Targapremir 210

Biological Activity

Targapremir 210 inhibits formation of mature miR-210 (IC₅₀ = 200 nM) by binding to Dicer binding site of the miR-210 hairpin precursor (K_d = 200 nM) and inhibits Dicer processing of the miRNA. Decreases levels of miR-210 and HIF-1α mRNA, and induces apoptosis in MDA-MB-231 cells cultured under hypoxic conditions. Reduces tumor expression of HIF-1α mRNA and miR-210, and tumor growth in a triple negative breast cancer mouse model.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Small molecule inhibition of microRNA-210 reprograms an oncogenic hypoxic circuit.
   Costales et al.
   J.Am.Chem.Soc., 2017;139:3446
2. Rationally designed small molecules targeting the RNA that causes myotonic dystrophy type 1 are potently bioactive.
   Childs-Disney et al.
   ACS.Chem.Biol, 2012;7:856

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