BiologicalActivity
Highaffinityandselectivecell-permeablep300/CBP-associatedfactor(PCAF)inhibitor(Ki=47nM).Exhibitsnosignificantactivityagainstapanelof48otherbromodomainsexceptGCN5(Kd=600nM).Exhibits>4500-foldselectivityforPCAFoverBRD4.AlsoexhibitsmetabolicstABIlityinmouseandhumanlivermicrosomesandnoobservablecytotoxicityinperipheralbloodmononuclearcells(PBMC).
LicensingInformation
ThiscompoundissuppliedinconjunctionwiththeStructuralGenomicsConsortium.Forfurthercharacterizationdetails,pleasevisittheL-MosesprobesummaryontheSGCwebsite.
TechnicalData
| M.Wt | 433.38 |
| Formula | C21H24N6.2HCl |
| Storage | DesiccateatRT |
| Purity | ≥98%(HPLC) |
| Smiles | C[C@@H]([C@H](C1=CC=CC=C1)N(C)C)NC2=NN3C(C)=NN=C3C4=CC=CC=C24 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solubility | Solubleto100mMinwaterandto100mMinDMSO |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight433.38.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.31mL | 11.54mL | 23.07mL |
| 5mM | 0.46mL | 2.31mL | 4.61mL |
| 10mM | 0.23mL | 1.15mL | 2.31mL |
| 50mM | 0.05mL | 0.23mL | 0.46mL |
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