Description | Leucine-RichRepeatKinase2(LRRK2)isamemberoftheleucine-richrepeatkinasefamily.MutationsintheLRRK2genehavebeenlinkedwithlate-onsetautosomaldominantParkinsonsdisease(PD).ArecentscreeningidentifiedtheanalogLRRK2-IN-1asapotentandselectiveinhibitorofLRRK2.ThisresearchbyDengetal(2011,NatChemBiol)showedthatLRRK2-IN-1suppressedLRRK2kinaseactivityinvivoleADIngtodephosphorylationofSer910/Ser935,lossof14-3-3bindingandaccumulationofLRRK2withinaggregratefibrillarstructures.LRRK2-IN-1,isthefirstselectiveandpotentinhibitorofLRRK2.LRRK2-IN-1inhibitsbothwild-typeandG2019SmutantLRRK2kinaseactivitywithIC50valuesof13nMand6nMrespectively(Dengetal2011,NatChemBiol). |
Relatedproducts | Leucine-RichRepeatKinase2inhibitorLRRK2-IN-1(10mg) |
BatchNo. | Seeproductlabel |
Unitsize | 5mg |
OtherNames | Protein:Leucine-richrepeatserine/threonine-proteinkinase2;Dardarin;LRRK2;PARK8 |
Accession | Q5S007LRRK2_HUMAN; |
MolecularWeight | 570.69g |
CompoundName | 2-((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.activity | LRRK2-IN-1inhibitsbothwild-typeandG2019SmutantLRRK2kinaseactivitywithIC50valuesof13nMand6nMrespectively(Dengetal2011,NatChemBiol). |
Applications | Biosensisrecommendsoptimaldilutions/concentrationsshouldbedeterminedbytheenduser. |
Appearance | Drypowder |
Storage | Storedry,unopenedvialprotectedfromlightforupto3monthsatRTorat-70ºCforupto1year.Reconstituteproductin100%ACSgradeDMSOandstoreat-80ºC,inaliquots,protectedfromlight,forupto1month.Preventmultiplefreeze-thawcycles.CASNumber1234480-84-2. |
ExpiryDate | Seestorageconditions |
SpecificReferences | 1.DengX.etal(2011)CharacterizationofaselectiveinhibitoroftheParkinson"sdiseasekinaseLRRK2NatChemBiol.2011Apr;7(4):203-5. |
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