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533168 DLK Inhibitor, GNE-3511 - CAS 1496581-76-0 - Calbiochem

Dual Leucine Zipper Kinase Inhibitor, GNE-3511; DLK inhibitor, GNE-3511

SDB (Sicherheitsdatenblätter), Analysenzertifikate und Qualitätszertifikate, Dossiers, Broschüren und andere verfügbare Dokumente.

Synonyme: 2-((6-(3,3-Difluoropyrrolidin-1-yl)-4-(1-(oxetan-3-yl)piperidin-4-yl)pyridin-2-yl)amino)isonicotinonitrile, MAP3K12 Inhibitor, GNE-3511, Dual Leucine Zipper Kinase, GNE-3511, GNE3511, GNE 3511

Primary Target: DLK
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533168
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Übersicht

Replacement Information

Key Spec Table

CAS #Empirical Formula
1496581-76-0C₂₃H₂₆F₂N₆O

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      Description
      OverviewA cell-permeable, orally bioavailable, blood-brain barrier permeant 2,6-diaminopyridine based compound that acts as a highly potent and selective inhibitor of dual leucine zipper kinase inhibitor (DLK; Ki = 500 pM). Exhibits an ideal balance of metabolic stability, potency, and efflux properties. Displays high selectivity over JNK (IC50 = 129, 514, and 364 nM for JNK1, 2, and 3, respectively) and MLK (IC50 = 67.8, 767, and 602 nM for MLK1, 2, and 3, respectively). Does not affect the activities of MKK4 and MKK7 (IC50 >5 µM). Protects neurons in an in vitro axon degeneration assay (IC50 = 107 nM). Also shown to reduce levels of phosphorylated c-Jun in retina and offer protection in a 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MTPT) model of Parkinson's disease. Exhibits desirable pharmacokinetic properties (t1/2 = 0.6 h; CLp = 56 ml/min/kg in mice; 1 mg/kg, i.v., or 5 mg/kg; p.o.).

      Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
      Catalogue Number533168
      Brand Family Calbiochem®
      Synonyms2-((6-(3,3-Difluoropyrrolidin-1-yl)-4-(1-(oxetan-3-yl)piperidin-4-yl)pyridin-2-yl)amino)isonicotinonitrile, MAP3K12 Inhibitor, GNE-3511, Dual Leucine Zipper Kinase, GNE-3511, GNE3511, GNE 3511
      DescriptionDLK Inhibitor, GNE-3511
      References
      ReferencesPatel, S., et al. 2014. J. Med. Chem. 57, in press.
      Product Information
      CAS number1496581-76-0
      FormYellow solid
      Hill FormulaC₂₃H₂₆F₂N₆O
      Chemical formulaC₂₃H₂₆F₂N₆O
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetDLK
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-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
      Bestellnummer GTIN
      5331680001 04055977281484

      Documentation

      DLK Inhibitor, GNE-3511 - CAS 1496581-76-0 - Calbiochem SDB

      Titel

      Sicherheitsdatenblatt (SDB) 

      Literatur

      Übersicht
      Patel, S., et al. 2014. J. Med. Chem. 57, in press.
      Datenblatt

      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.

      Revision09-September-2016 JSW
      Synonyms2-((6-(3,3-Difluoropyrrolidin-1-yl)-4-(1-(oxetan-3-yl)piperidin-4-yl)pyridin-2-yl)amino)isonicotinonitrile, MAP3K12 Inhibitor, GNE-3511, Dual Leucine Zipper Kinase, GNE-3511, GNE3511, GNE 3511
      DescriptionA cell-permeable, orally bioavailable, blood-brain barrier permeant 2,6-diaminopyridine based compound that acts as a highly potent and selective inhibitor of dual leucine zipper kinase inhibitor (DLK; Ki = 500 pM). Exhibits an ideal balance of metabolic stability, potency, and efflux properties. Displays high selectivity over JNK (IC50 = 129, 514, and 364 nM for JNK1, 2, and 3, respectively) and MLK (IC50 = 67.8, 767, and 602 nM for MLK1, 2, and 3, respectively). Does not affect the activities of MKK4 and MKK7 (IC50 >5 µM). Protects neurons in an in vitro axon degeneration assay (IC50 = 107 nM). Also shown to reduce levels of phosphorylated c-Jun in retina and offer protection in a 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MTPT) model of Parkinson's disease. Exhibits desirable pharmacokinetic properties (t1/2 = 0.6 h; CLp = 56 ml/min/kg in mice; 1 mg/kg, i.v., or 5 mg/kg; p.o.).
      FormYellow solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1496581-76-0
      Chemical formulaC₂₃H₂₆F₂N₆O
      Purity≥98% by HPLC
      SolubilityDMSO (20 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesPatel, S., et al. 2014. J. Med. Chem. 57, in press.