM; 72 h), while exhibiting no effect against the JAK3-independent growth in DU145, HDLM-2, and MDA-MB-468 cultures.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Kim, B.H., et al. 2010. Mol. Cancer9, 36.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Warning

Toxicity: Standard Handling (A)