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PD-98059isanoxanaphthalenone-basedinhibitorofMAPK-activatingenzyme,MAPK/ERKkinase(MEK),withoutsignificantinhibitoryactivityofMAPKitself.[1]PD-98059doesnotinhibitRaf-activatedMAPKK1,butratherpreventsactivationofMAPKK1byRaforMEKkinaseinvitroatIC50valuesof2-7uM.[2]
ExposureofMCF10Ahumanbreastepithelialcellsresultedinarapidlossofduallyphosphorylatedformsofextracellularsignal-regulatedkinaseatanIC50of1uM.PD-98059isbelievedtobealigandforthearylhydrocarbonreceptor(AHR)andfunctionsasanAHRantagoNISTatconcentrationscommonlyusedtoinhibitMEKatthesignallingprocessesthatentailMEKactivation.[3]
PD-98059hasalsobeenshowntodramaticallyreducehypoxia-inducedtranscriptionofHRE-drivenreportergenemoresothanthatofendogenousVEGFandEPO.[4]
Technicalinformation:
| ChemicalFormula: | C16H13NO3 | |
| CAS#: | 167869-21-8 | |
| MolecularWeight: | 267.28 | |
| Purity: | >98% | |
| Appearance: | Yellow | |
| ChemicalName: | 2-(2-amino-3-methoxyphenyl)-4H-chromen-4-one | |
| Solubility: | Upto75mMinDMSO | |
| Synonyms: | PD-98059,PD98059,PD98059 |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
Reference:
| 1. | Dudleyetal.,Asyntheticinhibitorofthemitogen-activatedproteinkinasecascade.Proc.Natl.Acad.Sci.1995,92(17),7686-7689.PubmedID:7644477 |
| 2. | Alessietal.,PD098059isaspecificinhibitoroftheactivationofmitogen-activatedproteinkinasekinaseinvitroandinvivo.J.Biol.Chem.1995,270(46),27489-27494.PubmedID:7499206 |
| 3. | Reinersetal.,PD98059isanequipotentantagonistofthearylhydrocarbonreceptorandinhibitorofmitogen-activatedproteinkinasekinase.Mol.Pharmacol.1998,53(3),438-445.PubmedID:9495809 |
| 4. | Huretal.,Mitogen-activatedproteinkinasekinaseinhibitorPD98059blocksthetrans-activationbutnotthestABIlizationorDNAbindingabilityofhypoxia-inducIBLefactor-1alpha.Mol.Pharmacol.2001,59(5),1216-1224.PubmedID:7499206 |
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