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438193 LRRK2-IN-1 - CAS 1234480-84-2 - Calbiochem

LRRK2-IN-1, CAS 1234480-84-2, is a cell-permeable, ATP competitive, selective LRRK2 inhibitor (IC50 = 13, 6 & 2.45 µM for WT, G2019S mutant & drug resistant A2016T mutant LRRK2, respectively).

LRRK2-IN-1 - CAS 1234480-84-2 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: LRRK2 Inhibitor I

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438193
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Overview

Key Spec Table

CAS #Empirical Formula
1234480-84-2C₃₁H₃₈N₈O₃

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      Description
      OverviewA cell-permeable, ATP competitive, potent, and selective LRRK2 inhibitor (IC50 of 13 nM, 6 nM, and 2.45 µM for wild type, G2019S mutant, and drug resistant A2016T mutant LRRK2, respectively, in an in vitro ATP-site competititon binding assay). While it is shown to inhibit DCLK2 (IC50 = 45 nM) and suppress MAPK7 autophosphorylation (EC50 = 160 nM), this compound (< 10 µM) demonstrates very good overall selectivity, targeting 12 out of 442 other kinases in a kinase-binding and biochemical assay. At 0.05–3 µM, it induces dose-dependent inhibition of Ser910 and Ser935 phosphorylation accompanied by loss of 14-3-3 binding to both wild-type LRRK2 and LRRK2[G2019S] in stably transfected HEK293 cells, but not in the drug-resistant LRRK2[A2016T] and LRRK2[A2016T + G2019S] mutants. Similar effects on endogenous LRRK2 phosphorylation and 14-3-3 binding can be observed in human lympho¬blastoid cells and for the LRRK2 G2019S mutant derived from a Parkinson's disease patient, and in human-derived neuroblastoma SHSY5Y cells, as well as in mouse Swiss 3T3 cells. 100 mg/kg of compound injected into mice elicits complete Ser910 and Ser935 dephosphorylation of LRRK2 in the kidney, but not in the brain which may result from an inability to penetrate the blood-brain barrier. In addition, it promotes relocalization of LRRK2 to more aggregate and fibrillar-like structures.
      Catalogue Number438193
      Brand Family Calbiochem®
      SynonymsLRRK2 Inhibitor I
      References
      ReferencesDeng, X., et al. 2011. Nat. Chem. Biol. 7, 203.
      Product Information
      CAS number1234480-84-2
      FormYellow-white to pale yellow powder
      Hill FormulaC₃₁H₃₈N₈O₃
      Chemical formulaC₃₁H₃₈N₈O₃
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      ApplicationLRRK2-IN-1, CAS 1234480-84-2, is a cell-permeable, ATP competitive, selective LRRK2 inhibitor (IC50 = 13, 6 & 2.45 µM for WT, G2019S mutant & drug resistant A2016T mutant LRRK2, respectively).
      Biological Information
      Purity≥95% by HPLC
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Regulatory Review
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freexe (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Global Trade Item Number
      Catalogue Number GTIN
      438193-5MG 07790788060954