MiRNAs are 21-25 nucleotide RNAs that negatively regulate gene expression through translational repression or cleavage of a target mRNA. They are transcribed as precursors that are processed by the nucleases Drosha and Dicer.
Small molecules targeting the secondary structure of precursor miRNAs can be more selective modulators of function than oligonucleotides that target RNA sequence.
MicroRNAs (miRNAs) and promoter hypermethylation are vital epigenetic mechanisms for transcriptional inactivation of tumor suppressor.
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BzDANP is a small molecule modulator of pre-miR-29a maturation by Dicer, effectively stabilizes the C-bulged RNA and suppresses Dicer-mediated processing of pre-miR-29a in a concentration dependent manner.
myomiRs-IN-1 is a small-molecule probe that selectively inhibits myogenic microRNAs (myomiRs) including miR-1, miR-133a, and miR-206; upregulates miR-221/222 level and suppresses myoD protein expression in C2C12 cells; inhibits the differentiation of C2C12 cells.
SID 3712249 is a small molecule inhibitor of the biogenesis of microRNA-544 (miR-544); causes apoptosis in triple negative breast cancer cell; bind directly to the precursor miRNA, blocking production of the mature microRNA and resulting in decreased miR-544, HIF-1α and ATM transcripts.
NSC 141562 (NSC141562;NSC-141562) is a potent small-molecule inhibitor of the MIR155 host gene/miR-155 axis; strongly inhibits mature miR-155 generation in a timedependent manner in U87 and primary GBM cells, reduces the proliferation, migration and invasion, increases the expression of PCDH9 and PCDH7, decreases the expression of mesenchymal transition-associated markers, N-cadherin, vimentin, MMP9 and β-catenin.
miR-21 inhibitor 37
miR-21 inhibitor 37 is a novel inhibitor of miR-21 function with EC50 of 5.3 uM in HeLa-miR21-Luc assays, displays no inhibition of miR-122; miR-21 inhibitor 37 has no effect on either mature or primary miR-21 levels in HeLa cells, as well as no effect on miR-21 transcription; exhibits low micromolar potency against different established cancer cells (MCF-7 and MIA PaCa-2, IC50=4.5 and 6.7 uM); shows significant rescue of both PDCD4 (9.5-fold increase) and PTEN (1.5-fold increase) levels in A498 RCC cells, sensitizes cells to topotecan-induced apoptosis.
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