BiologicalActivity
High-affinityinhibitorofE3ubiquitinligaseVHL(Kd=80-90nM).BlocksinteractionbetweenVHLandHIF-αdownstreamofHIF-αhydroxylation,initiatinghypoxicresponse.Resultsintime-andconcentration-dependentaccumulationofhydroxylatedHIF-α,andupregulatesmRNAandproteinlevelsofHIFtargetgenes.Cellpermeable.NegativecontrolcisVH298alsoavailable.
LicensingInformation
SoldunderlicencefromtheUniversityofDundee
ExternalPortalInformation
Chemicalprobes.orgisaportalthatoffersindependentguidanceontheselectionand/orapplicationofsmallmoleculesforresearch.TheuseofVH298isreviewedontheChemicalProbeswebsite.
TechnicalData
| M.Wt | 523.65 |
| Formula | C27H33N5O4S |
| Storage | Storeat-20°C |
| Purity | ≥98%(HPLC) |
| PubChemID | 122199236 |
| InChIKey | NDVQUNZCNAMROD-RZUBCFFCSA-N |
| Smiles | O=C(N[C@@H](C(C)(C)C)C(N1C[C@@H](C[C@H]1C(NCC2=CC=C(C3=C(N=CS3)C)C=C2)=O)O)=O)C4(C#N)CC4 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 52.37 | 100 | |
| ethanol | 52.37 | 100 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight523.65.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 1.91mL | 9.55mL | 19.1mL |
| 5mM | 0.38mL | 1.91mL | 3.82mL |
| 10mM | 0.19mL | 0.95mL | 1.91mL |
| 50mM | 0.04mL | 0.19mL | 0.38mL |
MolarityCalculator
ReconstitutionCalculator
Thereconstitutioncalculatorallowsyoutoquicklycalculatethevolumeofareagenttoreconstituteyourvial.Simplyenterthemassofreagentandthetargetconcentrationandthecalculatorwilldeterminetherest.