1. Signaling Pathways
  2. Epigenetics
  3. MicroRNA

MicroRNA

MicroRNAs (miRNAs) are a naturally occurring class of small (approximately 22 nucleotides long) non-coding RNAs that regulate post-transcriptional gene expression to control cellular processes, development, cell differentiation, and homeostasis. MicroRNAs are essential for embryo, cell, and tissue development, regulating cell differentiation, proliferation, and apoptosis, hence their importance in human reproduction. Meanwhile, abnormal expression or function of miRNAs are found to be closely associated with the occurrence or development of various human diseases, including cancers. In light of their significant roles in physiology and pathology, miRNAs are emerging as novel biomolecular targets for chemical-biological studies, including regulation and detection.

Multiple steps are involved in the generation of miRNAs. Most miRNAs are produced by the canonical biogenesis pathway, which involves transcription by RNA polymerase II to make a primary transcript (pri-miRNA) and cleavage by the microprocessor complex to yield a hairpin precursor miRNA (pre-miRNA) in the nucleus. The pre-miRNA is then exported into the cytoplasm, where cleavage by the enzyme Dicer creates a double-stranded RNA duplex. Only a single strand from the double-stranded RNA duplex forms the mature miRNA and is incorporated into the RNA-induced silencing complex (RISC), which guides the binding of Argonaute (AGO) proteins in the RISC to the 3’untranslated region (UTR) to either repress protein translation or promote mRNA degradation. In addition to canonical miRNA biogenesis pathways, non-canonical microprocessor-independent or Dicer-independent miRNA biogenesis pathways also exist. Despite miRNAs being mostly involved in the down-regulation of gene expression, there are reports of miRNAs promoting gene expression. In addition, relationships between miRNAs and their targets are not always one-to-one in a specific cell type. In fact, a single miRNA may regulate many mRNA targets, and conversely, a single mRNA target also can be regulated by many miRNAs.

MicroRNA Related Products (15):

Cat. No. Product Name Effect Purity
  • HY-100574A
    Cl-amidine hydrochloride Activator
    Cl-amidine hydrochloride is an orally active peptidylarginine deminase (PAD) inhibitor, with IC50 values of 0.8 μM, 6.2 μM and 5.9 μM for PAD1, PAD3, and PAD4, respectively. Cl-amidine hydrochloride induces apoptosis in cancer cells. Cl-amidine hydrochloride induces microRNA (miR)-16 (miRNA-16, microRNA-16) expression and causes cell cycle arrest. Cl-Amidine hydrochloride prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model.
  • HY-15843
    MIR96-IN-1 Inhibitor ≥98.0%
    MIR96-IN-1 targets the Drosha site in the miR-96 (miRNA-96, microRNA-96) hairpin precursor, inhibiting its biogenesis, derepressing downstream targets, and triggering apoptosis in breast cancer cells. MIR96-IN-1 binds to RNAs with Kds of 1.3, 9.4, 3.4, 1.3 and 7.4 μM for RNA1, RNA2, RNA3, RNA4 and RNA5, respectively.
  • HY-B0268A
    Enoxacin hydrate Activator 98.15%
    Enoxacin hydrate (Enoxacin sesquihydrate), a fluoroquinolone, interferes with DNA replication and inhibits bacterial DNA gyrase (IC50=126 µg/ml) and topoisomerase IV (IC50=26.5 µg/ml). Enoxacin hydrate is a miRNA processing activator and enhances siRNA-mediated mRNA degradation and promotes the biogenesis of endogenous miRNAs. Enoxacin hydrate has potent activities against gram-positive and -negative bacteria. Enoxacin hydrate is a cancer-specific growth inhibitor that acts by enhancing TAR RNA-binding protein 2 (TRBP)-mediated microRNA processing.
  • HY-15861
    Targapremir-210 Inhibitor 98.02%
    Targapremir-210 (TGP-210) is a potent and selective miR-210 (miRNA-210, microRNA-210) inhibitor. Targapremir-210 inhibits pre-miR-210 processing with high binding affinity (Kd~200 nM).
  • HY-122575
    Aurintricarboxylic acid Modulator
    Aurintricarboxylic acid is a nanomolar-potency, allosteric antagonist with selectivity towards αβ-methylene-ATP-sensitive P2X1Rs and P2X3Rs, with IC50s of 8.6 nM and 72.9 nM for rP2X1R and rP2X3R, respectively. Aurintricarboxylic acid is a potent anti-influenza agent by directly inhibiting the neuraminidase. Aurintricarboxylic acid is an inhibitor of topoisomerase II and apoptosis. Aurintricarboxylic acid is a selective inhibitor of the TWEAK-Fn14 signaling pathway. Aurintricarboxylic acid also acts as a cystathionine-lyase (CSE) inhibitor with an IC50 of 0.6 μM. Aurintricarboxylic acid is a modifier of miRNAs that regulate miRNA function, with an IC50 of 0.47 µM.
  • HY-116716
    PIN1 inhibitor API-1 Activator
    PIN1 inhibitor API-1 is a specific Pin1 (peptidyl-prolyl cis-trans isomerase NIMA-interacting 1) inhibitor (API-1) with an IC50 of 72.3 nM. PIN1 inhibitor API-1 directly and specifically binds to the Pin1 peptidyl-prolyl isomerase (PPIase) domain and potently inhibits Pin1 cis-trans isomerizing activity. PIN1 inhibitor API-1 retains the active conformation of pXPO5 and restores the ability of pXPO5 to transport pre-miRNAs from nucleus to cytoplasm, thus up-regulating the anticancer miRNA biogenesis to suppress both in vitro and in vivo hepatocellular carcinoma development.
  • HY-100692
    Lin28-let-7a antagonist 1 Antagonist 99.62%
    Lin28-let-7a antagonist 1 shows a clear antagonistic effect against the Lin28-let-7a interaction with an IC50 of 4.03 μM for Lin28A-let-7a-1 interaction.
  • HY-N0686
    Pseudoprotodioscin Inhibitor 98.76%
    Pseudoprotodioscin, a furostanoside, inhibits SREBP1/2 and microRNA 33a/b levels and reduces the gene expression regarding the synthesis of cholesterol and triglycerides.
  • HY-19731
    SID 3712249 Inhibitor 98.82%
    SID 3712249 (MiR-544 Inhibitor 1) is an inhibitor of the biogenesis of microRNA-544 (miR-544).
  • HY-123905
    LIN28 inhibitor LI71 Inhibitor 98.10%
    LIN28 inhibitor LI71 is a potent and cell-permeable LIN28 inhibitor, which abolishes LIN28-mediated oligouridylation with an IC50 of 7 uM. LIN28 inhibitor LI71 directly binds the cold shock domain (CSD) to suppress LIN28’s activity against let-7 in leukemia cells and embryonic stem cells.
  • HY-135276
    Targaprimir-96 Inhibitor
    Targaprimir-96 is a potent inhibitor of microRNA-96 (miR-96) processing. Targaprimir-96 selectively modulates miR-96 production in cancer cells and triggers apoptosis. Targaprimir-96 binds primary miR-96 (pri-miR-96) with low nanomolar affinity. Targaprimir-96 directly engages pri-miR-96 in breast cancer cells and is ineffective on healthy breast cells.
  • HY-B0268
    Enoxacin Activator 98.67%
    Enoxacin (AT 2266), a fluoroquinolone, interferes with DNA replication and inhibits bacterial DNA gyrase (IC50=126 µg/ml) and topoisomerase IV (IC50=26.5 µg/ml). Enoxacin is a miRNA processing activator and enhances siRNA-mediated mRNA degradation and promotes the biogenesis of endogenous miRNAs. Enoxacin has potent activities against gram-positive and -negative bacteria. Enoxacin is a cancer-specific growth inhibitor that acts by enhancing TAR RNA-binding protein 2 (TRBP)-mediated microRNA processing.
  • HY-100574B
    Cl-amidine TFA Activator
    Cl-amidine TFA is an orally active peptidylarginine deminase (PAD) inhibitor, with IC50 values of 0.8 μM, 6.2 μM and 5.9 μM for PAD1, PAD3, and PAD4, respectively. Cl-amidine TFA induces apoptosis in cancer cells. Cl-amidine TFA induces microRNA (miR)-16 (miRNA-16, microRNA-16) expression and causes cell cycle arrest. Cl-Amidine TFA prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model.
  • HY-100574
    Cl-amidine Activator
    Cl-amidine is an orally active peptidylarginine deminase (PAD) inhibitor, with IC50 values of 0.8 μM, 6.2 μM and 5.9 μM for PAD1, PAD3, and PAD4, respectively. Cl-amidine induces apoptosis in cancer cells. Cl-amidine induces microRNA (miR)-16 (miRNA-16, microRNA-16) expression and causes cell cycle arrest. Cl-Amidine prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model.
  • HY-131445
    RJW100 Activator
    RJW100 is a potent liver receptor homolog 1 (LRH-1, NR5A2) and steroidogenic factor-1 (SF-1, NR5A1) agonist with pEC50s of 6.6 and 7.5, respectively. RJW100 also causes strong activation of the miR-200c (miRNA-200c, microRNA-200c) promoter.
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