DC-PRC2in-01
DC-PRC2in-01 is a potent EZH2-EED interaction inhibitor with an IC50 of 4.21 μM and a Kd of 4.56 μM. DC-PRC2in-01 disrupts the EZH2-EED interaction, leading to degradation of PRC2 core proteins and decrease of H3K27me3 levels, inhibition of PRC2-driven lymphoma cell proliferation, and cell cycle arrest. DC-PRC2in-01 can be used for the research of PRC2-related cancers, such as Diffuse Large B-cell Lymphoma (DLBCL) and follicular lymphoma (FL).
For research use only. We do not sell to patients.
- CAS No.: 120430-77-5
- Formula: C27H29FN4O
- Molecular Weight:444.54
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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- References
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All Histone Methyltransferase Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
EZH2 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| DB | IC50 |
9.62 μM
Compound: 21; DC-PRC2in-01
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Antiproliferative activity against human DB cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo assay
Antiproliferative activity against human DB cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo assay
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[PMID: 34077206] |
| KARPAS-422 | IC50 |
5.97 μM
Compound: 21; DC-PRC2in-01
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Antiproliferative activity against human KARPAS-422 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo assay
Antiproliferative activity against human KARPAS-422 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo assay
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[PMID: 34077206] |
| Pfeiffer | IC50 |
3.77 μM
Compound: 21; DC-PRC2in-01
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Antiproliferative activity against human Pfeiffer cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo assay
Antiproliferative activity against human Pfeiffer cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo assay
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[PMID: 34077206] |
| SUD4 | IC50 |
5.87 μM
Compound: 21; DC-PRC2in-01
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Antiproliferative activity against human SU-DHL-4 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo assay
Antiproliferative activity against human SU-DHL-4 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo assay
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[PMID: 34077206] |
In Vitro
DC-PRC2in-01 (3 days) suppresses proliferation of DLBCL cell lines (Pfeiffer, SU-DHL-4, KARPAS-422, and DB cells) with IC50 values of 3.77, 5.97, 5.87, and 9.62 μM, respectively.[1].
DC-PRC2in-01 (0.625-5 μM, 2-3 days) dose-dependently induces G0/G1 phase cell cycle arrests in Pfeiffer and SU-DHL-4 cells[1].
DC-PRC2in-01 (0-10 μM, 3 days) specifically inhibits the PRC2 activity by disrupting the EZH2-EED interaction, leading to the depletion of PRC2 core components in Pfeiffer cells, resulting in a dose-dependent decrease of H3K27me3 levels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Pfeiffer and SU-DHL-4 cells
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Concentration:0.625, 1.25, 2.5, and 5 μM
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Incubation Time:2 days for Pfeiffer, 3 days for SU-DHL-4 cells
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Result:Dose-dependently induced G0/G1 phase cell cycle arrest in Pfeiffer and SU-DHL-4 cells with a concurrent decrease of cells in G2/M and S. led to an increase of cells in the G0/G1 phase at 5 μM from 52.3 to 76.2% and from 62.2 to 84% for Pfeiffer and SU-DHL-4 cells, respectively. Resulted in a decrease of Pfeiffer cells in G2/M and S phases from 14.9 to 6.2% and from 32.8 to 17.6%, and a decrease of SU-DHL-4 cells in G2/M and S phases from 8.6 to 0% and from 29.2 to 16%.
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Cell Line:Pfeiffer cells
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Concentration:0, 0.6, 1.3, 2.5, 5, and 10 μM
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Incubation Time:3 days
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Result:Caused a dose-dependent loss of H3K27me3, which virtually disappeared at 10 μM. Did not significantly affect the other histone H3 trimethylation marks (H3K4me3, H3K9me3, H3K36me3), suggesting its specific inhibition of PRC2 activity.
- BrdU Incorporation Assay
- Somatic Cell Culture
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Cell Cycle
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Cell Viability Determination by MTT Colorimetric Assay
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- PCNA Immunodetection Proliferation Assay
- Flow cytometric DNA-content cell-cycle staining
- Protocol for Cell Counting and Cell Density Analysis
- MTT Cell Proliferation Assay
Chemical Information
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CAS No. 120430-77-5
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Appearance Solid
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Molecular Weight 444.54
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Formula C27H29FN4O
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Color Light yellow to yellow
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SMILES
FC1=CC=C(CN2C(NC3CN(CC3)CCC4=CC=C(C=C4)OC)=NC5=C2C=CC=C5)C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Purity & Documentation
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Data Sheet (273 KB)
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SDS (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DC-PRC2in-01 Related Classifications
HY-178694 Related Classifications
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