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| 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)CharacterizationofaselectiveinhibitoroftheParkinsonsdiseasekinaseLRRK2NatChemBiol.2011Apr;7(4):203-5. |