Date published: 2026-4-1

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Dnmt3a Inhibitors

Dnmt3a Inhibitors target and modulate the activity of Dnmt3a, or DNA (cytosine-5)-methyltransferase 3A. Dnmt3a is a critical enzyme involved in the epigenetic modification of DNA through the process of DNA methylation. Structurally, Dnmt3a is a member of the DNA methyltransferase family, possessing catalytic domains that enable it to transfer methyl groups to cytosine residues in DNA. This epigenetic modification involves the addition of a methyl group to the cytosine base, predominantly at CpG dinucleotides, and plays a fundamental role in gene regulation, genomic stability, and cellular differentiation. The functions of Dnmt3a are integral to epigenetic regulation and cellular identity. Dnmt3a, along with its counterpart Dnmt3b, is primarily responsible for de novo DNA methylation, meaning it establishes DNA methylation patterns during development and in response to environmental cues. This process of DNA methylation can result in the silencing of genes, impacting various cellular processes such as cell differentiation and development. Dnmt3a Inhibitors are typically designed as small molecules or compounds engineered to interfere with the catalytic activity of Dnmt3a, disrupting its ability to add methyl groups to DNA.

Items 1 to 10 of 12 total

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Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

SGI-1027

1020149-73-8sc-473875
10 mg
$213.00
(0)

SGI-1027 is a quinoline compound that inhibits DNA methyltransferases, including Dnmt3a. It acts by binding to the catalytic site of the enzyme, preventing its interaction with the substrate.

5-Azacytidine

320-67-2sc-221003
500 mg
$280.00
4
(1)

5-Azacytidine is a nucleoside analog that incorporates into DNA and RNA. Once integrated, it inhibits DNA methyltransferases, including Dnmt3a, leading to demethylation and reactivation of silenced genes.

5-Aza-2′-Deoxycytidine

2353-33-5sc-202424
sc-202424A
sc-202424B
25 mg
100 mg
250 mg
$218.00
$322.00
$426.00
7
(1)

Decitabine is another nucleoside analog similar to 5-Azacytidine. It gets incorporated into DNA and acts as a covalent inhibitor of DNA methyltransferases, leading to decreased activity of enzymes like Dnmt3a.

RG 108

48208-26-0sc-204235
sc-204235A
10 mg
50 mg
$131.00
$515.00
2
(1)

RG108 is a non-nucleoside inhibitor of DNA methyltransferases. It specifically inhibits Dnmt3a by blocking its active site without causing DNA damage.

Procainamide hydrochloride

614-39-1sc-202297
10 g
$53.00
(1)

Procainamide has been found to inhibit DNA methylation. It can inhibit Dnmt3a by interacting with its catalytic domain, leading to reduced methylation activity.

1-Hydrazinophthalazine Hydrochloride

304-20-1sc-206167
10 g
$280.00
(0)

Studies show Hydralazine has inhibitory effects on DNA methyltransferases. It can inhibit Dnmt3a, leading to the reversal of aberrant methylation patterns observed in certain pathological conditions.

Zebularine

3690-10-6sc-203315
sc-203315A
sc-203315B
10 mg
25 mg
100 mg
$129.00
$284.00
$1004.00
3
(1)

Zebularine is a cytidine analog that acts as an inhibitor of DNA methyltransferases. It gets incorporated into DNA and forms a covalent complex with Dnmt3a, thereby inhibiting its activity.

Disulfiram

97-77-8sc-205654
sc-205654A
50 g
100 g
$53.00
$89.00
7
(1)

Disulfiram has been found to inhibit DNA methyltransferases. It can down-regulate Dnmt3a activity, although its precise mechanism in relation to Dnmt3a remains to be elucidated.

BIX01294 hydrochloride

1392399-03-9sc-293525
sc-293525A
sc-293525B
1 mg
5 mg
25 mg
$37.00
$112.00
$408.00
(1)

BIX-01294 is a specific inhibitor of G9a histone methyltransferase, but it also shows inhibitory effects on Dnmt3a. Its mechanism might involve disruption of Dnmt3a's interaction with specific cofactors essential for its activity.

Chaetocin

28097-03-2sc-200893
200 µg
$126.00
5
(1)

Although primarily known as an inhibitor of the SUV39H1 histone methyltransferase, chaetocin also shows inhibition of DNA methyltransferases. It can down-regulate Dnmt3a activity, potentially by modulating the cellular redox state, which is crucial for the function of these enzymes.