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475964 MK-2 Inhibitor IV, MK-25 - Calbiochem

475964
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₂₇H₂₅ClN₄O₂, HCl

Products

Catalogue NumberPackaging Qty/Pack
475964-10MG Glass bottle 10 mg
Description
OverviewA cell-permeable furanylcarboxamide compound that acts as a potent, reversible and non-ATP-competitive inhibitor of MK-2/MAPKAP-K2 activity (IC50 = 110 nM; EC50 = 350 nM for pHSP27 in IL-1β-stimulated SW1353 cells) with excellent selectivity over 150 kinases (% activity inhibition at 10 µM against human CK2, Haspin, Arg and CK1γ3 = 40, 40, 42 and > 70, respectively). Shown to efficiently suppress the secretions of TNFα, IL6 (IC50 = 4.4 and 5.2 µM in LPS-stimulated THP1 cell, respectively) and MMP-13 (IC50 = 5.7 and 2.2 µM in IL1β-stimulated SW1353 and in primary osteoarthritis-derived chondrocytes, respectively). Exhibits desirable bioavailability and weakly inhibits a panel of cytochrome P450 isozymes (IC50 > 20 µM for 3A4, 2D6 and 2C9).
Catalogue Number475964
Brand Family Calbiochem®
Synonyms5-(4-Chlorophenyl)-N-(4-(piperazin-1-yl)phenyl)-N-(pyridin-2-ylmethyl)furan-2-carboxamide, HCl, MAPKAP-K2 Inhibitor IV, MK-25
References
ReferencesHuang, X., et al. 2011. ACS Med. Chem. Lett. 2, 632.
Product Information
FormBeige solid
Hill FormulaC₂₇H₂₅ClN₄O₂, HCl
Chemical formulaC₂₇H₂₅ClN₄O₂, HCl
Hygroscopic Hygroscopic
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥95% by HPLC
Physicochemical Information
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 Regulatory Review
Storage -20°C
Protect from Light Protect from light
Hygroscopic Hygroscopic
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications

Documentation

MK-2 Inhibitor IV, MK-25 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

MK-2 Inhibitor IV, MK-25 - Calbiochem Certificates of Analysis

TitleLot Number
475964

References

Reference overview
Huang, X., et al. 2011. ACS Med. Chem. Lett. 2, 632.
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.

Revision28-September-2012 JSW
Synonyms5-(4-Chlorophenyl)-N-(4-(piperazin-1-yl)phenyl)-N-(pyridin-2-ylmethyl)furan-2-carboxamide, HCl, MAPKAP-K2 Inhibitor IV, MK-25
DescriptionA cell-permeable furanylcarboxamide compound that acts as a potent, reversible and non-ATP-competitive inhibitor of MK-2/MAPKAP-K2 activity (IC50 = 110 nM; EC50 = 350 nM for pHSP27 in IL-1β-stimulated SW1353 cells) with excellent selectivity over 150 kinases (% activity inhibition at 10 µM against human CK2, Haspin, Arg and CK1γ3 = 40, 40, 42 and > 70, respectively). Shown to efficiently suppress the secretions of TNFα, IL6 (IC50 = 4.4 and 5.2 µM in LPS-stimulated THP1 cell, respectively) and MMP-13 (IC50 = 5.7 and 2.2 µM in IL1β-stimulated SW1353 and in primary osteoarthritis-derived chondrocytes, respectively). Exhibits desirable bioavailability and weakly inhibits a panel of cytochrome P450 isozymes (IC50 > 20 µM for 3A4, 2D6 and 2C9).
FormBeige solid
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₂₇H₂₅ClN₄O₂, HCl
Structure formulaStructure formula
Purity≥95% by HPLC
SolubilityDMSO (25 mg/ml)
Storage -20°C
Hygroscopic
Protect from light
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity Regulatory Review
ReferencesHuang, X., et al. 2011. ACS Med. Chem. Lett. 2, 632.