Merck, 5383390001, HuR-ARE Interaction Inhibitor, CMLD-2

General description
A cell-permeable, 2H-chromen-2-one based compound that competitively binds to Hu antigen R (HuR; Ki = 350 nM) and disrupts the interaction of HuR and adenine- and uridine-rich element (ARE) of target mRNAs. Displays dose-dependent binding to full-length HuR protein and to RRM1/2 fragment. Exhibits cytotoxicity towards tumor cells and reduces their viability (IC₅₀ = 28.9 and 18.2 µM for HCT-116 and MioPaCa2 cells, respectively). Has much reduced effect on normal WI-38 and CCD 841 CoN cells. Shown to induce cleavage of poly (ADP-ribose) polymerase and pro-caspase 3 (~ 50 µM) and reduce the half-life of Bcl-2, Msi1, and XIAP in HCT-116 cells (~20 µM) treated with actinomycin D (5 µg/ml).

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
HuR
Reversible: yes
Target Ki: 350 nM for HuR binding
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°:). Stock solutions are stable for up to months at -20°C.
Other Notes
Wu, X., et al. 2015. ACS Chem. Biol.10, 1476.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)