BiologicalActivity
Potentandselective,ATP-competitiveglycogensynthasekinase-3(GSK-3)inhibitor(IC50=34.3nMforGSK-3α).EquallyeffectiveatinhibitinghumanGSK-3αandGSK-3β.Exhibitsminimalactivityagainst24otherproteinkinases(IC50>10μM).Stimulatesglycogensynthesisinlivercells,andinducesβ-catenin-dependentgenetranscription.Neuroprotective;alsoreducespulmonaryinflammationandfibrosisinamousemodel.Showntomaintainmouseembryonicstemcellsinapluripotentstate.
LicensingInformation
SoldforresearchpurposesunderagreementfromGlaxoSmithKline
TechnicalData
| M.Wt | 371.22 |
| Formula | C19H12Cl2N2O2 |
| Storage | StoreatRT |
| Purity | ≥98%(HPLC) |
| CASNumber | 280744-09-4 |
| PubChemID | 176158 |
| InChIKey | JCSGFHVFHSKIJH-UHFFFAOYSA-N |
| Smiles | CN1C=C(C2=CC=CC=C12)C1=C(C(=O)NC1=O)C1=C(Cl)C=C(Cl)C=C1 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 27.84 | 75 | |
| ethanol | 0.48 | 1.3 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight371.22.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.69mL | 13.47mL | 26.94mL |
| 5mM | 0.54mL | 2.69mL | 5.39mL |
| 10mM | 0.27mL | 1.35mL | 2.69mL |
| 50mM | 0.05mL | 0.27mL | 0.54mL |
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