One Compound. Two Epigenetic Targets: Exploring HDAC/EZH2 Dual Inhibition
Epigenetics / Research insights
ONE COMPOUND.
TWO EPIGENETIC TARGETS.
How can targeting HDACs and EZH2 in the same molecule support the study of chromatin regulation and cancer cell biology?
Gene expression depends not only on DNA sequence, but also on how DNA is organised around histone proteins. Two important regulatory activities are histone deacetylation and histone methylation. Studying them together offers a way to investigate how different epigenetic pathways influence cell state.
HDACs/EZH2-IN-1 (Compound 22a) is a dual-target research compound used to investigate HDAC and EZH2 inhibition in laboratory models. Its reported activity includes HDAC1, HDAC6 and the EZH2 Y641N variant.
| HDACs/EZH2-IN-1 | COMPOUND 22a | ||
| ↙ ↘ | ||
|
ERASER HDACHDAC1 / HDAC6 Histone deacetylation |
WRITER EZH2Y641N variant H3K27 methylation |
|
| ↘ ↙ | ||
| CHROMATIN & GENE-EXPRESSION RESEARCH | ||
Simplified pathway illustration. Cellular responses depend on the model, target engagement and experimental conditions.
Why explore two epigenetic mechanisms together?
HDAC enzymes remove acetyl groups from histones and other proteins. Histone deacetylation is frequently associated with reduced chromatin accessibility and changes in transcriptional activity.
EZH2, the catalytic component of Polycomb Repressive Complex 2 (PRC2), contributes to methylation of histone H3 at lysine 27 (H3K27). H3K27 trimethylation is often associated with transcriptional repression.
Dual-target molecules allow researchers to investigate both enzymatic activities in a single experimental system. They do not guarantee a particular chromatin state or therapeutic result; these outcomes must be established in the relevant assay and cell model.
REPORTED COMPOUND ACTIVITY
Three data points. One research tool.
|
HDAC1 0.23 µM IC50 |
HDAC6 0.07 µM IC50 |
EZH2 Y641N 98% inhibition at 50 nM |
Values reported in the QuantiMol product description; biochemical and cellular results are not directly interchangeable.
Where does this approach fit in research?
Reported experimental applications of HDACs/EZH2-IN-1 include studies involving:
|
01 EZH2-mutant lymphoma models |
02 Acute myeloid leukaemia cell models |
03 Differentiation and apoptosis research |
FEATURED RESEARCH COMPOUND
HDACs/EZH2-IN-1
Compound 22a | QuantiMol SKU: QM-0154276
Explore the product description and request a quotation, datasheet, SDS or COA directly from the QuantiMol product page.
| EXPLORE HDACs/EZH2-IN-1 → |
EXTEND YOUR EXPERIMENTAL TOOLKIT
Explore complementary epigenetics compounds
Depending on your study design, single-pathway inhibitors and reader-domain probes can provide useful comparison tools.
|
HDAC-IN-27 (dihydrochloride) Class I HDAC inhibitor | HDAC1–3 research |
|
EZH2-IN-2 EZH2 methyltransferase inhibition research |
|
I-CBP112 CBP/p300 bromodomain probe | Epigenetic reader research |
Looking for additional oncology research tools? Browse QuantiMol Cancer Research Compounds →
Scientific context & further reading
HDAC regulation of gene expression | PRC2, EZH2 and chromatin regulation
For laboratory research use only. Not for human or veterinary use. Reported biochemical and cell-based results are study- and assay-dependent. This article describes research applications, not established clinical efficacy.