622387-85-3

622387-85-3 structure

Name: OXSI-2
Chemical Name: 3-[(1-methylindol-3-yl)methylidene]-2-oxo-1H-indole-5-sulfonamide
CAS Number: 622387-85-3
Molecular Formula: C₁₈H₁₅N₃O₃S
Molecular Weight: 353.395
Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK Syk
Create Date: 2018-10-04 07:26:07
Modify Date: 2024-01-04 19:38:06
OXSI-2 is a bioavailable, cell-permeable Syk inhibitor with an EC50 of 313 nM and an IC50 of 14 nM[1][2].

Name	3-[(1-methylindol-3-yl)methylidene]-2-oxo-1H-indole-5-sulfonamide
Synonyms	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

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.