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Results for "

DNMTs

" in MedChemExpress (MCE) Product Catalog:

By Targets:	DNA Methyltransferase (36) ADC Cytotoxin (1) Apoptosis (7) Autophagy (1) Deubiquitinase (1) E1/E2/E3 Enzyme (1) HDAC (4) Histone Methyltransferase (7) Keap1-Nrf2 (1) Nucleoside Antimetabolite/Analog (1) Parasite (2) Potassium Channel (2) Small Interfering RNA (siRNA) (6) Virus Protease (1)
By Research Areas:	Cancer (43) Cardiovascular Disease (1) Endocrinology (1) Infection (3) Inflammation/Immunology (2) Metabolic Disease (1)
Oligonucleotides:	Pre-designed siRNA Sets (6) siRNAs (6)

Inhibitors & Agonists

Screening Libraries

Natural
Products

Oligonucleotides

Targets Recommended: DNA Methyltransferase

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-116217

5-Fluoro-2'-deoxycytidine 2 Publications Verification	DNA Methyltransferase	Cancer
5-Fluoro-2'-deoxycytidine, a fluoropyrimidine nucleoside analogue, is a DNA methyltransferase (DNMT) inhibitor. 5-Fluoro-2'-deoxycytidine is a tumor-selective proagent of the potent thymidylate synthase inhibitor 5-fluoro-2′-dUMP .

HY-144433

DNMT3A-IN-1 1 Publications Verification	DNA Methyltransferase	Infection
DNMT3A-IN-1 (compound 1) is an effective and selective DNMT3A inhibitor. DNMT3A-IN-1 exhibits inhibitory activity against DNMT3A, with K_I values ranging from 9.16 to 18.85 μM (AdoMet) and 11.37 to 23.34 μM (poly dI-dC). DNMT3A-IN-1 can induce apoptosis in acute myeloid leukemia (AML) cell lines (Apoptosis) .

HY-13962

SGI-1027 5+ Cited Publications	DNA Methyltransferase Apoptosis	Cancer
SGI-1027 is a DNA methyltransferase (DNMT) inhibitor, with IC₅₀s of 7.5 μM, 8 μM, and 12.5 μM for DNMT3B, DNMT3A, and DNMT1 with poly(dI-dC) as substrate.

HY-15449A

(S)-Kaempferide	DNA Methyltransferase	Cancer
(S)-Kaempferide (ZINC167686681) is a DNA methyltransferase (DNMT) inhibitor. (S)-Kaempferide can be used in tumor research .

HY-158075

DNMT/HDAC-IN-1	HDAC DNA Methyltransferase	Cancer
DNMT/HDAC-IN-1 (Compund 15a) is a dual *DNMT* and HDAC inhibitor with IC₅₀ values for HDAC1 and HDAC6 are 56.84 nM and 17.39 nM respectively. DNMT/HDAC-IN-1 can induce apoptosis and be used in tumor research.

HY-119054

DNMT1-IN-4	DNA Methyltransferase	Cancer
DNMT1-IN-4 is a potent non-nucleoside DNA methyltransferase 1 (DNMT1) inhibitor with an IC₅₀ value of 2.5 µM and selectivity towards other AdoMet-dependent protein methyltransferases. DNMT1-IN-4 significantly inhibits cancer cell proliferation .

HY-133030

DNMT-IN-1	DNA Methyltransferase	Cancer
DNMT-IN-1 is a potent *DNMT* inhibitor with an EC₅₀ value of 3.2 µM. DNMT-IN-1 shows antiproliferative active .

HY-168088

DNMT1/HDAC-IN-1	HDAC DNA Methyltransferase	Cancer
DNMT1/HDAC-IN-1 (compound (R)-23a) is a *DNMT1/HDAC* dual inhibitor (HDAC1:IC₅₀=0.05 μM), HDAC1 is a major HDAC isoform that interacts with *DNMT1* in multiple protein complexes for transcriptional silencing of TSGs. DNMT1/HDAC-IN-1 can reshape the tumor immune microenvironment and induce tumor regression, and effectively reverse cancer-specific epigenetic abnormalities .

HY-161694

DNMT1-IN-3	DNA Methyltransferase	Cancer
DNMT1-IN-3 (compound 7t-S) is an effective DNA methyltransferase 1 (DNMT1) inhibitor with an IC₅₀ value of 0.777 μM and a K_D value of 0.183 μM. DNMT1-IN-3 can bind to the methyl donor S-adenosyl-l-methionine (SAM) site in DNMT1. DNMT1-IN-3 can inhibit cell proliferation in K562 cells by inducing cells apoptosis and arresting cell cycle at G0 / G1 phase, which has the potential to be used for the research of hematologic tumor .

HY-149289

DNMT-IN-3	Parasite DNA Methyltransferase	Others
DNMT-IN-3 is an DNA Methyltransferase (DNMT) inhibitor, and plays an antimalarial role with IC₅₀ of 60 nM against Plasmodium falciparum (Plasmodium). DNMT-IN-3 can be used for malaria related research .

HY-154867

DNMT2-IN-1	DNA Methyltransferase	Cancer
DNMT2-IN-1 (compound 80) is a potent and selective DNMT2 (DNA methyltransferase 2) inhibitor with an IC₅₀ value of 1.2 μM, and has the potential for mental and metabolic disorders or cancer research .

HY-B2194

γ-Oryzanol 5+ Cited Publications	DNA Methyltransferase	Metabolic Disease Cancer
γ-Oryzanol is a potent DNA methyltransferases (DNMTs) inhibitor in the striatum of mice. γ-Oryzanol significantly inhibits the activities of *DNMT1* (IC₅₀=3.2 μM), *DNMT3a* (IC₅₀=22.3 μM).

HY-101925

CM-272 3 Publications Verification	Histone Methyltransferase DNA Methyltransferase Apoptosis	Cancer
CM-272 is a first-in-class, potent, selective, substrate-competitive and reversible dual G9a/DNA methyltransferases (DNMTs) inhibitor with antitumor activities. CM-272 inhibits G9a, *DNMT1, DNMT3A, DNMT3B* and GLP with IC₅₀s of 8 nM, 382 nM, 85 nM, 1200 nM and 2 nM, respectively. CM-272 inhibits cell proliferation and promotes apoptosis, inducing IFN-stimulated genes and immunogenic cell death .

HY-RS03908

DNMT1 Human Pre-designed siRNA Set A	Small Interfering RNA (siRNA)	Others
DNMT1 Human Pre-designed siRNA Set A contains three designed siRNAs for DNMT1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

DNMT1 Human Pre-designed siRNA Set A DNMT1 Human Pre-designed siRNA Set A

HY-RS03909

Dnmt1 Mouse Pre-designed siRNA Set A	Small Interfering RNA (siRNA)	Others
Dnmt1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Dnmt1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

Dnmt1 Mouse Pre-designed siRNA Set A Dnmt1 Mouse Pre-designed siRNA Set A

HY-RS03910

Dnmt1 Rat Pre-designed siRNA Set A	Small Interfering RNA (siRNA)	Others
Dnmt1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Dnmt1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

Dnmt1 Rat Pre-designed siRNA Set A Dnmt1 Rat Pre-designed siRNA Set A

HY-RS03911

DNMT3A Human Pre-designed siRNA Set A	Small Interfering RNA (siRNA)	Others
DNMT3A Human Pre-designed siRNA Set A contains three designed siRNAs for DNMT3A gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

DNMT3A Human Pre-designed siRNA Set A DNMT3A Human Pre-designed siRNA Set A

HY-RS03913

DNMT3L Human Pre-designed siRNA Set A	Small Interfering RNA (siRNA)	Others
DNMT3L Human Pre-designed siRNA Set A contains three designed siRNAs for DNMT3L gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

DNMT3L Human Pre-designed siRNA Set A DNMT3L Human Pre-designed siRNA Set A

HY-103236

NSC232003 2 Publications Verification	E1/E2/E3 Enzyme	Cancer
NSC232003 is a highly potent and cell-permeable UHRF1 inhibitor, which inhibits DNA methylation in vitro and disrupts DNMT1/UHRF1 interactions at a cellular level.

HY-RS03912

DNMT3B Human Pre-designed siRNA Set A	Small Interfering RNA (siRNA)	Others
DNMT3B Human Pre-designed siRNA Set A contains three designed siRNAs for DNMT3B gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

DNMT3B Human Pre-designed siRNA Set A DNMT3B Human Pre-designed siRNA Set A

HY-111544

EML741	Histone Methyltransferase	Cancer
EML741 is a histone lysine methyltransferase G9a/GLP inhibitor, with an IC₅₀ of 23 nM, K_d of 1.13 μM for G9a. EML741 also inhibits DNMT1 (IC₅₀, 3.1 μM), with no effect on DNMT3a or DNMT3b. EML741 exhibits low cell toxicity, and is membrane permeable and blood-brain barrier penetrated .

HY-117421A

CM-579 trihydrochloride	Histone Methyltransferase DNA Methyltransferase	Cancer
CM-579 trihydrochloride is a first-in-class reversible, dual inhibitor of G9a and *DNMT, with IC₅₀* values of 16 nM, 32 nM for G9a and DNMT, respectively. Has potent in vitro cellular activity in a wide range of cancer cells .

HY-117421

CM-579	Histone Methyltransferase DNA Methyltransferase	Cancer
CM-579 is a first-in-class reversible, dual inhibitor of G9a and *DNMT, with IC₅₀* values of 16 nM, 32 nM for G9a and DNMT, respectively. Has potent in vitro cellular activity in a wide range of cancer cells .

HY-111644

6-Methyl-5-azacytidine	DNA Methyltransferase	Cancer
6-Methyl-5-azacytidine is a potent DNMT inhibitor.

HY-139664

GSK-3685032 5 Publications Verification	DNA Methyltransferase	Cancer
GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible *DNMT1*-selective inhibitor, with an IC₅₀ of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition .

HY-150025

(4aS,8aR)-NPD-001	DNA Methyltransferase Apoptosis	Cancer
(4aS,8aR)-NPD-001 is a potent and allosteric inhibitor of *DNMT3A. (4aS,8aR)-NPD-001 inhibits DNMT3A activity by disrupting protein-protein interactions. (4aS,8aR)-NPD-001 induces apoptosis* of acute myeloid leukemia (AML) cell lines. (4aS,8aR)-NPD-001 induces differentiation of distinct AML cell lines including cells with mutated DNMT3A R882 .

HY-13642

RG108 5+ Cited Publications N-Phthalyl-L-tryptophan	DNA Methyltransferase	Cancer
RG108 (N-Phthalyl-L-tryptophan) is a non-nucleoside DNA methyltransferases (DNMTs) inhibitor (IC₅₀=115 nM) that blocks the DNMTs active site. RG108 (N-Phthalyl-L-tryptophan) causes demethylation and reactivation of tumor suppressor genes, but it does not affect the methylation of centromeric satellite sequences .

HY-139664A

(R)-GSK-3685032	DNA Methyltransferase	Cancer
(R)-GSK-3685032 is the R-enantiomer of GSK-3685032. GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible *DNMT1*-selective inhibitor, with an IC₅₀ of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition .

HY-150249

GSK3735967 1 Publications Verification	DNA Methyltransferase	Cancer
GSK3735967 is an selective, reversible, non-nucleoside inhibitor of *DNMT1* with an IC₅₀ value of 40 nM. GSK3735967 contains a planar dicyanopyridine core that can specifically embed DNMT1 bound hemimethylated CpG dinucleotides. GSK3735967 has three binding sites, one of which can bind to histone H4K20me3 .

HY-12746

DC-05 1 Publications Verification	DNA Methyltransferase	Cancer
DC-05 is a DNA methyltransferase 1 (DNMT1) inhibitor, with an IC₅₀ and a K_d of 10.3 μM and 1.09 μM, respectively.

HY-12747

DC_517 2 Publications Verification	DNA Methyltransferase	Cancer
DC_517 is a DNA methyltransferase 1 (DNMT1) inhibitor, with an IC₅₀ and a K_d of 1.7 μM and 0.91 μM, respectively.

HY-149389

PNMT-IN-1	Others	Endocrinology
PNMT-IN-1 (inhibtor 4) is a specific inhibitor of phenylethanolamine N-methyltransferas (PNMT) with a K_i value of 1.2 nM and a IC₅₀ value of 81 nM. PNMT-IN-1 also inhibits the vitality of DNMT1 and DNMT3b, with the IC₅₀ value of 61 μM and 17 μM, respectively, and has an antagonistic effect on epinephrine.PNMT-IN-1 (inhibtor 4 ) is a second generation inhibitor .

HY-139664B

(S)-GSK-3685032	Others	Cancer
(S)-GSK-3685032 is the isomer of GSK-3685032 (HY-139664), and can be used as an experimental control. GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible *DNMT1*-selective inhibitor, with an IC₅₀ of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition .

HY-15229

Guadecitabine sodium 5+ Cited Publications SGI-110 sodium; S-110 sodium	DNA Methyltransferase	Cancer
Guadecitabine sodium (SGI-110 sodium) is a second-generation DNA methyltransferases (DNMT) inhibitor for research of acute myeloid leukemia (AML) and myelodysplastic syndromes (MDS) .

HY-13542

Guadecitabine SGI-110	DNA Methyltransferase	Cancer
Guadecitabine (SGI-110) is a second-generation DNA methyltransferases (DNMT) inhibitor for research of acute myeloid leukemia (AML) and myelodysplastic syndromes (MDS) .

HY-151136

DY-46-2	DNA Methyltransferase	Cancer
DY-46-2 is a high potency and selectivity novel non-nucleoside DNA methyltransferase 3A (DNMT3A) inhibitor with an IC₅₀ value of 0.39 μM .

HY-B2230

Hinokitiol 5 Publications Verification β-Thujaplicin	Keap1-Nrf2 DNA Methyltransferase Virus Protease	Infection Cancer
Hinokitiol is a component of essential oils isolated from Chymacyparis obtusa, reduces Nrf2 expression, and decreases *DNMT1* and UHRF1 mRNA and protein expression, with anti-infective, anti-oxidative, and anti-tumor activities.

HY-124131

DS-437	Histone Methyltransferase	Inflammation/Immunology Cancer
DS-437 is a dual PRMT5/7 inhibitor (IC₅₀s of PRMT5/7=6 μM). DS-437 is selective for PRMT5 and PRMT7 over 29 other human protein-, DNA-, and RNA-methyltransferases. DS-437 is a S-adenosylmethionine (SAM)-competitive inhibitor of PRMT5. DS-437 also inhibits DNMT3A and DNMT3B, with IC₅₀s of 52 and 62 μM, respectively. DS-437 inhibits the methylation of FOXP3 .

HY-15647

BRD9539 1 Publications Verification	Histone Methyltransferase	Cancer
BRD9539 is a histone methyltransferase G9a inhibitor with an IC₅₀ of 6.3 μM. BRD9539 also inhibits PRC2 activity and is inactive against SUV39H1, NSD2 and DNMT1 .

HY-123346

SW155246	DNA Methyltransferase	Cancer
SW155246 is a DNA methyltransferase (DNMT1) selective inhibitor with IC₅₀s of 1.2 and 38 μM for hDNMT1 and mDNMT3A, respectively. SW155246 can be used for the research of cancer and other diseases .

HY-135146

GSK-3484862 Maximum Cited Publications 11 Publications Verification	DNA Methyltransferase	Cancer
GSK-3484862 is a non-covalent inhibitor for DNA methyltransferase (Dnmt1). GSK-3484862 induces DNA hypomethylation to against cancer. GSK-3484862 mediates dramatic demethylation in murine embryonic stem cells with minimal non-specific toxicity .

HY-19826

Isofistularin-3	DNA Methyltransferase ADC Cytotoxin Autophagy Apoptosis	Cancer
Isofistularin-3 is a direct, DNA-competitive *DNMT1* inhibitor, with an IC₅₀ of 13.5 μM. Isofistularin-3, as a DNA demethylating agent, induces cell cycle arrest and sensitization to TRAIL in cancer cells. Isofistularin-3 can be used as an ADC cytotoxin .

HY-103397

Nanaomycin A 2 Publications Verification	DNA Methyltransferase Parasite	Infection Cancer
Nanaomycin A is the first selective *DNMT3B* inhibitor with an IC₅₀ of 500 nM. Nanaomycin A, a quinone antibiotics, reactivates silenced tumor suppressor genes in human cancer cells . Nanaomycin A inhibits in vitro growth of the human malaria parasite Plasmodium falciparum with an IC₈₀ value of 33.1 nM .

HY-15228

RX-3117 1 Publications Verification TV-1360; Fluorocyclopentenylcytosine	Nucleoside Antimetabolite/Analog Apoptosis	Cancer
RX-3117 (TV-1360) is a potent and orally active anticancer and antimetaboliteagent. RX-3117 inhibits DNA methyltransferase 1 (DNMT1). RX-3117 shows antiproliferative and anti-tumour activity. RX-3117 induces cell cycle arrest at S phase and apoptosis .

HY-121093

DC-S239	Histone Methyltransferase	Cancer
DC-S239 is a selective histone methyltransferase SET7 inhibitor with an IC₅₀ value of 4.59 μM. DC-S239 also displays selectivity for DNMT1, DOT1L, EZH2, NSD1, SETD8 and G9a. DC-S239 has anticancer activity .

HY-163803

CM-444	HDAC DNA Methyltransferase	Cancer
CM-444 is inhibitor for HDAC (IC₅₀ is 6 nM-0.6 μM) and DNA methyltransferases (DNMT, IC₅₀ is 1.8-2.3 μM). CM-444 is an inducer for the differentiation of acute myeloid leukemia cells. CM-444 exhibits anti-leukemic activity and improves the survival rate in mouse models .

HY-135146A

(Rac)-GSK-3484862	Others	Cancer
(Rac)-GSK-3484862 is the isomer of GSK-3484862 (HY-135146), and can be used as an experimental control. GSK-3484862 is a non-covalent inhibitor for DNA methyltransferase (Dnmt1). GSK-3484862 induces DNA hypomethylation to against cancer. GSK-3484862 mediates dramatic demethylation in murine embryonic stem cells with minimal non-specific toxicity .

HY-139015

5-Aza-4'-thio-2'-deoxycytidine 5-Aza-T-dCyd; NTX-301	DNA Methyltransferase	Cancer
5-Aza-4'-thio-2'-deoxycytidine (5-Aza-T-dCyd) is an orally active DNA methyltransferase I (DNMT1) inhibitor. 5-Aza-4'-thio-2'-deoxycytidine, a sulfur-containing deoxy-cytidine analog, has the potential for DNA hypomethylating and has antitumor effects .

HY-A0084

Procainamide hydrochloride 4 Publications Verification Procaine amide hydrochloride; SP 100 hydrochloride	DNA Methyltransferase Potassium Channel	Cancer
Procainamide hydrochloride (Procaine amide hydrochloride) is a specific and potent inhibitor of DNA methyltransferase 1 (DNMT1), which reactivates the expression of tumor suppressor factors by demethylating tumor suppressor genes. Procainamide hydrochloride induces vacuolization in various cell types and reduces cell proliferation and migration. Procainamide hydrochloride relaxes airway smooth muscle by activating potassium channels. Procainamide hydrochloride can be used in cancer and arrhythmia research .

HY-A0084A

Procainamide 4 Publications Verification Procaine amide; SP 100	DNA Methyltransferase Potassium Channel	Cardiovascular Disease Cancer
Procainamide (Procaine amide) is a specific and potent inhibitor of DNA methyltransferase 1 (DNMT1), which reactivates the expression of tumor suppressor factors by demethylating tumor suppressor genes. Procainamide induces vacuolization in various cell types and reduces cell proliferation and migration. Procainamide relaxes airway smooth muscle by activating potassium channels. Procainamide can be used in cancer and arrhythmia research .

Cat. No.	Product Name

HY-L203

Methylation Compound Library

259 compounds

Methylation is an epigenetic modification mechanism that involves adding methyl groups to molecules such as DNA and histones, which can alter gene expression without changing the DNA sequence. This process is catalyzed by enzymes such as DNA methyltransferases (DNMTs) and histone methyltransferases (HMTs), and can be reversed by demethylases. The balance of methylation and demethylation is crucial for maintaining cellular function and genomic stability. Abnormal regulation of methylation may lead to a variety of diseases, including cancer, neurological disorders, and developmental abnormalities. A deep understanding of the molecular mechanisms of methylation metabolism is essential for developing therapeutic strategies for diseases associated with methylation dysregulation.

MCE contains 259 compounds targeting methylation/demethylation enzymes, which is of significant value for studying the pathways of methylation metabolism and exploring their mechanisms of action in diseases.

HY-L005

Epigenetics Compound Library

1,340 compounds

Epigenetics refers to changes in phenotype that are not rooted in DNA sequence. Many types of epigenetic processes have been identified, including DNA methylation, alteration in the structure of histone proteins and gene regulation by small noncoding microRNAs. Modification of DNA, protein, or RNA, resulting in changes to the function and/or regulation of these molecules, without altering their primary sequences, reveals the complexities of cellular differentiation, embryology, the regulation of gene expression, aging, cancer, and other diseases.

MCE provide a unique collection of 1,340 epigenetics-related compounds that can be used in the research of the related diseases.

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