BiologicalActivity
Saltinduciblekinase(SIK)inhibitor(IC50valuesare67,250and430nMforSIK2,SIK1andSIK3respectively).AlsoinhibitsTBK1,MARK1-4,IKKεandNUAK1(IC50valuesare19,27-52,160and230nMrespectively).HasnoeffectonIKKαorIKKβ.InducesIL-10secretionandinhibitsTNF-αandIL-6secretioninbacterialLPS-stimulatedmacrophages.AlsoenhancesIL-1-inducedactivationofNFκB-dependentgenetranscriptioninmouseembryonicfibroblast(MEF)cells.Inhibitsautophagy.
TechnicalData
| M.Wt | 537.52 |
| Formula | C26H36N6O2.2HCl |
| Storage | DesiccateatRT |
| Purity | ≥98%(HPLC) |
| PubChemID | 90489013 |
| InChIKey | ZIKXPHATVRPOQG-UHFFFAOYSA-N |
| Smiles | O=C(C5CCC5)NCCCNC1=C(C4CC4)C=NC(NC2=CC(CN3CCOCC3)=CC=C2)=N1.Cl.Cl |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 53.75 | 100 | |
| water | 10.75 | 20 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight537.52.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 1.86mL | 9.3mL | 18.6mL |
| 5mM | 0.37mL | 1.86mL | 3.72mL |
| 10mM | 0.19mL | 0.93mL | 1.86mL |
| 50mM | 0.04mL | 0.19mL | 0.37mL |
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ProductDatasheets
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