Date published: 2026-4-29

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MLL4 Inhibitors

MLL4 inhibitors represent a class of small molecules characterized by their ability to selectively target and interfere with the activity of the MLL4 protein, also known as KMT2D (Lysine Methyltransferase 2D). MLL4 is a crucial member of the histone methyltransferase family, playing a pivotal role in the epigenetic regulation of gene expression. These inhibitors are primarily designed to disrupt the methyltransferase function of MLL4, which is responsible for catalyzing the addition of methyl groups to histone H3 lysine 4 (H3K4). This epigenetic modification, known as histone methylation, plays a central role in controlling gene transcription and, consequently, cellular processes such as differentiation, development, and proliferation. Chemically, MLL4 inhibitors often possess specific structural features that allow them to target the SET domain of MLL4. The SET domain is a conserved catalytic domain found in lysine methyltransferases, and it is critical for their methyltransferase activity. MLL4 inhibitors are designed to bind to this domain, thereby disrupting the enzyme's ability to methylate histone H3 at lysine 4. By inhibiting this epigenetic modification, MLL4 inhibitors can influence gene expression patterns, making them valuable tools for researchers studying the intricacies of epigenetic regulation and its role in various cellular processes. Additionally, these inhibitors can help elucidate the biological functions of MLL4 and its involvement in normal and disease-related molecular pathways, paving the way for a deeper understanding of gene regulation at the epigenetic level.
Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

N-[3-[[2-[[4-[[1-(2-Fluoroethyl)-3-azetidinyl]amino]-2-methoxyphenyl]amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]phenyl]-2-propenamide

1375465-09-0sc-499486
5 mg
$340.00
(0)

This is a small molecule inhibitor that targets multiple lysine methyltransferases, including KMT2B. It has been reported to disrupt the interaction between KMT2B and its coactivators, thereby inhibiting its methyltransferase activity.

THZ1

1604810-83-4sc-507542
1 mg
$95.00
(0)

Although THZ1 is primarily known as a CDK7 inhibitor, it also inhibits MLLTHZ1 has shown promise in research studies that investigate several cancer types, including acute myeloid leukemia and breast cancer.

UNC1999

1431612-23-5sc-475314
5 mg
$142.00
1
(0)

UNC1999 is a selective inhibitor of the lysine methyltransferases KMT2A (MLL1) and KMT2B (MLL4). It has demonstrated potent inhibitory activity against these enzymes in research studies.

A-366

1527503-11-2sc-507495
10 mg
$195.00
(0)

A-366 is a small molecule inhibitor that selectively targets KMT2B and KMT2D (MLL2). It has been reported to inhibit the methyltransferase activity of these enzymes and exhibit antiproliferative effects in cancer cell lines.

Epz004777

1338466-77-5sc-507560
100 mg
$575.00
(0)

EPZ004777 is a potent and selective inhibitor of KMT2B. It binds to the catalytic SET domain of the enzyme and inhibits its methyltransferase activity.

UNC 1215

1415800-43-9sc-475020
10 mg
$380.00
(0)

UNC 1215 is a small molecule inhibitor that has been developed to target MLL3 and MLL4, both of which belong to the same family of lysine methyltransferases. It has been used in research to explore the biological functions of MLL4.

EPZ6438

1403254-99-8sc-507456
1 mg
$66.00
(0)

E7438 is an inhibitor that has been developed to target various histone methyltransferases, including MLLIt.

GSK126

1346574-57-9sc-490133
sc-490133A
sc-490133B
1 mg
5 mg
10 mg
$92.00
$243.00
$306.00
(0)

GSK126 is a selective inhibitor of the lysine methyltransferase KMT2B. It binds to the catalytic SET domain of KMT2B and inhibits its methyltransferase activity.

SP2509

1423715-09-6sc-492604
5 mg
$284.00
(0)

SP-2509 is a small molecule inhibitor that targets the histone methyltransferases MLL1 and MLLIt has been explored in research studies.