BiologicalActivity
PotentinhibitoroftheH3K27histonedemethylasesJMJD3(KDM6B)andUTX(KDM6A)(IC50valuesare28and53nMrespectively).AlsoinhibitsKDM5B,KDM5CandKDM5A(IC50valuesare170,550and6,800nMrespectively).Exhibitsnoactivityagainstapanelofotherhistonedemethylases(IC50>20μM),anddisplaysnosignificantinhibitoryactivityagainst100proteinkinasesataconcentrationof30μM.Ethylesterderivativealsoavailable.
LicensingInformation
ThisprobeissuppliedinconjunctionwiththeStructuralGenomicsConsortium.Forfurthercharacterizationdetails,pleasevisittheGSKJ1probesummaryontheSGCwebsite.
CompoundLibraries
GSKJ1isalsoofferedaspartoftheTocriscreenPlusandTocriscreenEpigeneticsToolbox.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 389.45 |
| Formula | C22H23N5O2 |
| Storage | DesiccateatRT |
| Purity | ≥99%(HPLC) |
| CASNumber | 1373422-53-7 |
| PubChemID | 56963315 |
| InChIKey | AVZCPICCWKMZDT-UHFFFAOYSA-N |
| Smiles | O=C(CCNC1=NC(C2=CC=CC=N2)=NC(N3CCC(C=CC=C4)=C4CC3)=C1)O |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 38.94 | 100 | |
| ethanol | 38.94 | 100 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight389.45.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.57mL | 12.84mL | 25.68mL |
| 5mM | 0.51mL | 2.57mL | 5.14mL |
| 10mM | 0.26mL | 1.28mL | 2.57mL |
| 50mM | 0.05mL | 0.26mL | 0.51mL |
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ProductDatasheets
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