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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.

Cat. No. Product Name CAS No. Information
H6618

PIN1 inhibitor VS10

920849-78-1

PIN1 inhibitor VS10 is a novel potent small molecule inhibitor of PIN1 (peptidyl-prolyl cis-trans isomerase, NIMA-interacting 1), inhibits human PIN1 isomerization with IC50 of 13.4 uM, displays >2-fold more potency than ATRA; reduces cancer cell viability of ovarian cancer cell lines with IC50 of 53.9-76.4 uM; targets PIN1 to the proteasome, and induces PIN1 protein degradation in NIH3T3 fibroblasts, also shows inhibitory effects on PIN1 target proteins (cyclin D1, pSer473-Akt and β-catenin) in the OVCAR3 cell line.

H6617

Pin1 inhibitor API-1

680622-70-2

Pin1 inhibitor API-1 (API-1) is a potent, specific inhibitor of peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 (Pin1) and inhibits Pin1 cis-trans isomerizing activity with IC50 of 72.3 nM, displays remarkable selectivity over other peptidyl-prolyl cis-trans isomerases, including Pin4, FKBP12, and cyclophilin A; suppresses in vitro cell proliferation and migration of HCC cells with low IC50 values, which is depended on both Pin1 expression and XPO5 phosphorylation; recognizes and isomerizes the phosphorylated serine-proline motif of phosphorylated XPO5 and passivates phosphorylated XPO5, maintains the active pXPO5 conformation, rescues the pre-miRNA loading of pXPO5 and increases mature miRNA biogenesis; suppresses tumour growth in mice.

H8364

NSC 141562 Bromide

1029089-56-2

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.

H2817

Targaprimir-96

1655508-14-7

A small molecule that selectively modulates miR-96 production in cancer cells and triggers apoptosis; directly engages pri-miR-96 in breast cancer cells, and has a favorable pharmacokinetic profile and decreases tumor burden in a mouse model of triple-negative breast cancer.

H2816

SID-3712249

522606-67-3

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.

H2815

NSC 141562

1029221-71-3

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.

H2814

myomiRs-IN-1

1392224-59-7

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.

H2813

miR544-IN-1

522606-67-3

miR544-IN-1 (SID 3712249) is a selective small molecule inhibitor of miR-544 biogenesis; selectively inhibits production of the mature microRNA, sensitizes cells to 5-fluorouracil, and derepresses mRNAs affected by miR-544 in cellulo and in vivo, including boosting mTOR expression; reverses a tumor cell's physiological response to hypoxia.

H2811

miR-21 inhibitor 37

2241028-18-0

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.

H2810

BzDANP

1994258-88-6

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.

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