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

Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
1496581-76-0C₂₃H₂₆F₂N₆O

Products

Catalog NumberPackaging Qty/Pack
5.33168.0001 Glass bottle 10 mg
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®
SynonymsMAP3K12 Inhibitor, GNE-3511, Dual Leucine Zipper Kinase, GNE-3511, GNE3511, GNE 3511, 2-((6-(3,3-Difluoropyrrolidin-1-yl)-4-(1-(oxetan-3-yl)piperidin-4-yl)pyridin-2-yl)amino)isonicotinonitrile
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
Catalog Number GTIN
5.33168.0001 04055977281484

Documentation

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

Title

Safety Data Sheet (SDS) 

References

Reference overview
Patel, S., et al. 2014. J. Med. Chem. 57, in press.
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.

Revision09-September-2016 JSW
SynonymsMAP3K12 Inhibitor, GNE-3511, Dual Leucine Zipper Kinase, GNE-3511, GNE3511, GNE 3511, 2-((6-(3,3-Difluoropyrrolidin-1-yl)-4-(1-(oxetan-3-yl)piperidin-4-yl)pyridin-2-yl)amino)isonicotinonitrile
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.