Introduction:Basic information about CAS 622387-85-3|OXSI-2, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | OXSI-2 |
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| CAS Number | 622387-85-3 | Molecular Weight | 353.395 |
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| Density | 1.5±0.1 g/cm3 | Boiling Point | / |
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| Molecular Formula | C18H15N3O3S | Melting Point | / |
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| MSDS | / | Flash Point | / |
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Names
| Name | 3-[(1-methylindol-3-yl)methylidene]-2-oxo-1H-indole-5-sulfonamide |
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| Synonym | More Synonyms |
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OXSI-2 BiologicalActivity
| Description | OXSI-2 is a bioavailable, cell-permeable Syk inhibitor with an EC50 of 313 nM and an IC50 of 14 nM[1][2]. |
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| Related Catalog | Signaling Pathways >>Protein Tyrosine Kinase/RTK >>SykResearch Areas >>Inflammation/Immunology |
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| 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. |
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| 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. |
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Chemical & Physical Properties
| Density | 1.5±0.1 g/cm3 |
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| Molecular Formula | C18H15N3O3S |
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| Molecular Weight | 353.395 |
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| Exact Mass | 353.083405 |
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| PSA | 102.57000 |
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| LogP | 2.55 |
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| Index of Refraction | 1.730 |
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| InChIKey | MLKHXLFEYOOYEY-OVCLIPMQSA-N |
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| SMILES | Cn1cc(C=C2C(=O)Nc3ccc(S(N)(=O)=O)cc32)c2ccccc21 |
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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 |