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Chromatin/Epigenetic

DNA Methyltransferase

(78)

Epigenetic Reader Domain

HIF/HIF Prolyl-Hydroxylase

(194)

Histone Acetyltransferase

(119)

Histone Demethylase

(182)

Histone Methyltransferase

Methionine Adenosyltransferase (MAT)

MicroRNA

MicroRNAs (miRNAs) are a class of endogenous non-coding RNAs, about 22 nucleotides in length, that regulate gene expression by inhibiting the translation of mRNAs or decreasing their stability. miRNAs can act as oncogenes or tumor suppressor genes, and by using miRNA mimics or anti-miRNAs to modulate specific miRNA changes, it is possible to restore gene regulatory networks and signaling pathways, and even reverse the phenotype of cancer cells. Compared with traditional small molecule drugs, miRNAs have the natural property of regulating multiple target genes and are located at the center of multi-target regulatory networks.

Filter HomeSignaling PathwaysChromatin/EpigeneticMicroRNA

Cl-amidine hydrochloride

T10831L1373232-26-8

Cl-amidine hydrochloride is an orally available PAD inhibitor that blocks histone 3 deimination and neutrophil extracellular trap formation and improves survival in septic mice. It induces apoptosis in cancer cells and induces miR-16 to cause cell cycle arrest.

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Camptothecin

T11237689-03-4

Camptothecin (CPT) belongs to the alkaloid group of natural products and is a specific DNA topoisomerase I (Topo I) inhibitor (IC50=679 nM) with specificity. Camptothecin has antitumor activity and induces apoptosis.

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Guanosine-5'-triphosphate disodium salt

T1151156001-37-7

Guanosine-5'-triphosphate disodium salt (5'-GTP disodium salt) is an enhancer of myogenic cell differentiation and serves as an energy source for translation and other critical cellular processes.

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TGP-377/421

T6108516752-89-9

TGP-377/421 (Targapre-miR-377/421) is a potent dual inhibitor that binds to and inhibits miR-377 and miR-421 at their functional sites.

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Rubone

T2474473694-15-2

Rubone (2'-Hydroxy-2,4,4',5,6'-pentamethoxychalcone), a natural product and a modulator of miR-34a (microRNA-34), upregulates miR-34a expression in a p53-dependent manner, which in turn downregulates the expression of downstream targets Bcl-2, cyclin-D1, CDK6, SIRT1, and FOXP1, thereby inhibiting tumor growth and reversal of hepatocellular carcinoma (HCC) and chemoresistance in prostate cancer.

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Aurintricarboxylic acid

T83334431-00-9

Aurintricarboxylic acid (NSC-4056) is a strong inhibitor of topoisomerases and other nucleases. It is a potent inhibitor of ribonuclease and topoisomerase II by preventing the binding of the nucleic acid to the enzyme.

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Diosgenin

T2867512-04-9

Diosgenin (Nitogenin) is a spirostan found in DIOSCOREA and other plants. It has favorable effects in the improvement of diabetes and regulation of lipid metabolism.

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Pseudoprotodioscin

T5S0246102115-79-7

1. Pseudoprotodioscin has moderate cytotoxicity.

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PIN1 inhibitor API-1

T16538680622-70-2

PIN1 inhibitor API-1 is a specific Pin1 inhibitor (IC50: 72.3 nM) that retains the active conformation of pXPO5, restoring its ability to transport pre-miRNAs from the nucleus to the cytoplasm, thereby up-regulating anticancer miRNA biogenesis to suppress hepatocellular carcinoma development both in vitro and in vivo. PIN1 inhibitor API-1 directly and specifically binds to the Pin1 peptidyl-prolyl isomerase domain, effectively inhibiting Pin1 cis-trans isomerizing activity.

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RJW100

T386801276664-20-0In house

RJW100 is a compound that acts as a potent agonist of liver receptor homolog 1 (LRH-1, NR5A2) and steroidogenic factor-1 (SF-1, NR5A1), exhibiting pEC50 values of 6.6 and 7.5, respectively. Additionally, RJW100 induces robust activation of the miR-200c (miRNA-200c, microRNA-200c) promoter.

$247

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LIN28 inhibitor LI71

T118501357248-83-9

LIN28 inhibitor LI71 is a potent and cell-permeable compound that effectively abolishes LIN28-mediated oligouridylation, with an IC50 of 7 µM (micromolar).

$139

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Targapremir-210

T169911049722-30-6

Targapremir-210 (TGP-210) is a selective and potent inhibitor of miRNA-210 (miRNA-210), which inhibits pre-miR-210 processing and induces apoptosis in breast cancer cells.

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Enoxacin

T0717L74011-58-8

Enoxacin (NSC-629661) is a broad-spectrum 6-fluoronaphthyridinone antibacterial agent (fluoroquinolones) structurally related to nalidixic acid.

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MicroRNA-21-IN-2

T61093303018-40-8

MicroRNA-21-IN-2 is a potential miR-21 inhibitor with an AC50 value of 3.29 μM. MicroRNA-21-IN-2 can be used to study cancer.

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Enoxacin hydrate

T071784294-96-2

Enoxacin hydrate (AT-2266 hydrate) is a broad-spectrum 6-fluoronaphthyridinone antibacterial agent.

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Lin281632

T27835108825-65-6

Lin28 1632 is an inhibitor of RNA binding protein Lin28. It promotes mESC differentiation. Lin281632 is also bromodomain inhibitor.

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Lin28-let-7a antagonist 1

T118512024548-03-4

Lin28-let-7a antagonist 1, with an IC50 of 4.03 μM for Lin28A-let-7a-1 interaction,and shows a clear antagonistic effect against the Lin28-let-7a interaction.

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(R)-SKBG-1

T791562955634-67-8

(R)-SKBG-1 is an inhibitor of the RNA-binding protein NONO, with an EC50 value of 1.5 μM in 22Rv1 cells. (R)-SKBG-1 reduces mRNA and protein expression of the androgen receptor (AR) and its splice variants (AR-FL and AR-V7), inhibits the proliferation of various cancer cells, and affects the transcriptome and proteome of cancer cells.

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SID 3712249

T16882522606-67-3In house

SID 3712249 is an inhibitor of the biogenesis of microRNA-544 (miR-544).

5 days

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Cl-amidine

T10831913723-61-2

Cl-amidine is an orally active inhibitor of peptidyl arginine deiminase (PAD) with IC50 values of 0.8 μM, 6.2 μM, and 5.9 μM for PAD1, PAD3, and PAD4, respectively. It induces apoptosis in cancer cells.

$1,520

1-2 weeks

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Eldocasiran

T745742615098-65-0

Eldocasiran, a micro-RNA-193a-3p analogue, exhibits anticancer properties. It is utilized in cancer research [1].

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microRNA-21-IN-1

T638792848720-31-8

MicroRNA-21-IN-1 (compound 7A) is an effective inhibitor of microRNA with antiproliferative effects on Hela and HCT-116 cells, showing IC50 values of 5.5 μM and 2.8 μM, respectively. It also induces apoptosis in Hela cells and increases the expression of PTEN, EGR1, and SLIT2, which are functional targets downstream of microRNA-21. This compound holds potential for anticancer research [1].

$1,520

10-14 weeks

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Thymidine 3',5'-diphosphate tetrasodium

T73824118675-87-9

Thymidine 3',5'-diphosphate tetrasodium (Deoxythymidine 3′,5′-diphosphate tetrasodium) acts as a selective inhibitor targeting staphylococcal nuclease, tudor domain-containing 1 (SND1, a MicroRNA regulatory complex RISC subunit), and [3,5-2H2] tyrosyl nuclease. It possesses anti-tumor properties and serves as a catalyst in various biochemical reactions [1] [2].

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TRBP-IN-1

T207594

TRBP-IN-1 (Compound 13j) is an orally active inhibitor of TAR RNA-binding protein 2 (TRBP) with an IC50 of 12.72 μM. It exhibits significant anti-hepatocellular carcinoma (HCC) activity, effectively suppressing proliferation and metastasis of HCC cells [HCCLM3 cells (IC50: 18.96 μM) and SK-Hep-1 cells (IC50: 16.45 μM)]. TRBP-IN-1 modulates miRNA biosynthesis by targeting TRBP, inhibiting the expression of oncogenic miRNAs. It induces apoptosis and pyroptosis in HCC cells by decreasing miRNA levels. TRBP-IN-1 is suitable for research on targeted HCC therapy.

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