2. Epigenetics
  3. Histone Methyltransferase
  4. DC-PRC2in-01

DC-PRC2in-01 是一种强效的 EZH2-EED 相互作用抑制剂，其 IC50 为 4.21 μM，Kd 为 4.56 μM。DC-PRC2in-01 破坏 PRC2 复合体的稳定性，导致 PRC2 核心蛋白降解和 H3K27me3 水平降低，从而抑制 PRC2 驱动的淋巴瘤细胞增殖并导致细胞周期阻滞。DC-PRC2in-01 可用于研究 PRC2 相关的癌症，如弥漫性大 B 细胞淋巴瘤 (DLBCL) 和滤泡性淋巴瘤 (FL)。

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DC-PRC2in-01

DC-PRC2in-01 Chemical Structure

CAS No. : 120430-77-5

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DC-PRC2in-01 相关抗体

Top Publications Citing Use of Products

查看 Histone Methyltransferase 亚型特异性产品:

查看所有亚型
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

体外研究
(In Vitro)

DC-PRC2in-01 (3 天) 抑制 DLBCL 细胞系 (Pfeiffer、SU-DHL-4、KARPAS-422 和 DB 细胞) 的增殖，IC50 值分别为 3.77、5.97、5.87 和 9.62 μM[1]。
DC-PRC2in-01 (0.625-5 μM，2-3 天) 以计量依赖的方式在 Pfeiffer 和 SU-DHL-4 细胞中诱导 G0/G1 期细胞周期阻滞[1]。
DC-PRC2in-01 (0-10 μM，3 天) 通过破坏 EZH2-EED 相互作用特异性地抑制 PRC2 活性，导致 Pfeiffer 细胞中 PRC2 核心成分的耗竭，从而导致 H3K27me3 水平呈剂量依赖性下降[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

DC-PRC2in-01 相关抗体:

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.
分子量

444.54

Formula

C27H29FN4O
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

DC-PRC2in-01 相关分类

  • 摩尔计算器

  • 稀释计算器

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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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