OXSI-2

Names

[ Name ]:
OXSI-2

[Synonym ]:
1H-Indole-5-sulfonamide, 2,3-dihydro-3-[(1-methyl-1H-indol-3-yl)methylene]-2-oxo-, (3Z)-
3-(1-Methylindol-3-ylmethylene)-2-oxo-2,3-dihydroindole-5-sulfonic acid amide
oxsi 2
(3Z)-3-[(1-Methyl-1H-indol-3-yl)methylene]-2-oxo-5-indolinesulfonamide
in1070
(3Z)-3-[(1-methyl-1H-indol-3-yl)methylidene]-2-oxo-2,3-dihydro-1H-indole-5-sulfonamide

Biological Activity

[Description]:

OXSI-2 is a bioavailable, cell-permeable Syk inhibitor with an EC50 of 313 nM and an IC50 of 14 nM[1][2].

[Related Catalog]:

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Syk

Research Areas >> Inflammation/Immunology

[In Vitro]

OXSI-2 (2 μM) completely inhibits Convulxin-induced platelet aggregation and shape change. OXSI-2 (2 μM) also completely blocks GPVI-mediated dense granule release. OXSI-2 (100 nM) does not affect the platelet functional responses induced by Convulxin, and modest shape change is still evident at 1 μM[1]. Adaptor protein LAT is a known substrate of Syk Kinase. OXSI-2 completely inhibits LAT Y191 phosphorylation. OXSI-2 inhibits Syk mediated events in platelets[1]. OXSI-2 (2 μM) inhibits inflammasome assembly, caspase-1 activation, IL-1β processing and release, mitochondrial ROS generation, and pyroptotic cell death[2]. Western Blot Analysis[1] Cell Line: Aspirin-treated, washed human platelets Concentration: 2 μM Incubation Time: Result: Completely inhibited Syk-mediated LAT Y191 phosphorylation.

[References]

[1]. Kamala Bhavaraju, et al. 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. Eur J Pharmacol. 2008 Feb 12;580(3):285-90.

[2]. Jordan R Yaron, et al. The oxindole Syk inhibitor OXSI-2 blocks nigericin-induced inflammasome signaling and pyroptosis independent of potassium efflux. Biochem Biophys Res Commun. 2016 Apr 8;472(3):545-50.

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Molecular Formula ]:
C₁₈H₁₅N₃O₃S

[ Molecular Weight ]:
353.395

[ Exact Mass ]:
353.083405

[ PSA ]:
102.57000

[ LogP ]:
2.55

[ Index of Refraction ]:
1.730

Related Compounds

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