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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 : FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

Synonymes: LRRK2 Inhibitor I

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438193
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Tableau de caractéristiques principal

CAS #Empirical Formula
1234480-84-2C₃₁H₃₈N₈O₃

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438193-5MG
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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
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      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
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Référence GTIN
      438193-5MG 07790788060954

      Documentation

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

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      LRRK2-IN-1 - CAS 1234480-84-2 - Calbiochem Certificats d'analyse

      TitreNuméro de lot
      438193

      Références bibliographiques

      Aperçu de la référence bibliographique
      Deng, X., et al. 2011. Nat. Chem. Biol. 7, 203.
      Fiche technique

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision06-September-2011 RFH
      SynonymsLRRK2 Inhibitor I
      DescriptionA 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.
      FormYellow-white to pale yellow powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1234480-84-2
      Chemical formulaC₃₁H₃₈N₈O₃
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      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.
      Toxicity Regulatory Review
      ReferencesDeng, X., et al. 2011. Nat. Chem. Biol. 7, 203.