A cell-permeable, chromene-fused benzopyran-embedded tetracyclic compound that selectively and directly binds to the DNA binding domain box A of high mobility group box (HMGB) proteins and blocks their post-translational phosphorylation and acetylation. Diminishes the cytoplasmic accumulation of HMGB2 in microglial cells. Blocks lipopolysaccharide (LPS)-induced nitrite release in BV-2 microglial cells, RAW 264.7 macrophages, and mouse primary microglial cultures (~50 nM to 20 µM) without inducing any toxicity. However, it is shown to be less potent in primary astrocytes. Suppresses LPS-stimulated increase in the levels of IL-6, IL-1b, NOS2, and TNFα genes and inhibits the nuclear translocation of NF-κB. Also shown to reduce LPS-induced phosphorylation of ERK, JNK, and p38 MAP kinases in microglia. Reduces neuroinflammation, neurite damage, and spinal cord demyelination in a murine model of auto-immune encephalitis (~10 mg/kg).
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 HMGB2
Reversible: yes
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
Lee, S., et al. 2014. Nat. Chem. Biol.10, in press.
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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