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Cellagentech/BIRB796 (Doramapimod) | P38 MAPK inhibitor/C2796-5/5 mg (powder)188bio精品生物—专注于实验室精品爆款的电商平台 - 蚂蚁淘旗下精选188款生物医学科研用品
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Cellagentech/BIRB796 (Doramapimod) | P38 MAPK inhibitor/C2796-5/5 mg (powder)

ProductDescription

BIRB796(Doramapimod)isapyrazole-basedallostericinhibitorofp38MAPKinasewithaKdof0.1nM.BIRB796hasslowbindingkinetics,asevidencedbyanmarkedincreaseinapparentIC50afterpreincubationperiodsupto2h,aswellasdissociationratesofuptosixordersofmagnitudegreaterwhencomparedtootherMAPKinhibitors.(1)BIRB796possessesanexcellentselectivityprofileoverapanelofrelevantkinases,withthemostactivebeinginhibitionofJNK2a2at100nM(330-foldselectivity).(2)

RelatedstudieshaveshownthatBIRB796alsoinhibitsactivityandactivationofSAPK3/p38g(3%remainingactivityat10uM).Attheseconcentrations,BIRB796blocksstress-inducedphosphorylationofscaffoldproteinSAP97.(3)

Technicalinformation:

ChemicalFormula: C31H37N5O3
CAS#: 285983-48-4
MolecularWeight: 527.66
Purity: >98%
Appearance: White
ChemicalName: 1-(3-tert-butyl-1-p-tolyl-1H-pyrazol-5-yl)-3-(4-(2-morpholinoethoxy)naphthalen-1-yl)urea-Seemoreat:http://www.Selleckchem.com/products/BIRB-796-(Doramapimod).html#sthash.FpSrDH3J.dpuf
Solubility: Upto100mMinDMSO
Synonyms: BIRB796,BIRB796,Doramapimod

ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.

Reference:

1.Pargellisetal.,Inhibitionofp38MAPkinasebyutilizinganovelallostericbindingsite.Nat.Struct.Biol.2002,9(4),268-272.PubmedID:11896401
2.Reganetal.,PyrazoleUrea-BasedInhibitorsofp38MAPKinase:FromLeadCompoundtoClinicalCandidate.J.Med.Chem.2002,45,2994-3008.PubmedID:12086485
3.Kumaetal.,BIRB796InhibitsAllp38MAPKIsoformsinVitroandinVivo.J.Biol.Chem.2005,280(20),19472-19479.PubmedID:15755732

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