A cell-permeable, naphthalene based compound that acts as a narrow spectrum kinase inhibitor and reduces pro-inflammatory cytokine synthesis in LPS-activated primary human macrophages (IC50 = 0.63 and 1.66 nM for TNFα and IL-6), monocytes (IC50 = 0.97, 1.1, and 1.32 nM for TNFα, IL-6, and IL-8), and synovial fibroblasts (5.45 and 1.61 nM for IL-6 and IL-8). Shown to simultaneously inhibit the activity of p38α, p38γ, and Src (c-Src and Hck, and Syk). Also reported to inhibit antigen-induced release of beta-Hex, LTC4, and PGD2 (IC50 = 18, 11, and 21 nM, respectively) in cord blood derived mast cells.
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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target p-38α, p38γ, c-Src, Hck and SyK
Reversible: yes
Target IC50: 5.45 nM, 1.61 nM for IL-6, IL-8 inhibition respectively in activated rheumatoid arthritis synovial fibroblasts
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
To, W. S., et al. 2015. Br. J. Pharmacol.172, 3805.
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
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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