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506306 IKKε/TBK1 Inhibitor II, MRT67307 - CAS 1190378-57-4 - Calbiochem

A cell-permeable, potent, ATP-competitive, and reversible dual kinase inhibitor of TBK1/IKKε (IC₅₀ = 19 and 160 nM, respectively).

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Synonymes: TANK Binding Kinase 1/IKKinducible Inhibitor II, N-(3-(5-Cyclopropyl-2-(3-(morpholinomethyl)phenylamino)pyrimidin-4-ylamino)propyl)cyclobutanecarboxamide

Primary Target: TBK1 kinase dimer interface
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506306
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Tableau de caractéristiques principal

CAS #Empirical Formula
1190378-57-4C₂₆H₃₆N₆O₂

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      Description
      OverviewA cell-permeable BX795 analog (Cat. No. 204001) that acts as a potent, ATP-competitive, and reversible dual kinase inhibitor of TBK1/IKKε (IC50 = 19 and 160 nM, respectively) with excellent selectivity over IKKα and IKKβ (IC50 > 10 µM). Interacts with the TBK1 kinase dimer interface and stabilizes the inactive DFG-out conformation. Also blocks the activity of MARK (microtubule- associated protein (MAP)-microtubule affinity regulating kinase) 1, 2, 3, and 4 (IC50 = 27, 52, 36, and 41 nM, respectively), SIK2 (IC50 = 67 nM) and Aurora B, JAK2, and MLK1,3 (> than 90% inhibition at 1 µM) in a 108-kinase panel. Increases TNF-α-stimulated NF-κB-dependent gene transcription in wild-type macrophages and enhances CREB-dependent gene transcription by promoting dephosphorylation of CREB-regulated transcription coactivator (CRTC3). Shown to aid TLR-stimulated production of anti-Inflammatory cytokines in macrophages while suppressing the secretion of pro-inflammatory cytokines. In response to pro-inflammatory stimuli, pre-treatment of BX795 robustly suppresses the activation of JNK and p38α, whereas MRT67307 does not exhibit such off-target effects.

      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 and salt.
      Catalogue Number506306
      Brand Family Calbiochem®
      SynonymsTANK Binding Kinase 1/IKKinducible Inhibitor II, N-(3-(5-Cyclopropyl-2-(3-(morpholinomethyl)phenylamino)pyrimidin-4-ylamino)propyl)cyclobutanecarboxamide
      References
      ReferencesBruni, D., et al. 2013. J. Immunol. 190, 2844.
      Tu, D., et al. Cell Reports 3, 747.
      Larabi, A., et al. Cell Reports 3, 734.
      Clark, K., et al. 2012. Proc. Natl. Acad. Sci. USA 109, 16986.
      Clark, K., et al. 2011. Proc. Natl. Acad. Sci. USA 108, 17093.
      Clark, K., et al. 2011. Biochem. J. 434, 93.
      Product Information
      CAS number1190378-57-4
      FormAmber solid
      Hill FormulaC₂₆H₃₆N₆O₂
      Chemical formulaC₂₆H₃₆N₆O₂
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetTBK1 kinase dimer interface
      Secondary targetIKKe, MARK, SIK
      Purity≥95% 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 Ambient Temperature Only
      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
      Référence GTIN
      5063060001 04055977243253

      Documentation

      IKKε/TBK1 Inhibitor II, MRT67307 - CAS 1190378-57-4 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Références bibliographiques

      Aperçu de la référence bibliographique
      Bruni, D., et al. 2013. J. Immunol. 190, 2844.
      Tu, D., et al. Cell Reports 3, 747.
      Larabi, A., et al. Cell Reports 3, 734.
      Clark, K., et al. 2012. Proc. Natl. Acad. Sci. USA 109, 16986.
      Clark, K., et al. 2011. Proc. Natl. Acad. Sci. USA 108, 17093.
      Clark, K., et al. 2011. Biochem. J. 434, 93.
      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.

      Revision15-December-2017 JSW
      SynonymsTANK Binding Kinase 1/IKKinducible Inhibitor II, N-(3-(5-Cyclopropyl-2-(3-(morpholinomethyl)phenylamino)pyrimidin-4-ylamino)propyl)cyclobutanecarboxamide
      DescriptionA cell-permeable BX795 analog (Cat. No. 204001) that acts as a potent, ATP-competitive, and reversible dual kinase inhibitor of TBK1/IKKε (IC50 = 19 and 160 nM, respectively) with excellent selectivity over IKKα and IKKβ (IC50 > 10 µM). Interacts with the TBK1 kinase dimer interface and stabilizes the inactive DFG-out conformation. Also blocks the activity of MARK (microtubule- associated protein (MAP)-microtubule affinity regulating kinase) 1, 2, 3, and 4 (IC50 = 27, 52, 36, and 41 nM, respectively), SIK2 (IC50 = 67 nM) and Aurora B, JAK2, and MLK1,3 (> than 90% inhibition at 1 µM) in a 108-kinase panel. Increases TNF-α-stimulated NF-κB-dependent gene transcription in wild-type macrophages and enhances CREB-dependent gene transcription by promoting dephosphorylation of CREB-regulated transcription coactivator (CRTC3). Shown to aid TLR-stimulated production of anti-Inflammatory cytokines in macrophages while suppressing the secretion of pro-inflammatory cytokines. In response to pro-inflammatory stimuli, pre-treatment of BX795 robustly suppresses the activation of JNK and p38α, whereas MRT67307 does not exhibit such off-target effects.
      FormAmber solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1190378-57-4
      Chemical formulaC₂₆H₃₆N₆O₂
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (100 mg/m)
      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
      ReferencesBruni, D., et al. 2013. J. Immunol. 190, 2844.
      Tu, D., et al. Cell Reports 3, 747.
      Larabi, A., et al. Cell Reports 3, 734.
      Clark, K., et al. 2012. Proc. Natl. Acad. Sci. USA 109, 16986.
      Clark, K., et al. 2011. Proc. Natl. Acad. Sci. USA 108, 17093.
      Clark, K., et al. 2011. Biochem. J. 434, 93.