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Art. -Nr.: HY-178694

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DC-PRC2in-01

DC-PRC2in-01 is a potent EZH2-EED interaction inhibitor with an IC₅₀ of 4.21 μM and a K_d 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).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 120430-77-5
Formel: C₂₇H₂₉FN₄O
Molecular Weight:444.54

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (273 KB)

DC-PRC2in-01 Chemical Structure

CAS. Nr.: 120430-77-5

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

EZH2

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen :

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.

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.

Chemical Information

CAS. Nr. 120430-77-5
Molecular Weight 444.54
Formel C₂₇H₂₉FN₄O
SMILES

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

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Du D, et al. Structure-Guided Development of Small-Molecule PRC2 Inhibitors Targeting EZH2-EED Interaction. J Med Chem. 2021;64(12):8194-8207. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

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100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Reinheit & Dokumentation
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DC-PRC2in-01

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

DC-PRC2in-01 Related Classifications

HY-178694 Related Classifications