BiologicalActivity
β-TrCP1ligaseinhibitor.InhibitsIκBαubiquitination(IC50=5.2μM)withoutaffectingproteasomeactivity.BlocksLPS-inducedexpressionofinflammatorycytokinesinhumanmyelomonocyticcells.Suppressesantigen-inducedNFκBexpression,inflammationandmucusproductioninairwaysofOVA-sensitizedmice.
CompoundLibraries
GS143isalsoofferedaspartoftheTocriscreenPlus.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 466.46 |
| Formula | C28H19FN2O4 |
| Storage | Storeat+4°C |
| Purity | ≥98%(HPLC) |
| CASNumber | 916232-21-8 |
| PubChemID | 11963988 |
| InChIKey | IZPMWFSVTDOCDI-QJOMJCCJSA-N |
| Smiles | FC1=CC=CC=C1C2=CC=C(/C=C3C(CC4=CC=CC=C4)=NN(C5=CC=C(C(O)=O)C=C5)C3=O)O2 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 46.65 | 100 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight466.46.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.14mL | 10.72mL | 21.44mL |
| 5mM | 0.43mL | 2.14mL | 4.29mL |
| 10mM | 0.21mL | 1.07mL | 2.14mL |
| 50mM | 0.04mL | 0.21mL | 0.43mL |
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