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Biosensis/Leucine-Rich Repeat Kinase 2 inhibitor LRRK2-IN-1 (5mg)/PE-1608-5/5mg

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¥5340.00
货号:PE-1608-5
浏览量:127
品牌:Biosensis
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商品描述
DescriptionLeucine-RichRepeatKinase2(LRRK2)isamemberoftheleucine-richrepeatkinasefamily.MutationsintheLRRK2genehavebeenlinkedwithlate-onsetautosomaldominantParkinson’sdisease(PD).ArecentscreeningidentifiedtheanalogLRRK2-IN-1asapotentandselectiveinhibitorofLRRK2.ThisresearchbyDengetal(2011,NatChemBiol)showedthatLRRK2-IN-1suppressedLRRK2kinaseactivityinvivoleADIngtodephosphorylationofSer910/Ser935,lossof14-3-3bindingandaccumulationofLRRK2withinaggregratefibrillarstructures.LRRK2-IN-1,isthefirstselectiveandpotentinhibitorofLRRK2.LRRK2-IN-1inhibitsbothwild-typeandG2019SmutantLRRK2kinaseactivitywithIC50valuesof13nMand6nMrespectively(Dengetal2011,NatChemBiol).
RelatedproductsLeucine-RichRepeatKinase2inhibitorLRRK2-IN-1(10mg)
BatchNo.Seeproductlabel
Unitsize5mg
OtherNamesProtein:Leucine-richrepeatserine/threonine-proteinkinase2;Dardarin;LRRK2;PARK8
AccessionQ5S007LRRK2_HUMAN;
MolecularWeight570.69g
CompoundName2-((2-Methoxy-4-(4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl)phenyl)amino)-5,11-dimethyl-5H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6(11H)-one
Purity>97%byHPLC
Biol.activityLRRK2-IN-1inhibitsbothwild-typeandG2019SmutantLRRK2kinaseactivitywithIC50valuesof13nMand6nMrespectively(Dengetal2011,NatChemBiol).
ApplicationsBiosensisrecommendsoptimaldilutions/concentrationsshouldbedeterminedbytheenduser.
AppearanceDrypowder
StorageStoredry,unopenedvialprotectedfromlightforupto3monthsatRTorat-70ºCforupto1year.Reconstituteproductin100%ACSgradeDMSOandstoreat-80ºC,inaliquots,protectedfromlight,forupto1month.Preventmultiplefreeze-thawcycles.CASNumber1234480-84-2.
ExpiryDateSeestorageconditions
SpecificReferences1.DengX.etal(2011)CharacterizationofaselectiveinhibitoroftheParkinson"sdiseasekinaseLRRK2NatChemBiol.2011Apr;7(4):203-5.