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製品番号: 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).

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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CAS 番号: 120430-77-5
分子式: C₂₇H₂₉FN₄O
分子量:444.54

保管条件:

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

Data Sheet (273 KB)

DC-PRC2in-01 構造式

CAS 番号: 120430-77-5

容量

価格（税別）

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数量

Amount: USD 0.00

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Fluorescent Dye

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

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target^[1]

EZH2

Histone Methyltransferase アイソフォーム固有の製品をすべて表示 :

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]

体外実験

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.

化学情報

CAS 番号 120430-77-5
分子量 444.54
分子式 C₂₇H₂₉FN₄O
SMILES

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

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (273 KB)
COA (2659 KB)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[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

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

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

Minimum order quantity

100 mg

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Amount: USD 0.00

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
化学情報
純度とドキュメンテーション
参考文献

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DC-PRC2in-01

Histone Methyltransferase アイソフォーム固有の製品をすべて表示

生物活性

化学情報

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

DC-PRC2in-01 関連分類

HY-178694 関連分類