Chemical Name: N-(3-Azidopropyl)-4-[3-[6-(4-methyl-1-piperazinyl)[2,6'-bi-1H-benzimidazol]-2'-yl]phenoxy]butanamide
Biological ActivityTargapremir 210 inhibits formation of mature miR-210 (IC50 = 200 nM) by binding to Dicer binding site of the miR-210 hairpin precursor (Kd = 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.
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Complete Your Research
Small molecule inhibition of microRNA-210 reprograms an oncogenic hypoxic circuit.
Costales et al.
Rationally designed small molecules targeting the RNA that causes myotonic dystrophy type 1 are potently bioactive.
Childs-Disney et al.
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