BiologicalActivity
PotentandselectiveBRD1andTAF1inhibitor(IC50valuesare6-67and8-13nM,respectively).Displaysselectivityoverotherbromodomains(>30-foldoverothermembersoftheBRPFfamily;BRD9andATAD2;>300-foldoverBRD4).DisplaysBRD1andTAF1inhibitioninaNanoBRETcellassay.InhibitsbindingofBRD1andTAF1tohistoneH4(IC50valuesare575nMand0.9μM,respectively)andhistoneH3.3(IC50valuesare825nMand1.4μM,respectively).
LicensingInformation
ThisprobeissuppliedinconjunctionwiththeStructuralGenomicsConsortium.Forfurthercharacterizationdetails,pleasevisittheBAY299probesummaryontheSGCwebsite.
ExternalPortalInformation
Chemicalprobes.orgisaportalthatoffersindependentguidanceontheselectionand/orapplicationofsmallmoleculesforresearch.TheuseofBAY299isreviewedontheChemicalProbeswebsite.
TechnicalData
| M.Wt | 429.47 |
| Formula | C25H23N3O4 |
| Storage | Storeat-20°C |
| Purity | ≥98%(HPLC) |
| CASNumber | 2080306-23-4 |
| PubChemID | 122705990 |
| InChIKey | OFWWWKWUCDUISA-UHFFFAOYSA-N |
| Smiles | OCCCC1=CC=C(C(N2C3=C(C)C=C(N(C)C(N4C)=O)C4=C3)=O)C5=C1C=CC=C5C2=O |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 42.95 | 100 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight429.47.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.33mL | 11.64mL | 23.28mL |
| 5mM | 0.47mL | 2.33mL | 4.66mL |
| 10mM | 0.23mL | 1.16mL | 2.33mL |
| 50mM | 0.05mL | 0.23mL | 0.47mL |
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ProductDatasheets
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