MicroRNA-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/MicroRNA.html MicroRNAmiRNAMicroRNAs (miRNAs) are a naturally occurring class of small (approximately 22 nucleotides long) non-coding RNAs that regulatepost-transcriptional gene expression to control cellular processes, development, cell differentiation, and ho

2、meostasis. MicroRNAsare essential for embryo, cell, and tissue development, regulating cell differentiation, proliferation, and apoptosis, hence theirimportance in human reproduction. Meanwhile, abnormal expression or function of miRNAs are found to be closely associated withthe occurrence or develo

3、pment of various human diseases, including cancers. In light of their significant roles in physiology andpathology, 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 miRN

4、As are produced by the canonical biogenesis pathway, whichinvolves transcription by RNA polymerase II to make a primary transcript (pri-miRNA) and cleavage by the microprocessor complexto yield a hairpin precursor miRNA (pre-miRNA) in the nucleus. The pre-miRNA is then exported into the cytoplasm, w

5、here cleavageby the enzyme Dicer creates a double-stranded RNA duplex. Only a single strand from the double-stranded RNA duplex forms themature miRNA and is incorporated into the RNA-induced silencing complex (RISC), which guides the binding of Argonaute (AGO)proteins in the RISC to the 3untranslate

6、d region (UTR) to either repress protein translation or promote mRNA degradation. Inaddition to canonical miRNA biogenesis pathways, non-canonical microprocessor-independent or Dicer-independent miRNAbiogenesis pathways also exist. Despite miRNAs being mostly involved in the down-regulation of gene

7、expression, there are reportsof miRNAs promoting gene expression. In addition, relationships between miRNAs and their targets are not always one-to-one in aspecific cell type. In fact, a single miRNA may regulate many mRNA targets, and conversely, a single mRNA target also can beregulated by many mi

8、RNAs.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/MicroRNA.html MicroRNA HYPERLINK https:/www.MedChemE/Targets/MicroRNA.html HYPERLINK https:/www.MedChemE/Targets/MicroRNA.html Inhibitors, HYPERLINK https:/www.MedChemE/Targets/MicroRNA.html HYPERLINK https:/www.MedChemE/Targets/MicroRNA.html

9、 Agonists, HYPERLINK https:/www.MedChemE/Targets/MicroRNA.html HYPERLINK https:/www.MedChemE/Targets/MicroRNA.html Antagonists, HYPERLINK https:/www.MedChemE/Targets/MicroRNA.html HYPERLINK https:/www.MedChemE/Targets/MicroRNA.html Activators HYPERLINK https:/www.MedChemE/Targets/MicroRNA.html HYPER

10、LINK https:/www.MedChemE/Targets/MicroRNA.html & HYPERLINK https:/www.MedChemE/Targets/MicroRNA.html HYPERLINK https:/www.MedChemE/Targets/MicroRNA.html Modulators HYPERLINK https:/www.MedChemE/aurintricarboxylic-acid.html Aurintricarboxylic HYPERLINK https:/www.MedChemE/aurintricarboxylic-acid.html

11、 HYPERLINK https:/www.MedChemE/aurintricarboxylic-acid.html acidCat. No.: HY-122575 HYPERLINK https:/www.MedChemE/Campathecin.html Camptothecin(Campathecin; (S)-(+)-Camptothecin; CPT) Cat. No.: HY-16560Aurintricarboxylic acid is a nanomolar-potency,allosteric antagonist with selectivity towards-meth

12、ylene-ATP-sensitive P2X1Rs and P2X3Rs,with IC s of 8.6 nM and 72.9 nM for rP2X1R and50rP2X3R, respectively.Camptothecin (CPT), a kind of alkaloid, is a DNAtopoisomerase I (Topo I) inhibitor with an IC of50679 nM.Purity: 98%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 100 mgPurity: 99.69%C

13、linical Data: LaunchedSize: 10 mM 1 mL, 100 mg, 500 mg HYPERLINK https:/www.MedChemE/camptothecin-d5.html Camptothecin-d5(Campathecin-d5; (S)-(+)-Camptothecin-d5; CPT-d5) Cat. No.: HY-16560S HYPERLINK https:/www.MedChemE/Cl-amidine.html Cl-amidineCat. No.: HY-100574Camptothecin-d5 (Campathecin-d5) i

14、s the deuteriumlabeled Camptothecin. Camptothecin (CPT), a kindof alkaloid, is a DNA topoisomerase I (Topo I)inhibitor with an IC of 679 nM.50Cl-amidine is an orally active peptidylargininedeminase (PAD) inhibitor, with IC values of 0.850M, 6.2 M and 5.9 M for PAD1, PAD3, and PAD4,respectively. Cl-a

15、midine induces apoptosis incancer cells.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Cl-amidine_hydrochloride.html Cl-amidine HYPERLINK https:/www.MedChemE/Cl-amidine_hydrochloride.htm

16、l HYPERLINK https:/www.MedChemE/Cl-amidine_hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/Cl-amidine_hydrochloride.html HYPERLINK https:/www.MedChemE/cl-amidine-tfa.html Cl-amidine HYPERLINK https:/www.MedChemE/cl-amidine-tfa.html HYPERLINK https:/www.MedChemE/cl-amidine-tfa.html TFA

17、Cat. No.: HY-100574A Cat. No.: HY-100574BCl-amidine hydrochloride is an orally activepeptidylarginine deminase (PAD) inhibitor, withIC values of 0.8 M, 6.2 M and 5.9 M for PAD1,50PAD3, and PAD4, respectively. Cl-amidinehydrochloride induces apoptosis in cancer cells.Cl-amidine TFA is an orally activ

18、e peptidylargininedeminase (PAD) inhibitor, with IC values of 0.850M, 6.2 M and 5.9 M for PAD1, PAD3, and PAD4,respectively. Cl-amidine TFA induces apoptosis incancer cells.Purity: 99.10%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data

19、: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/enoxacin.html Enoxacin HYPERLINK https:/www.MedChemE/enoxacin.html HYPERLINK https:/www.MedChemE/Enoxacin-hydrate.html Enoxacin HYPERLINK https:/www.MedChemE/Enoxacin-hydrate.html HYPERLINK https:/www.MedChemE/Enoxacin-hydrate.h

20、tml hydrate(AT 2266; CI 919) Cat. No.: HY-B0268 (Enoxacin sesquihydrate; AT-2266 hydrate; CI-919 hydrate) Cat. No.: HY-B0268AEnoxacin (AT 2266), a fluoroquinolone, interfereswith DNA replication and inhibits bacterial DNAgyrase (IC =126 g/ml) and topoisomerase IV50(IC =26.5 g/ml).50Enoxacin hydrate

21、(Enoxacin sesquihydrate), afluoroquinolone, interferes with DNA replicationand inhibits bacterial DNA gyrase (IC =126 g/ml)50and topoisomerase IV (IC =26.5 g/ml).50Purity: 98.67%Clinical Data: LaunchedSize: 1 mg, 5 mgPurity: 98.15%Clinical Data: LaunchedSize: 100 mg, 500 mg HYPERLINK https:/www.MedC

22、hemE/enoxacin-d8.html Enoxacin-d8 HYPERLINK https:/www.MedChemE/enoxacin-d8.html HYPERLINK https:/www.MedChemE/enoxacin-d8-hydrochloride.html Enoxacin-d8 HYPERLINK https:/www.MedChemE/enoxacin-d8-hydrochloride.html HYPERLINK https:/www.MedChemE/enoxacin-d8-hydrochloride.html hydrochlorideCat. No.: H

23、Y-B0268S Cat. No.: HY-B0268S1Enoxacin-d8 (AT 2266-d8) is the deuterium labeledEnoxacin. Enoxacin (AT 2266), a fluoroquinolone,interferes with DNA replication and inhibitsbacterial DNA gyrase (IC =126 g/ml) and50topoisomerase IV (IC =26.5 g/ml).50Enoxacin-d8 (hydrochloride) is deuterium labeledEnoxac

24、in. Enoxacin (AT 2266), a fluoroquinolone,interferes with DNA replication and inhibitsbacterial DNA gyrase (IC50=126 g/ml) andtopoisomerase IV (IC50=26.5 g/ml).Purity: 98%Clinical Data:Size: 2.5 mg, 25 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg2 Tel: 609-228-6898 Fax: 609-22

25、8-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/gypenoside-li.html Gypenoside HYPERLINK https:/www.MedChemE/gypenoside-li.html HYPERLINK https:/www.MedChemE/gypenoside-li.html LICat. No.: HY-N8207 HYPERLINK https:/www.MedChemE/lademirsen.html Lademirsen(SAR339375; RG-012) Cat. No.: HY-1325

26、99Gypenoside LI, a gypenoside monomer, possessesanti-tumor activity. Gypenoside LI induces cellapoptosis, cell cycle and migration.Lademirsen (SAR339375; RG-012) is a highlyspecific antisense oligonucleotide (ASO) targetingmiR-21. Lademirsen has the potential for Alportnephropathy research.Purity: 9

27、8.29%Clinical Data: No Development ReportedSize: 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/lin28-inhibitor-li71.html LIN28 HYPERLINK https:/www.MedChemE/lin28-inhibitor-li71.html HYPERLINK https:/www.MedChemE/lin28-inhibitor-li71.html inhibit

28、or HYPERLINK https:/www.MedChemE/lin28-inhibitor-li71.html HYPERLINK https:/www.MedChemE/lin28-inhibitor-li71.html LI71 HYPERLINK https:/www.MedChemE/lin28-inhibitor-li71.html HYPERLINK https:/www.MedChemE/Lin28-let-7a_antagonist_1.html Lin28-let-7a HYPERLINK https:/www.MedChemE/Lin28-let-7a_antagon

29、ist_1.html HYPERLINK https:/www.MedChemE/Lin28-let-7a_antagonist_1.html antagonist HYPERLINK https:/www.MedChemE/Lin28-let-7a_antagonist_1.html HYPERLINK https:/www.MedChemE/Lin28-let-7a_antagonist_1.html 1Cat. No.: HY-123905 Cat. No.: HY-100692LIN28 inhibitor LI71 is a potent andcell-permeable LIN2

30、8 inhibitor, which abolishesLIN28-mediated oligouridylation with an IC of 750uM.Lin28-let-7a antagonist 1 shows a clearantagonistic effect against the Lin28-let-7ainteraction with an IC of 4.03 M for50Lin28A-let-7a-1 interaction.Purity: 98.10%Clinical Data: No Development ReportedSize: 5 mg, 10 mg,

31、50 mg, 100 mgPurity: 99.62%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/MIR96-IN-1.html MIR96-IN-1Cat. No.: HY-15843 HYPERLINK https:/www.MedChemE/miravirsen.html Miravirsen(SPC-3649) Cat. No.: HY-132598MIR96-IN-1 targets the Drosha

32、 site in themiR-96 (miRNA-96, microRNA-96) hairpinprecursor, inhibiting its biogenesis, derepressingdownstream targets, and triggering apoptosis inbreast cancer cells.Miravirsen (SPC-3649), a -d-oxy-locked nucleicacid-modified phosphorothioate antisenseoligonucleotide, inhibit the biogenesis ofmiR-1

33、22. Miravirsen (SPC-3649) is used in thestudy for HCV infections.Purity: 95.82%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg HYPERLINK https:/www.MedChemE/mtl-cebpa.html MTL-CEBPA HYPERLINK h

34、ttps:/www.MedChemE/mtl-cebpa.html HYPERLINK https:/www.MedChemE/pin1-inhibitor-api-1.html PIN1 HYPERLINK https:/www.MedChemE/pin1-inhibitor-api-1.html HYPERLINK https:/www.MedChemE/pin1-inhibitor-api-1.html inhibitor HYPERLINK https:/www.MedChemE/pin1-inhibitor-api-1.html HYPERLINK https:/www.MedChe

35、mE/pin1-inhibitor-api-1.html API-1Cat. No.: HY-132607 Cat. No.: HY-116716MTL-CEPBA is a small activating RNA targeting forupregulation of C/EBP. MTL-CEPBA hasanti-inflammatory and anti-cancer activity.PIN1 inhibitor API-1 is a specific Pin1(peptidyl-prolyl cis-trans isomeraseNIMA-interacting 1) inhi

36、bitor (API-1) with an ICof 72.3 nM.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 97.03%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/pseudoprotodioscin.html Pseudoprotodioscin HYPERLINK https:/www.

37、MedChemE/pseudoprotodioscin.html HYPERLINK https:/www.MedChemE/remlarsen.html RemlarsenCat. No.: HY-N0686(MRG-201) Cat. No.: HY-132602Pseudoprotodioscin, a furostanoside, inhibitsSREBP1/2 and microRNA 33a/b levels and reduces thegene expression regarding the synthesis ofcholesterol and triglycerides

38、.Remlarsen (MRG-201), a miR-29b mimic, acts amiR-29b agonist. Remlarsen has the potentialfor preventiong formation of a fibrotic scar orcutaneous fibrosis.Purity: 98.76%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 20 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgwww.

39、MedChemE 3 HYPERLINK https:/www.MedChemE/rg-101.html RG-101 HYPERLINK https:/www.MedChemE/rg-101.html HYPERLINK https:/www.MedChemE/rjw100.html RJW100Cat. No.: HY-132600 Cat. No.: HY-131445RG-101 is a hepatocyte targetedN-acetylgalactosamine conjugated oligonucleotidethat antagonises miR-122. miR-12

40、2 is animportant host factor for hepatitis C virus (HCV)replication.RJW100 is a potent liver receptor homolog 1 (LRH-1,NR5A2) and steroidogenic factor-1 (SF-1, NR5A1)agonist with pEC s of 6.6 and 7.5,50respectively. RJW100 also causes strong activationof the miR-200c (miRNA-200c, microRNA-200c)promo

41、ter.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg HYPERLINK https:/www.MedChemE/SID-3712249.html SID HYPERLINK https:/www.MedChemE/SID-3712249.html HYPERLINK https:/www.MedChemE/SID-3712249.html 3712249(MiR-544 Inh

42、ibitor 1) Cat. No.: HY-19731 HYPERLINK https:/www.MedChemE/Targapremir-210.html Targapremir-210(TGP-210) Cat. No.: HY-15861SID 3712249 (MiR-544 Inhibitor 1) is an inhibitorof the biogenesis of microRNA-544 (miR-544).Target: MiR-544 MiR-544 represses expression ofmTOR, promoting tumor cell survival in a hypoxicenvironment.