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).
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- CAS No.: 120430-77-5
- Formule: C27H29FN4O
- Masse moléculaire:444.54
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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EZH2 |
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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] |
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.
Chemical Information
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CAS No. 120430-77-5
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Masse moléculaire 444.54
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Formule C27H29FN4O
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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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DC-PRC2in-01 Related Classifications
HY-178694 Related Classifications
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