2. Epigenetics
  3. Histone Methyltransferase
  4. 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.

DC-PRC2in-01

DC-PRC2in-01 Chemical Structure

CAS No. : 120430-77-5

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DC-PRC2in-01 Related Antibodies

Top Publications Citing Use of Products

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

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Description

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)[1].

IC50 & Target[1]

EZH2

 

Cellular Effect
Cell Line Type Value Description References
DB IC50
9.62 μM
Compound: 21; DC-PRC2in-01
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
[PMID: 34077206]
KARPAS-422 IC50
5.97 μM
Compound: 21; DC-PRC2in-01
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
[PMID: 34077206]
Pfeiffer IC50
3.77 μM
Compound: 21; DC-PRC2in-01
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
[PMID: 34077206]
SUD4 IC50
5.87 μM
Compound: 21; DC-PRC2in-01
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
[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.

DC-PRC2in-01 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: Pfeiffer and SU-DHL-4 cells
Concentration: 0.625, 1.25, 2.5, and 5 μM
Incubation Time: 2 days for Pfeiffer, 3 days for SU-DHL-4 cells
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%.

Western Blot Analysis[1]

Cell Line: Pfeiffer cells
Concentration: 0, 0.6, 1.3, 2.5, 5, and 10 μM
Incubation Time: 3 days
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.
Molecular Weight

444.54

Formula

C27H29FN4O
CAS No.
SMILES

FC1=CC=C(CN2C(NC3CN(CC3)CCC4=CC=C(C=C4)OC)=NC5=C2C=CC=C5)C=C1
Shipping

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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DC-PRC2in-01 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DC-PRC2in-01120430-77-5Histone MethyltransferasePRC2-related physiology and pathology,PRC2 core proteins,astemizole,EZH2-EED PPI,G0/G1 phase,cocrystal structure,EED,chemical probe,global H3K27me3 levels,PRC2 complex,binding mode,PRC2-driven lymphomasInhibitorinhibitorinhibit

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