Date published: 2025-10-25

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MLL3 Inhibitors

MLL3, also known as mixed-lineage leukemia 3, is a member of the MLL (mixed-lineage leukemia) family of histone lysine methyltransferases. These enzymes play critical roles in the epigenetic regulation of gene expression by catalyzing the methylation of histone proteins, particularly histone H3 lysine 4 (H3K4), a modification associated with transcriptional activation. MLL3 is involved in the deposition of mono-, di-, and trimethylation marks on H3K4, which contribute to the formation of transcriptionally permissive chromatin states necessary for the activation of gene expression programs essential for various cellular processes, including development, differentiation, and proliferation. As a key epigenetic regulator, MLL3 exerts its functions by associating with transcriptional regulatory complexes and chromatin-modifying enzymes, orchestrating the precise spatial and temporal control of gene expression patterns required for normal cellular function. The inhibition of MLL3 activity can be achieved through various mechanisms that disrupt its catalytic function, protein-protein interactions, or subcellular localization. One common strategy involves the development of small molecule inhibitors that target the catalytic SET domain of MLL3, thereby blocking its methyltransferase activity and disrupting the deposition of methyl marks on histone H3. Additionally, inhibition of protein-protein interactions essential for the formation of functional MLL3-containing complexes can disrupt its recruitment to target genes and subsequent chromatin modification. Furthermore, modulation of upstream signaling pathways or post-translational modifications that regulate MLL3 activity can also serve as effective means of inhibition. By interfering with the epigenetic regulation of gene expression mediated by MLL3, inhibition strategies offer avenues for studying the functional consequences of MLL3 dysregulation and exploring interventions targeting MLL3-associated diseases.

Items 1 to 10 of 11 total

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Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

UNC1999

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

Dual inhibitor of histone methyltransferases (HMTs) G9a and GLP, influencing histone methylation and chromatin remodeling. UNC1999 can potentially modulate MLL3 activity by affecting the epigenetic landscape and histone modifications related to MLL3 function.

9-[5-Deoxy-5-[[cis-3-[2-[6-(1,1-dimethylethyl)-1H-benzimidazol-2-yl]ethyl]cyclobutyl](1-methylethyl)amino]-β-D-ribofuranosyl]-9H-purin-6-amine

1380288-87-8sc-500607
50 mg
$13500.00
(0)

DOT1L (DOT1-like) inhibitor targeting histone H3 lysine 79 (H3K79) methylation. EPZ-5676 can influence MLL3 indirectly by affecting a shared pathway involved in histone methylation, potentially modulating MLL3-dependent gene expression.

GSK126

1346574-57-9sc-490133
sc-490133A
sc-490133B
1 mg
5 mg
10 mg
$90.00
$238.00
$300.00
(0)

Enhancer of zeste homolog 2 (EZH2) inhibitor influencing histone methylation. GSK126 targets EZH2, potentially affecting the trimethylation of histone H3 lysine 27 (H3K27) and indirectly modulating MLL3 activity through epigenetic regulation.

(S)-2-(4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-N-(4-hydroxyphenyl)acetamide

202590-98-5sc-501130
2.5 mg
$330.00
(0)

Bromodomain and extraterminal (BET) protein inhibitor affecting chromatin remodeling. OTX015 targets BET proteins, potentially modulating MLL3 activity by influencing the recruitment of MLL3 to specific chromatin regions and altering histone modifications.

SGC-CBP30

1613695-14-9sc-473871
sc-473871A
5 mg
10 mg
$178.00
$338.00
(0)

CREB-binding protein (CBP) and p300 bromodomain inhibitor affecting histone acetylation. SGC-CBP30 can modulate MLL3 indirectly by influencing histone acetylation patterns and chromatin structure associated with MLL3-dependent gene regulation.

GSK343

1346704-33-3sc-397025
sc-397025A
5 mg
25 mg
$148.00
$452.00
1
(0)

EZH2 inhibitor affecting histone methylation. GSK343 targets EZH2, potentially influencing MLL3 indirectly through alterations in the trimethylation of histone H3 lysine 27 (H3K27) and the epigenetic regulation of shared target genes.

C646

328968-36-1sc-364452
sc-364452A
10 mg
50 mg
$260.00
$925.00
5
(1)

Histone acetyltransferase (HAT) inhibitor targeting p300/CBP-associated factor (PCAF). C646 can potentially modulate MLL3 activity by affecting histone acetylation patterns associated with MLL3-dependent gene expression and chromatin remodeling.

(±)-JQ1

1268524-69-1sc-472932
sc-472932A
5 mg
25 mg
$226.00
$846.00
1
(0)

BET protein inhibitor affecting chromatin structure. JQ1 targets BET proteins, potentially influencing MLL3 activity by modulating the recruitment of MLL3 to specific chromatin regions and altering histone modifications associated with MLL3-dependent processes.

CPI-203

1446144-04-2sc-501599
1 mg
$170.00
(0)

BET protein inhibitor influencing chromatin structure. CPI-203 targets BET proteins, potentially modulating MLL3 activity by affecting the recruitment of MLL3 to specific chromatin regions and altering histone modifications associated with MLL3-dependent processes.

UNC0638

1255580-76-7sc-397012
10 mg
$315.00
(0)

G9a and GLP histone methyltransferase inhibitor affecting histone methylation. UNC0638 can potentially modulate MLL3 activity by influencing the epigenetic landscape and histone modifications associated with MLL3-dependent gene regulation.