3-(1-Methylindol-3-ylmethylene)-2-oxo-2,3-dihydroindole-5-sulfonic acid amide

Description

Spleen tyrosine kinase (Syk) is a non-receptor tyrosine kinase that upon phosphorylation binds to immunoreceptor tyrosine-based activation motifs (ITAMs) of FcRγ chains and mediates downstream signaling related to platelet function and inflammation. Syk inhibitor is an oxindole compound that potently blocks Syk activity with an IC₅₀ value of 14 nM and inhibits FcεRI-mediated rat RBL-2H3 basophil cell degranulation (EC₅₀ = 313 nM). At 2 μM, this compound completely abolishes convulxin-induced platelet aggregation and shape change.

Uses

OXSI 2 is a Syk selective inhibitor.

References

[1] PAUL J. COX  et al. et al. Potent Small Molecule Inhibitors of Spleen Tyrosine Kinase (Syk).[J]. ChemInform, 2003, 34 51. DOI: 10.1002/chin.200351119
[2] KAMALA BHAVARAJU . Evaluation of [3-(1-methyl-1H-indol-3-yl-methylene)-2-oxo-2, 3-dihydro-1H-indole-5-sulfonamide] (OXSI-2), as a Syk-selective inhibitor in platelets[J]. European journal of pharmacology, 2008, 580 3: Pages 285-290. DOI: 10.1016/j.ejphar.2007.11.009