A cell-permeable aminothioaryl-thiazolo compound that potently inhibits ITK kinase activity (IC50 = 19nM; [ATP] = 1uM) in an ATP-competitive manner by stabilizing ITK activation loop in a substrate-blocking, inactive conformation, inhibiting Fyn, IR, Lck, Btk only at much higher concentrations (IC50 ≥1.1uM) and exhibiting little or no activity against 14 other kinases (IC50 ≥11uM). Inhibits ITK-dependent cellular signaling (IC50 <300nM against alphaCD3-stimulated PLC-gamma1 Tyr phosphorylation and Ca2+ mobilization in Jurkat cells) in vitro and alleviate OVA challenge-induced airway leukocytes infiltration (ED50 = 25mg/kg s.c.) in OVA-sensitized mice in vivo.
Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 12 months after receipt at -20°C. Reconstitute with sterile buffer or ddH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
