BiologicalActivity
PotentandselectiveBRD4bromodomaininhibitor(Ki=30-50nMforthefirstbromodomain(BRD4(1)).Exhibits10-foldselectivityforBRD4(1)overBRD4(2).BlocksBRD4transcriptionalactivityinlipopolysaccharide-inducedproductionofbothnitricoxideandIL-6inmousemacrophages(IC50valuesare3.8and4.9μM,respectively).Attenuatesmelanomacellproliferationinvitro.
LicensingInformation
SoldunderlicensefromIcahnSchoolofMedicineatMountSinai.
CompoundLibraries
MS436isalsoofferedaspartoftheTocriscreenEpigeneticsToolbox.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 383.42 |
| Formula | C18H17N5O3S |
| Storage | Storeat-20°C |
| Purity | ≥98%(HPLC) |
| CASNumber | 1395084-25-9 |
| PubChemID | 60171585 |
| InChIKey | BBJDRANVVNBXAR-JWGURIENSA-N |
| Smiles | NC1=C(/N=N/C2=CC=C(S(NC3=NC=CC=C3)(=O)=O)C=C2)C=C(C)C(O)=C1 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 38.31 | 100 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight383.42.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.61mL | 13.04mL | 26.08mL |
| 5mM | 0.52mL | 2.61mL | 5.22mL |
| 10mM | 0.26mL | 1.3mL | 2.61mL |
| 50mM | 0.05mL | 0.26mL | 0.52mL |
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ProductDatasheets
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