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 |