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

Description	Leucine-Rich Repeat Kinase 2 (LRRK2) is a member of the leucine-rich repeat kinase family. Mutations in the LRRK2 gene have been linked with late-onset autosomal dominant Parkinsons disease (PD). A recent screening identified the analog LRRK2-IN-1 as a potent and selective inhibitor of LRRK2. This research by Deng et al (2011, Nat Chem Biol) showed that LRRK2-IN-1 suppressed LRRK2 kinase activity in vivo leading to dephosphorylation of Ser910/Ser935, loss of 14-3-3 binding and accumulation of LRRK2 within aggregrate fibrillar structures. LRRK2-IN-1, is the first selective and potent inhibitor of LRRK2. LRRK2-IN-1 inhibits both wild-type and G2019S mutant LRRK2 kinase activity with IC50 values of 13nM and 6nM respectively (Deng et al 2011, Nat Chem Biol).
Related products	Leucine-Rich Repeat Kinase 2 inhibitor LRRK2-IN-1 (10mg)
Batch No.	See product label
Unit size	5mg
Other Names	Protein: Leucine-rich repeat serine/threonine-protein kinase 2; Dardarin; LRRK2; PARK8
Accession	Q5S007 LRRK2_HUMAN;
Molecular Weight	570.69g
Compound Name	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% by HPLC
Biol. activity	LRRK2-IN-1 inhibits both wild-type and G2019S mutant LRRK2 kinase activity with IC50 values of 13nM and 6nM respectively (Deng et al 2011, Nat Chem Biol).
Applications	Biosensis recommends optimal dilutions/concentrations should be determined by the end user.
Appearance	Dry powder
Storage	Store dry, unopened vial protected from light for up to 3 months at RT or at -70ºC for up to 1 year. Reconstitute product in 100% ACS grade DMSO and store at -80ºC, in aliquots, protected from light, for up to 1 month. Prevent multiple freeze-thaw cycles. CAS Number 1234480-84-2.
Expiry Date	See storage conditions
Specific References	1. Deng X. et al (2011) Characterization of a selective inhibitor of the Parkinsons disease kinase LRRK2 Nat Chem Biol. 2011 Apr;7(4):203-5.

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