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Leucine-Rich Repeat Kinase 2 inhibitor LRRK2-IN-1 (10mg)

$457.00USD


Catalogue No. PE-1608-10
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 Parkinson’s 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).
Batch No. See product label
Unit size 10mg
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 Parkinson's disease kinase LRRK2 Nat Chem Biol. 2011 Apr;7(4):203-5.
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Leucine-Rich Repeat Kinase 2 inhibitor LRRK2-IN-1 (10mg)


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