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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).

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 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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Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
1190378-57-4C₂₆H₃₆N₆O₂

Products

Catalog NumberPackaging Qty/Pack
5.06306.0001 Glass bottle 5 mg
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
Catalog Number GTIN
5.06306.0001 04055977243253

Documentation

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