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. Synonyms: N-(5-(5-(4-Acetylpiperazine-1-carbonyl)-4-methoxy-2-methylphenylthio)thiazol-2-yl)-4-((3,3-dimethylbutan-2-ylamino)methyl)benzamide, N-(5-((3-((4-Acetylpiperazin-1-yl)carbonyl)-4-methyl-6-methoxyphenyl)thio)thiazol-2-yl)-4-(N-1,2-dimethylpropylaminomethyl)benzamide, BMS509744, EMT Inhibitor, IL-2-Inducible T Cell Kinase Inhibitor CAS No: 439575-02-7 Molecular Formula: C32H41N5O4S2 Molecular Weight: 623.8 Solubility: DMSO Primary Target: ITK Primary Target IC50: 19nM for ITK Storage and Stability: Lyophilized powder may be stored at -20C. Stable for 12 months after receipt at -20C. Reconstitute with sterile buffer or ddH2O. Aliquot to avoid repeated freezing and thawing. Store at -20C. 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.
Molecular Weight:
623.8
Purity:
97% (HPLC)
Form:
Pale yellow powder.
CAS Number:
[439575-02-7]
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