DNA Methyltransferases

Cat. No.

A10292

CAS No.

2353-33-5

Decitabine

Synonyms: Dacogen; 5-Aza-dC

Decitabine is a hypomethylating agent.It hypomethylates DNA by inhibiting DNA methyltransferase.

Cat. No.

A12744

CAS No.

929901-49-5

Guadecitabine (SGI-110)

Synonyms: SGI110

SGI-110 is a second generation DNA-hypomethyating agent.

Cat. No.

A10105

CAS No.

320-67-2

Azacitidine

Synonyms: 5-azacytidine; Mylosar; Ladakamycin; Vidaza

Azacitidine is a chemical analogue of the cytosine nucleoside used in DNA and RNA that is mainly used in the treatment of myelodysplastic syndrome (MDS).

Cat. No.

A11432

CAS No.

382607-78-5

O6BTG-octylglucoside

Synonyms: Glucose-conjugated MGMT inhibitor

O6BTG-octylglucoside is a potent O6-methylguanine-DNAmethyl-transferase (MGMT) inhibitor, with IC50s of 32 nM in vitro (cell extracts) and 10 nM in HeLa S3 cells.

Cat. No.

A12721

CAS No.

3690-10-6

Zebularine

Synonyms: NSC309132; 4-Deoxyuridine

Zebularine (NSC309132; 4-Deoxyuridine) is a DNA methyltransferase inhibitor.

Cat. No.

A12785

CAS No.

192441-08-0

Lomeguatrib

Synonyms: O6-(4-bromothenyl)guanine

Lomeguatrib is a potent inhibitor of O6-alkylguanine-DNA-alkyltransferase.

Cat. No.

A13054

CAS No.

48208-26-0

RG108

RG108 is a non-nucleoside inhibitor of DNA methyltransferase with IC50 of 115 nM.

Cat. No.

A13391

CAS No.

105330-94-7

6-Methyl-5-azacytidine

6-Methyl-5-azacytidine is a potent DNMT inhibitor.

Cat. No.

A13706

CAS No.

19916-73-5

O6-Benzylguanine

Synonyms: CCRIS 9383

O6-Benzylguanine is an effective substrate and efficient inactivator of DNA alkyltransferase. O6-Benzylguanine is an inhibitor of MGMT.

Cat. No.

A14120

CAS No.

1020149-73-8

SGI 1027

SGI 1027 is a DNMT inhibitor with IC50 of 6, 8, 7.5 uM for DNMT1, DNMT3A, and DNMT3B, respectively.

Cat. No.

A14240

CAS No.

614-39-1

Procainamide HCl

Procainamide HCl is a sodium channel blocker, and also a DNA methyltransferase inhibitor.

Cat. No.

A17173

CAS No.

1846570-31-7

CM-272

CM-272 is a reversible dual small molecule inhibitor against G9a and DNMTs in hematological malignancies. CAS: 1846570-31-7 (free base) 1846570-32-8 (TFA)

Cat. No.

A17328

CAS No.

11042-64-1

γ-Oryzanol

Synonyms: Oliver; Gammariza; Gamma-Oryzanol

γ-Oryzanol is an effective inhibitor of DNA methyltransferases (DNMTs) with a primary focus on DNMT1 and DNMT3a. It demonstrates significant inhibitory activity, with an IC50 of 3.2 μM for DNMT1 and 22.3 μM for DNMT3a. This compound has important implications for epigenetic research and may be useful in studies exploring gene expression regulation and potential therapeutic applications in cancer and other diseases associated with aberrant DNA methylation.

Cat. No.

A18692

CAS No.

1846570-40-8

CM-579

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.

Cat. No.

A22095

CAS No.

420092-79-1

SW155246

SW155246 is a potent and selective DNMT1 (DNA methyltransferase 1) inhibitor with IC50 of 1.2 μM. SW155246 induces re-expression of the tumor suppressor geneRASSF1 in A549 cells.

Cat. No.

A24058

CAS No.

1418131-46-0

RSC133

RSC133 is a dual epigenetic modulator that inhibits both histone deacetylases (HDACs) and DNA methyltransferases (DNMTs). It effectively enhances the reprogramming of human somatic cells into induced pluripotent stem cells (iPSCs) and supports the maintenance of pluripotency by promoting an undifferentiated state. RSC133 is a valuable tool for stem cell research and epigenetic reprogramming studies.

Cat. No.

A24341

CAS No.

2170137-61-6

GSK-3685032

GSK-3685032 is a first-in-class, reversible, non-time-dependent, and noncovalent inhibitor that selectively targets DNA methyltransferase 1 (DNMT1), with an IC₅₀ of 0.036 μM. It induces robust DNA demethylation, leading to transcriptional activation and inhibition of cancer cell growth, making it a promising candidate for epigenetic therapy in oncology.

Cat. No.

A24342

CAS No.

2170136-65-7

GSK-3484862

GSK-3484862 is a non-covalent and selective inhibitor of DNA methyltransferase 1 (DNMT1). It effectively induces DNA hypomethylation, making it a promising agent for cancer therapy. In murine embryonic stem cells, GSK-3484862 mediates robust and targeted demethylation with minimal off-target toxicity, supporting its potential for epigenetic reprogramming and therapeutic applications.

Cat. No.

A24343

CAS No.

2436747-44-1

Bobcat339 hydrochloride

Bobcat339 hydrochloride is a potent and selective cytosine-based inhibitor of TET (ten-eleven translocation) enzymes, with IC₅₀ values of 33 μM for TET1 and 73 μM for TET2. By inhibiting TET-mediated DNA demethylation, it modulates epigenetic regulation and gene transcription. Bobcat339 hydrochloride is a valuable tool in epigenetics research and serves as a potential lead compound for developing therapeutics targeting DNA methylation-related diseases.

Cat. No.

A24344

CAS No.

890643-16-0

DC-05

DC-05 is a DNA methyltransferase 1 (DNMT1) inhibitor with an IC₅₀ of 10.3 μM and a binding affinity (K\_d) of 1.09 μM. It interferes with DNMT1-mediated DNA methylation, making it a useful compound for studying epigenetic regulation and exploring potential therapeutic applications in diseases involving aberrant DNA methylation.

Cat. No.

A24345

CAS No.

10356-76-0

5-Fluoro-2'-deoxycytidine (FdCyd, NSC-48006)

Synonyms: FdCyd; NSC-48006

5-Fluoro-2'-deoxycytidine (FdCyd) is a fluoropyrimidine nucleoside analogue that functions as a DNA methyltransferase (DNMT) inhibitor. It also serves as a tumor-selective prodrug of 5-fluoro-2′-dUMP, a thymidylate synthase inhibitor. FdCyd induces cell cycle arrest in tumor cells by activating the DNA damage response and exhibits potent anti-tumor activity, making it a promising agent in epigenetic and chemotherapeutic cancer research.

Cat. No.

A24361

CAS No.

110659-91-1

Psammaplin A

Psammaplin A, a marine-derived metabolite, is a potent inhibitor of HDAC1 (IC50: 45 nM), DNA methyltransferases (IC50: 18.6 nM), and aminopeptidase N (IC50: 18 μM). It also suppresses DNA topoisomerase and farnesyl protein transferase activities. As a PPARγ activator, Psammaplin A induces apoptosis and exhibits antitumor, anti-inflammatory, and anti-angiogenic properties. Additionally, it demonstrates antibacterial activity against Gram-positive bacteria by inhibiting DNA synthesis and DNA

Cat. No.

A24362

CAS No.

1445703-64-9

TFMB-(S)-2-HG

TFMB-(S)-2-HG is a potent inhibitor of TET2 and EglN prolyl hydroxylases. It downregulates Wnt3a and intranuclear β-catenin protein expression, and inhibits osteogenic differentiation of cells. TFMB-(S)-2-HG shows potential for research in acute myeloid leukemia (AML).

Cat. No.

A24363

CAS No.

838-07-3

5-Methyl-2'-deoxycytidine

5-Methyl-2'-deoxycytidine (5mdC) is an endogenous substrate of DNA methyltransferases, including mammalian 5-C-MTase, and binds to DNA in a manner dependent on DNA stem-loop structure formation. It directs de novo DNA methylation by serving as a methylation mark, promoting methylation of adjacent CpG sites in single-stranded DNA via cis-acting mechanisms. 5mdC regulates DNA methylation patterns by recruiting methyltransferases to specific chromatin regions, influencing chromatin condensation and gene expression. In plant cells, its distribution correlates with cell proliferation and differentiation stages, with lower methylation levels in proliferating cells and higher levels in differentiated cells.

Cat. No.

A24364

CAS No.

1105110-83-5

DY-46-2

DY-46-2 is a highly potent and selective non-nucleoside inhibitor of DNA methyltransferase 3A (DNMT3A), exhibiting an IC50 value of 0.39 μM.