2. Epigenetics
  3. Histone Methyltransferase Epigenetic Reader Domain
  4. EED-IN-3

EED-IN-3 是一种口服有效的 EED 抑制剂。EED-IN-3 通过与 EED (IC50 = 0.62 μM) 结合有效抑制 PRC2，并下调 H3K27me3 水平。EED-IN-3 可以高效选择性地抑制 PC3 细胞，IC50 为 3.69 μM，并可以显著抑制集落形成和迁移。EED-IN-3 可用于前列腺癌症的研究[1]。

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EED-IN-3 Chemical Structure

EED-IN-3 Chemical Structure

CAS No. : 3051817-48-9

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EED-IN-3 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

EED-IN-3 is an orally active EED inhibitor. EED-IN-3 effectively inhibits PRC2 by binding to EED (IC50 = 0.62 μM) and downregulates H3K27me3. EED-IN-3 can efficiently and selectively inhibit PC3 cells with the IC50 of 3.69 μΜ and could significantly suppress colony formation and migration. EED-IN-3 can be used for research on prostate cancer[1].

体外研究
(In Vitro)

EED-IN-3 (Compound 39) (7 天) 对 PC3 细胞表现出高选择性的抗癌活性并且对正常细胞表现出低毒性[1]。
EED-IN-3 (0-16 μM) 显著降低 PC3 细胞中 H3K27me3 的水平[1]。
EED-IN-3 (0-16 μM，24 或 48 小时) 可以以时间和浓度依赖的方式抑制 PC3 细胞的迁移和侵袭[1]。
EED-IN-3 (8-16 μM，12 天) 显著抑制 PC3 细胞中细胞集落的形成[1]。

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

EED-IN-3 相关抗体:

Cell Viability Assay[1]

Cell Line: PC3, EC109, KYSE150, PC9 and H9C2 cells
Concentration: /
Incubation Time: 7 days
Result: Significantly selective inhibited PC3 (IC50 = 3.69 μM), instead of EC109 (IC50 = 26.8 μM), KYSE150 (IC50 = 24.53 μM) and PC9(IC50 = 18.43 μM).

Western Blot Analysis[1]

Cell Line: PC3 cells
Concentration: 3 μM or 6 μM
Incubation Time: 4 days
Result: Effectively upregulated the expression of E-Cadherin and downregulated the expression of N-Cadherin.
体内研究
(In Vivo)

EED-IN-3 (Compound 39) (single dose 2 g/kg；i.g.) 在 C57BL/6 野生型小鼠体内具有相对较弱的毒性[1]。
EED-IN-3 (50 mg/kg-100 mg/kg；i.g.；每日一次；持续 14 天) 对注射了 PC3 细胞的 BALB/C-nu 小鼠的肿瘤生长具有显著的抑制作用[1]。

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

Animal Model: C57BL/6 wild-type mice (8-12 weeks)[1]
Dosage: Single dose 2 g/kg
Administration: Oral gavage (i.g.)
Result: Did not cause any abnormal weight changes and did not cause histopathological changes in important organs.
Animal Model: 1×107 PC3 cells injected the BALB/C-nu mice[1]
Dosage: 50 mg/kg or 100 mg/kg
Administration: Oral gavage (i.g.); once daily for 14 days
Result: Inhibited tumor growth by nearly 50% in the 50 mg/kg/day group and nearly 80 % in the 100 mg/kg/day group, steadily increased body weight.
分子量

451.51

Formula

C25H29N3O5
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

EED-IN-3 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

EED-IN-33051817-48-9Histone MethyltransferaseEpigenetic Reader DomainEEDPRC2anticancerprostate cancerInhibitorinhibitorinhibit

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