438193 LRRK2-IN-1 - Calbiochem

438193
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₃₁H₃₈N₈O₃

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      438193-5MG
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          Glass bottle 5 mg
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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
          FormYellow-white to pale yellow powder
          Hill FormulaC₃₁H₃₈N₈O₃
          Chemical formulaC₃₁H₃₈N₈O₃
          Structure formula ImageStructure formula Image
          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

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          438193

          References

          Reference overview
          Deng, X., et al. 2011. Nat. Chem. Biol. 7, 203.
          Data Sheet

          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
          Chemical formulaC₃₁H₃₈N₈O₃
          Structure formulaStructure formula
          Purity≥95% by HPLC
          SolubilityDMSO (50 mg/ml)
          Storage +2°C to +8°C
          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.
          Toxicity Regulatory Review
          ReferencesDeng, X., et al. 2011. Nat. Chem. Biol. 7, 203.