2. Epigenetics Metabolic Enzyme/Protease Cell Cycle/DNA Damage Apoptosis
  3. Histone Methyltransferase HSP Apoptosis
  4. EZH2/HSP90-IN-29

EZH2/HSP90-IN-29 是 EZH2 和 HSP90 的双效抑制剂，IC50 值分别为 6.29 nM 和 60.1 nM。EZH2/HSP90-IN-29 上调细胞凋亡 (apoptosis)/坏死相关基因的表达，在 M 期诱导细胞阻滞，抑制活性氧分解代谢途径。EZH2/HSP90-IN-29 能够穿过血脑屏障 (BBB)。

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EZH2/HSP90-IN-29 Chemical Structure

EZH2/HSP90-IN-29 Chemical Structure

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Customer Review

EZH2/HSP90-IN-29 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 SETDB1/KMT2G SETD2/KMT3A SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

查看 HSP 亚型特异性产品:

查看所有亚型
HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EZH2/HSP90-IN-29 is a dual inhibitor for EZH2 and HSP90, with IC50s of 6.29 nM and 60.1 nM, for EZH2 and HSP90, respectively. EZH2/HSP90-IN-29 increases apoptosis/necrosis-related gene expression, induces cell cycle arrest at M phase and inhibits reactive oxygen species (ROS) catabolism pathway. EZH2/HSP90-IN-29 is able to cross the blood-brain-barrier (BBB)[1].

IC50 & Target

EZH2

6.29 nM (IC50)

HSP90

60.1 nM (IC50)

体外研究
(In Vitro)

EZH2/HSP90-IN-29 通过调节 EZH2 和 HSP90 分子伴侣的平衡，抑制 TMZ 耐药胶质母细胞瘤 (GBM) 的增殖 (IC50 为 1.015 μM)[1]。
EZH2/HSP90-IN-29 (5 μM) 减少着丝粒蛋白 (CENP)、CDK1 和细胞周期蛋白 B1，从而调节着丝粒组装和有丝分裂，在 M 期阻滞细胞周期[1]。
EZH2/HSP90-IN-29 (2 μM) 通过下调 Pt3R 细胞中 RB 结合蛋白 (RBBP8)、BRCA1、DNA 修复和重组蛋白 RAD54B、RAD21以及交叉连接核酸内切酶 EME1 和 BRIP1 的表达来抑制 DNA 修复能力[1]。
EZH2/HSP90-IN-29 (5 μM) 上调 ROS 和裂解 caspase-3 的水平，增加线粒体衍生的 ROS[1]。

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

EZH2/HSP90-IN-29 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: Pt3R
Concentration: 0-50 μM
Incubation Time: 72 h
Result: Inhibited 50% cell viability with concentration of 1.015 μM.

Western Blot Analysis[1]

Cell Line: Pt3 and Pt3R
Concentration: 0-5 μM
Incubation Time: 72 h
Result: Decreased expressions of CDK1 and cyclin B1, increased cleaved caspase-3.
体内研究
(In Vivo)

EZH2/HSP90-IN-29 (20 mg/kg，腹腔注射，每周两次，共 40 天) 抑制 Pt3R 异种移植 NOD.CB17-Prkdcscid/NCrCrl 小鼠中 Pt3R 诱导的肿瘤生长[1]。

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

Animal Model: Pt3R xenograft NOD.CB17-Prkdcscid/NCrCrl mice[1]
Dosage: 10-20 mg/kg
Administration: i.p., twice a week for 40 days
Result: Inhibited tumor growth.
分子量

680.83

Formula

C40H48N4O6
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

EZH2/HSP90-IN-29 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 *
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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:

EZH2/HSP90-IN-29Histone MethyltransferaseHSPApoptosisHeat shock proteinsPt3-RGBMCENPsInhibitorinhibitorinhibit

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