2. PROTAC Epigenetics Apoptosis Cell Cycle/DNA Damage
  3. PROTACs Histone Methyltransferase Bcl-2 Family Caspase PARP
  4. PROTAC EZH2 Degrader-44

PROTAC EZH2 Degrader-44 (compound 60) 是一种高效的、靶向 EZH2-PRC2 复合物的 PROTAC 降解剂。PROTAC EZH2 Degrader-44 通过募集 CRBN E3 连接酶并依赖蛋白酶体系统，同步诱导核心组分 EZH2、SUZ12 及 EED 的降解，进而显著降低 H3K27me3 和 CARM1 水平。PROTAC EZH2 Degrader-44 通过双重机制发挥抗增殖作用：一方面引发线粒体功能障碍导致膜电位降低，另一方面通过调控 Bcl-2 家族蛋白（上调 Bax、Caspase-3 和 PARP，下调 Bcl-2）强力促进细胞凋亡。PROTAC EZH2 Degrader-44 在人正常乳腺上皮、肝及肾细胞中仅表现出极低的细胞毒性，显示出良好的安全性窗口。PROTAC EZH2 Degrader-44 是探索三阴性乳腺癌靶向治疗机制的理想工具分子。

(粉色: Histone Methyltransferase 配体 (HY-147230)；蓝色: VHL 配体 (HY-125845)；黑色: )。

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PROTAC EZH2 Degrader-44

PROTAC EZH2 Degrader-44 Chemical Structure

CAS No. : 3093642-25-9

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PROTAC EZH2 Degrader-44 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

查看所有亚型
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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

查看 Bcl-2 Family 亚型特异性产品:

查看所有亚型
Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

查看 Caspase 亚型特异性产品:

查看所有亚型
Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

查看 PARP 亚型特异性产品:

查看所有亚型
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC EZH2 Degrader-44 (compound 60) is a highly efficient PROTAC degrader targeting the EZH2-PRC2 complex. By recruiting the CRBN E3 ligase and relying on the proteasome system, PROTAC EZH2 Degrader-44 simultaneously induces the degradation of core components EZH2, SUZ12 and EED, thereby significantly reducing the levels of H3K27me3 and CARM1. PROTAC EZH2 Degrader-44 exerts antiproliferative effects through a dual mechanism: on the one hand, it triggers mitochondrial dysfunction leading to decreased membrane potential; on the other hand, it strongly promotes apoptosis by regulating Bcl-2 family proteins (upregulating Bax, Caspase-3 and PARP, and downregulating Bcl-2). PROTAC EZH2 Degrader-44 exhibits only extremely low cytotoxicity in human normal mammary epithelial, liver and kidney cells, showing a favorable safety window. PROTAC EZH2 Degrader-44 is an ideal tool molecule for exploring the mechanisms of targeted therapy for triple-negative breast cancer[1].
(Pink: Histone Methyltransferase ligand (HY-147230); Blue: VHL ligand (HY-125845); Black: ).

IC50 & Target

EZH2

 

Caspase 3

 

体外研究
(In Vitro)

EZH2 是组蛋白甲基转移酶 (histone methyltransferase)，也是多梳抑制复合物 2（PRC2）的催化亚基。它通过转录抑制肿瘤抑制基因，在肿瘤表观遗传学中发挥“关键作用” (pivotal role)。EZH2 是一个在肿瘤发生发展中起核心调控作用的表观遗传酶，既是现有疗法的靶点，也是新一代蛋白降解技术 (PROTACs) 的重点研究对象[1]。

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

PROTAC EZH2 Degrader-44 相关抗体:
分子量

1193.50

Formula

C65H84N12O8S
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

PROTAC EZH2 Degrader-44 相关分类

  • 摩尔计算器

  • 稀释计算器

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浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
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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:

PROTAC EZH2 Degrader-443093642-25-9PROTACsHistone MethyltransferaseBcl-2 FamilyCaspasePARPpoly ADP ribose polymeraseH3K27me3SUZ12EZH2BaxEEDBcl-2cleaved caspase-3CARM1triple-negative breast cancerInhibitorinhibitorinhibit

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