MilliporeSigma™ Calbiochem™ ITK Inhibitor, BMS-509744

Description

A cell-permeable aminothioaryl-thiazolo compound that potently inhibits ITK kinase activity (IC₅₀ = 19nM; [ATP] = 1μM) 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

A cell-permeable aminothioaryl-thiazolo compound that potently inhibits ITK kinase activity (IC₅₀ = 19nM; [ATP] = 1μM) 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 ≥1.1μM) and exhibiting little or no activity against 14 other kinases (IC₅₀ ≥11μM). Inhibits ITK-dependent cellular signaling (IC₅₀ <300nM against αCD3-stimulated PLCγ1 Tyr phosphorylation and Ca²⁺ mobilization in Jurkat cells) in vitro and alleviate OVA (Cat. No. 32467) challenge-induced airway leukocytes infiltration (ED₅₀ = 25mg/kg s.c.) in OVA-sensitized mice in vivo .

Specifications

• Color: Pale Yellow
• Description: 97% by HPLC
• Target Proteins: ITK
• CAS: 439575-02-7
• Molecular Formula: C₃₂H₄₁N₅O₄S₂
• Formula Weight: 623.8g/mol
• Solubility: DMSO
• Content And Storage: Protect from light
• Form: Powder
• Quantity: 5 mg