The MK-2 Inhibitor IV, MK-25 controls the biological activity of MK-2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
Synonym(s):
5-(4-Chlorophenyl)-N-(4-(piperazin-1-yl)phenyl)-N-(pyridin-2-ylmethyl)furan-2-carboxamide, HCl, MAPKAP-K2 Inhibitor IV, MK-25
OK to freeze desiccated (hygroscopic) protect from light
color
beige
solubility
DMSO: 25 mg/mL
shipped in
ambient
storage temp.
−20°C
General description
A 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).
Packaging
Packaged under inert gas
Warning
Toxicity: Regulatory Review (Z)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Huang, X., et al. 2011. ACS Med. Chem. Lett.2, 632.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Regulatory Listings
Regulatory Listings are mainly provided for chemical products. Only limited information can be provided here for non-chemical products. No entry means none of the components are listed. It is the user’s obligation to ensure the safe and legal use of the product.
JAN Code
475964-MG: 475964-10MG:
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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