2. Epigenetics Apoptosis Immunology/Inflammation NF-κB Metabolic Enzyme/Protease
  3. Histone Methyltransferase Apoptosis Reactive Oxygen Species (ROS)
  4. NSD2/H3K36me2 modulator-1

NSD2/H3K36me2 modulator-1 是一种口服有效的 NSD2/H3K36me2 调节剂。NSD2/H3K36me2 modulator-1 与 NSD2 的 SAM 口袋竞争性结合，有效抑制 NSD2 表达并抑制 H3K36me2 甲基化。NSD2/H3K36me2 modulator-1 还能逆转上皮-间质转化 (EMT)，抑制细胞迁移，并诱导 G0/G1 期阻滞和细胞凋亡 (apoptosis)。NSD2/H3K36me2 modulator-1 可降低线粒体膜电位 (MMP) 并导致活性氧 (ROS) 生成。NSD2/H3K36me2 modulator-1 可用于研究靶向 NSD2 的表观遗传抗癌策略在肝细胞癌 (HCC) 中的应用。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

NSD2/H3K36me2 modulator-1

NSD2/H3K36me2 modulator-1 Chemical Structure

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Customer Review

NSD2/H3K36me2 modulator-1 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

NSD2/H3K36me2 modulator-1 is an orally active NSD2/H3K36me2 modulator. NSD2/H3K36me2 modulator-1 competitively binds to the SAM pocket of NSD2, potently inhibits NSD2 expression and suppresses H3K36me2 methylation. NSD2/H3K36me2 modulator-1 reverses epithelial-mesenchymal transition (EMT), inhibits cell migration, and induces G0/G1 phase arrest and apoptosis. NSD2/H3K36me2 modulator-1 induces decreased Mitochondrial membrane potential (MMP) and subsequent Reactive oxygen species (ROS) generation. NSD2/H3K36me2 modulator-1 can be used to research the NSD2-targeting epigenetic anticancer strategies for hepatocellular carcinoma (HCC)[1].

IC50 & Target[1]

NSD2

 

体外研究
(In Vitro)

NSD2/H3K36me2 modulator-1 (Compound 5b) (24 小时) 对所有五种癌细胞系均显示出 IC50 < 5 μM 的抑制活性 (在 A549, HepG-2, PC-3, HCT-116 和 MCF-7 细胞中的 IC50 值分别为 4.67, 2.12, 2.64, 4.56 和 4.99 μM)，证实了其卓越的广谱抗肿瘤活性[1]。
NSD2/H3K36me2 modulator-1 对 HepG-2 细胞的肿瘤选择性高于 HaCaT 细胞 (IC50 = 19.2 μM) (选择性指数 (SI) = 9.06)[1]。
NSD2/H3K36me2 modulator-1 (2 μM, 24 小时, 37-62 ℃) 能有效结合 HepG-2 细胞内的 NSD2[1]。
NSD2/H3K36me2 modulator-1 (2, 4 μM, 24 小时) 抑制 NSD2 并选择性下调 HepG-2 细胞中 NSD2 介导的 H3K36me2[1]。
NSD2/H3K36me2 modulator-1 (2, 4 μM, 24 小时) 在分子水平上逆转 EMT，这可能是通过抑制 NSD2 并随后下调 TWIST1 实现的，从而导致上皮-间质转化 (EMT) 关键调控因子的表达改变[1]。
NSD2/H3K36me2 modulator-1 (2, 4 μM, 18, 36 小时) 显著抑制 HepG-2 细胞的迁移和增殖[1]。
NSD2/H3K36me2 modulator-1 (2, 4 μM, 24 小时) 对 HepG-2 细胞具有多种调节作用，包括有效诱导细胞凋亡、触发浓度依赖性的 G0/G1 期阻滞、剂量依赖性地降低线粒体膜电位 (MMP) 以及有效促进 ROS 的产生[1]。

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

NSD2/H3K36me2 modulator-1 相关抗体:

Western Blot Analysis[1]

Cell Line: HepG-2 cells
Concentration: 2, 4 μM
Incubation Time: 24 h
Result: Suppressed NSD2 expression in a dose-dependent manner, with notably strong inhibition at 4 μM.
Exhibited high selective inhibition of H3K36me2.
Bound effectively to NSD2 within cells.

Apoptosis Analysis[1]

Cell Line: HepG-2 cells
Concentration: 2, 4 μM
Incubation Time: 24 h
Result: Significantly increased the total apoptosis rate in HepG-2 cells with the elevation of the concentration.
Exhibited slightly superior apoptosis-inducing capacity at the concentration of 4 μM.

Western Blot Analysis[1]

Cell Line: HepG-2 cells
Concentration: 2, 4 μM
Incubation Time: 24 h
Result: Significantly suppressed TWIST1 expression.
Dose-dependently downregulated N-Cadherin and Vimentin.
Upregulated E-Cadherin and Occludin in a dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line: HepG-2 cells
Concentration: 0, 2, 4 μM
Incubation Time: 24 h
Result: Elevated the proportion of HepG-2 cells in G0/G1 phase from 53.8 % to 65.7 %, with the concentration increasing from 0 to 2 μM.
Increased the G0/G1 subpopulation to 79.6 %, with the concentration reaching 4 μM, and exceeded that of 5-Fluorouracil (HY-90006) (73.5 %).
Induced a marked decrease in the levels of cell cycle regulators CDK2, CDK4, and CDK6, effectively blocking cell cycle progression in a concentration-dependent manner.
体内研究
(In Vivo)

NSD2/H3K36me2 modulator-1 (Compound 5b) (20, 40 mg/kg，每日口服，连续 18 天) 在 HepG-2 细胞异种移植模型中表现出强大的抗肿瘤作用，有效抑制肿瘤生长，且安全性良好，这体现在体重、器官指数和形态特征方面没有显著差异[1]。

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

Animal Model: An HepG-2 xenograft model established in female BALB/c nude mice (6-8 weeks old)[1]
Dosage: 20, 40 mg/kg
Administration: daily oral gavage (p.o.) for 18 consecutive days
Result: Significantly suppressed tumor growth in a dose-dependent manner.
Exhibited the strongest antitumor effect at 40 mg/kg.
分子量

695.37

Formula

C41H59ClN2O5
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

NSD2/H3K36me2 modulator-1 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:

NSD2/H3K36me2 modulator-1Histone MethyltransferaseApoptosisReactive Oxygen Species (ROS)Panaxadiol derivativesNSD2H3K36me2EMTEpigenetic modulatorsAntitumor agentsHepatocellular carcinomaInhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
NSD2/H3K36me2 modulator-1
目录号：
HY-179427
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z