ITK Inhibitor, BMS-509744 – CAS 439575-02-7 – Calbiochem

Descrição detalhada : A cell-permeable aminothioaryl-thiazolo compound that potently inhibits ITK kinase activity (IC50 = 19 nM; [ATP] = 1 M) 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 = 1.1, 1.1, 2.4, and 4.1 M, respectively) and exhibiting little or no activity against 14 other kinases (IC50 >=11 M). Inhibits ITK-dependent, but not ITK-independent, PLCgamma1 tyrosine phosphorylation (IC50<300 nM in alphaCD3-stimulated Jurkat T-cells) as well as downstream signaling events, including Ca2+ mobilization (IC50 = 52 nM in alphaCD3-stimulated Jurkat T-cells), IL-2 secretion (IC50 = 72, 250, 380, and 390 nM, respectively, in alphaCD3-stimulated EL4, Jurkat, murine splenocytes, and human PBMCs), and proliferation (IC50 = 430 nM against APC-induced primary human T-cell expansion). BMS-509744 is also efficacious in alleviating OVA (Cat. No. 32467) challenge-induced airway leukocytes infiltration (50% and 75% reduction, respectively, of total and eosinophil cell count; 25 mg/kg s.c.) in OVA- sensitized mice in vivo., A cell-permeable aminothioaryl-thiazolo compound that potently inhibits ITK kinase activity (IC50 = 19 nM; [ATP] = 1 M) 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 >=1.1 M) and exhibiting little or no activity against 14 other kinases (IC50 >=11 M). Inhibits ITK-dependent cellular signaling (IC50<300 nM against alphaCD3-stimulated PLCgamma1 Tyr phosphorylation and Ca2+ mobilization in Jurkat cells) in vitro and alleviate OVA (Cat. No. 32467) challenge-induced airway leukocytes infiltration (ED50 = 25 mg/kg s.c.) in OVA-sensitized mice in vivo.
Sinónimos : ITK Inhibitor, BMS-509744 - CAS 439575-02-7 - Calbiochem
Fórmula molecula r: C32H41N5O4S2
Armazenamento : -20C
Embalagem : 1X5MG