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

506306
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₆H₃₆N₆O₂ 1190378-57-4

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.06306.0001
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          Glass bottle 5 mg
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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®
          SynonymsN-(3-(5-Cyclopropyl-2-(3-(morpholinomethyl)phenylamino)pyrimidin-4-ylamino)propyl)cyclobutanecarboxamide, TANK Binding Kinase 1/IKKinducible Inhibitor II
          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
          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

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          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.
          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.

          Revision15-December-2017 JSW
          SynonymsN-(3-(5-Cyclopropyl-2-(3-(morpholinomethyl)phenylamino)pyrimidin-4-ylamino)propyl)cyclobutanecarboxamide, TANK Binding Kinase 1/IKKinducible Inhibitor II
          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 +2°C to +8°C
          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.
          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.