5.38339

CMLD-2

≥98% (HPLC), RNA stability modulator, solid

• Synonym(e): HuR-ARE Interaction Inhibitor, CMLD-2, 5,7-dimethoxy-8-(1-(4-methoxyphenyl)-3-oxo-3-(pyrrolidin-1-yl)propyl)-4-phenyl-2H-chromen-2-one
• Empirische Formel (Hill-System): C₃₁H₃₁NO₆
• Molekulargewicht: 513.58
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥98% (HPLC)
• Form: solid
• Quality level: 100
• Storage condition: OK to freeze, protect from light

Eigenschaften

• Produktname: HuR-ARE Interaction Inhibitor, CMLD-2,
• Quality Level: 100
• assay: ≥98% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: white
• solubility: DMSO: 50 mg/mL
• storage temp.: 2-8°C

Beschreibung

General description

A cell-permeable, 2H-chromen-2-one based compound that competitively binds to Hu antigen R (HuR; K_i = 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 K_i: 350 nM for HuR binding

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20&deg:). 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)

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable