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5.38339 Sigma-Aldrich

HuR-ARE Interaction Inhibitor, CMLD-2 - Calbiochem

Synonym: 5,7-dimethoxy-8-(1-(4-methoxyphenyl)-3-oxo-3-(pyrrolidin-1-yl)propyl)-4-phenyl-2H-chromen-2-one, HuR-ARE Interaction Inhibitor, CMLD-2 - Calbiochem

  • Empirical Formula (Hill Notation) C31H31NO6

  • Molecular Weight 513.58

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Properties

Quality Level   100
assay   ≥98% (HPLC)
form   solid
mfr. no.   Calbiochem®
storage condition   OK to freeze
  protect from light
storage conditions   +2C to +8C
color   white
solubility   DMSO: 50 mg/mL

Description

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).

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

Warning

Toxicity: Standard Handling (A)

Reconstitution

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.

Safety & Documentation

Safety Information

Safety Information for this product is unavailable at this time.
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