BiologicalActivity
PanJumonjihistonedemethylaseinhibitor(IC50valuesare230,340,435,445,855and1100nMforJARID1A,JMJD2E,JMJD2B,JMJD2A,JMJD3andJMJD2Crespectively).ExhibitsnegligIBLeactivityatPHD2andTET1.SelectivelyblockscancercellgrowthinvitroanddiminishestumorgrowthinH358andA549mousexenograftmodelsinvivo.Prolongssurvivalinamousemodelofbreastcancer.
CompoundLibraries
JIB04isalsoofferedaspartoftheTocriscreenPlusandTocriscreenEpigeneticsToolbox.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 308.76 |
| Formula | C17H13ClN4 |
| Storage | Storeat+4°C |
| Purity | ≥99%(HPLC) |
| CASNumber | 199596-05-9 |
| PubChemID | 6519698 |
| InChIKey | YHHFKWKMXWRVTJ-OQKWZONESA-N |
| Smiles | ClC(C=C3)=CN=C3N/N=C(C2=CC=CC=C2)/C1=CC=CC=N1 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 30.88 | 100 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight308.76.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 3.24mL | 16.19mL | 32.39mL |
| 5mM | 0.65mL | 3.24mL | 6.48mL |
| 10mM | 0.32mL | 1.62mL | 3.24mL |
| 50mM | 0.06mL | 0.32mL | 0.65mL |
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